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profilePhilip Arthur Cole, M.D.,Ph.D.

TitleProfessor of Medicine
InstitutionHarvard Insitutes of Medicine
DepartmentMedicine
AddressHarvard Medical School
Genetics BWH
77 Avenue Louis Pasteur
Boston MA 02115
Phone617/432-0930
vCardDownload vCard (login for email)
Other Positions
TitleProfessor of Biological Chemistry and Molecular Pharmacology
InstitutionHarvard Medical School
DepartmentBiological Chemistry & Molecular Pharmacology


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Collapse research activities and funding
The research activities and funding listed below are automatically derived from NIH ExPORTER and other sources, which might result in incorrect or missing items. Faculty can login to make corrections and additions.
R01GM099092     (LEAHY, DANIEL J)Mar 1, 2012 - Jan 31, 2016
NIH/NIGMS
Mechanistic Studies of EGFR/ErbB Receptor Tyrosine Kinases
Role: Co-Principal Investigator

R24DK093434     (COLE, PHILIP A)Sep 15, 2011 - Aug 31, 2013
NIH/NIDDK
Development and Application of Ghrelin O-acyltransferase Inhibitors
Role: Principal Investigator

R01AG019186     (COLE, PHILIP A)Apr 1, 2001 - Mar 31, 2010
NIH/NIA
Serotonin N-acethyltransferase Regulation &Inhibition
Role: Principal Investigator

R37GM062437     (COLE, PHILIP A)Feb 1, 2001 - Feb 28, 2023
NIH/NIGMS
Protein Acylation and Methylation Mechanisms
Role: Principal Investigator

R01GM062437     (COLE, PHILIP A)Feb 1, 2001 - Mar 31, 2013
NIH/NIGMS
Histone Modification Mechanisms and Inhibition
Role: Principal Investigator

Collapse Bibliographic 
Collapse selected publications
Publications listed below are automatically derived from MEDLINE/PubMed and other sources, which might result in incorrect or missing publications. Faculty can login to make corrections and additions.
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  1. Wang Z, Kim MS, Martinez-Ferrando I, Koleske AJ, Pandey A, Cole PA. Analysis of Cellular Tyrosine Phosphorylation via Chemical Rescue of Conditionally Active Abl Kinase. Biochemistry. 2018 Feb 27; 57(8):1390-1398. PMID: 29341593.
    View in: PubMed
  2. Kalin JH, Wu M, Gomez AV, Song Y, Das J, Hayward D, Adejola N, Wu M, Panova I, Chung HJ, Kim E, Roberts HJ, Roberts JM, Prusevich P, Jeliazkov JR, Roy Burman SS, Fairall L, Milano C, Eroglu A, Proby CM, Dinkova-Kostova AT, Hancock WW, Gray JJ, Bradner JE, Valente S, Mai A, Anders NM, Rudek MA, Hu Y, Ryu B, Schwabe JWR, Mattevi A, Alani RM, Cole PA. Targeting the CoREST complex with dual histone deacetylase and demethylase inhibitors. Nat Commun. 2018 01 04; 9(1):53. PMID: 29302039.
    View in: PubMed
  3. Michaelides MR, Kluge A, Patane M, Van Drie JH, Wang C, Hansen TM, Risi RM, Mantei R, Hertel C, Karukurichi K, Nesterov A, McElligott D, de Vries P, Langston JW, Cole PA, Marmorstein R, Liu H, Lasko L, Bromberg KD, Lai A, Kesicki EA. Discovery of Spiro Oxazolidinediones as Selective, Orally Bioavailable Inhibitors of p300/CBP Histone Acetyltransferases. ACS Med Chem Lett. 2018 Jan 11; 9(1):28-33. PMID: 29348807.
    View in: PubMed
  4. Esadze A, Rodriguez G, Weiser BP, Cole PA, Stivers JT. Measurement of nanoscale DNA translocation by uracil DNA glycosylase in human cells. Nucleic Acids Res. 2017 Dec 01; 45(21):12413-12424. PMID: 29036472.
    View in: PubMed
  5. Boija A, Mahat DB, Zare A, Holmqvist PH, Philip P, Meyers DJ, Cole PA, Lis JT, Stenberg P, Mannervik M. CBP Regulates Recruitment and Release of Promoter-Proximal RNA Polymerase II. Mol Cell. 2017 Nov 02; 68(3):491-503.e5. PMID: 29056321.
    View in: PubMed
  6. Lasko LM, Jakob CG, Edalji RP, Qiu W, Montgomery D, Digiammarino EL, Hansen TM, Risi RM, Frey R, Manaves V, Shaw B, Algire M, Hessler P, Lam LT, Uziel T, Faivre E, Ferguson D, Buchanan FG, Martin RL, Torrent M, Chiang GG, Karukurichi K, Langston JW, Weinert BT, Choudhary C, de Vries P, Van Drie JH, McElligott D, Kesicki E, Marmorstein R, Sun C, Cole PA, Rosenberg SH, Michaelides MR, Lai A, Bromberg KD. Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours. Nature. 2017 10 05; 550(7674):128-132. PMID: 28953875.
    View in: PubMed
  7. Rodriguez G, Esadze A, Weiser BP, Schonhoft JD, Cole PA, Stivers JT. Disordered N-Terminal Domain of Human Uracil DNA Glycosylase (hUNG2) Enhances DNA Translocation. ACS Chem Biol. 2017 09 15; 12(9):2260-2263. PMID: 28787572.
    View in: PubMed
  8. Cao J, Peng J, An H, He Q, Boronina T, Guo S, White MF, Cole PA, He L. Endotoxemia-mediated activation of acetyltransferase P300 impairs insulin signaling in obesity. Nat Commun. 2017 07 25; 8(1):131. PMID: 28743992.
    View in: PubMed
  9. Weiser BP, Stivers JT, Cole PA. Investigation of N-Terminal Phospho-Regulation of Uracil DNA Glycosylase Using Protein Semisynthesis. Biophys J. 2017 Jul 25; 113(2):393-401. PMID: 28746850.
    View in: PubMed
  10. Zucconi BE, Cole PA. Allosteric regulation of epigenetic modifying enzymes. Curr Opin Chem Biol. 2017 Aug; 39:109-115. PMID: 28689145.
    View in: PubMed
  11. Chen Z, Jiang H, Xu W, Li X, Dempsey DR, Zhang X, Devreotes P, Wolberger C, Amzel LM, Gabelli SB, Cole PA. A Tunable Brake for HECT Ubiquitin Ligases. Mol Cell. 2017 May 04; 66(3):345-357.e6. PMID: 28475870.
    View in: PubMed
  12. Mo GC, Ross B, Hertel F, Manna P, Yang X, Greenwald E, Booth C, Plummer AM, Tenner B, Chen Z, Wang Y, Kennedy EJ, Cole PA, Fleming KG, Palmer A, Jimenez R, Xiao J, Dedecker P, Zhang J. Genetically encoded biosensors for visualizing live-cell biochemical activity at super-resolution. Nat Methods. 2017 Apr; 14(4):427-434. PMID: 28288122.
    View in: PubMed
  13. Henry RA, Mancuso P, Kuo YM, Tricarico R, Tini M, Cole PA, Bellacosa A, Andrews AJ. Interaction with the DNA Repair Protein Thymine DNA Glycosylase Regulates Histone Acetylation by p300. Biochemistry. 2016 Dec 13; 55(49):6766-6775. PMID: 27951654.
    View in: PubMed
  14. Henager SH, Chu N, Chen Z, Bolduc D, Dempsey DR, Hwang Y, Wells J, Cole PA. Enzyme-catalyzed expressed protein ligation. Nat Methods. 2016 Nov; 13(11):925-927. PMID: 27669326.
    View in: PubMed
  15. Philip P, Boija A, Vaid R, Churcher AM, Meyers DJ, Cole PA, Mannervik M, Stenberg P. Erratum to: CBP binding outside of promoters and enhancers in Drosophila melanogaster. Epigenetics Chromatin. 2016; 9(1):38. PMID: 27625704; PMCID: PMC5020526.
  16. Hsiao PY, Kalin JH, Sun IH, Amin MN, Lo YC, Chiang MJ, Giddens J, Sysa-Shah P, Gabrielson K, Wang LX, Powell JD, Cole PA. An Fc-Small Molecule Conjugate for Targeted Inhibition of the Adenosine 2A Receptor. Chembiochem. 2016 10 17; 17(20):1951-1960. PMID: 27432157.
    View in: PubMed
  17. Zucconi BE, Luef B, Xu W, Henry RA, Nodelman IM, Bowman GD, Andrews AJ, Cole PA. Modulation of p300/CBP Acetylation of Nucleosomes by Bromodomain Ligand I-CBP112. Biochemistry. 2016 07 12; 55(27):3727-34. PMID: 27332697; PMCID: PMC5007619.
  18. Chen Z, Thomas SN, Bolduc DM, Jiang X, Zhang X, Wolberger C, Cole PA. Enzymatic Analysis of PTEN Ubiquitylation by WWP2 and NEDD4-1 E3 Ligases. Biochemistry. 2016 07 05; 55(26):3658-66. PMID: 27295432.
    View in: PubMed
  19. Dancy BM, Cole PA. Correction to Protein Lysine Acetylation by p300/CBP. Chem Rev. 2016 07 27; 116(14):8314. PMID: 27304234.
    View in: PubMed
  20. Chen Z, Dempsey DR, Thomas SN, Hayward D, Bolduc DM, Cole PA. Molecular Features of Phosphatase and Tensin Homolog (PTEN) Regulation by C-terminal Phosphorylation. J Biol Chem. 2016 Jul 01; 291(27):14160-9. PMID: 27226612; PMCID: PMC4933174 [Available on 07/01/17].
  21. Robert C, Nagaria PK, Pawar N, Adewuyi A, Gojo I, Meyers DJ, Cole PA, Rassool FV. Histone deacetylase inhibitors decrease NHEJ both by acetylation of repair factors and trapping of PARP1 at DNA double-strand breaks in chromatin. Leuk Res. 2016 06; 45:14-23. PMID: 27064363.
    View in: PubMed
  22. Hayward D, Cole PA. LSD1 Histone Demethylase Assays and Inhibition. Methods Enzymol. 2016; 573:261-78. PMID: 27372757.
    View in: PubMed
  23. Tu S, Guo SJ, Chen CS, Liu CX, Jiang HW, Ge F, Deng JY, Zhou YM, Czajkowsky DM, Li Y, Qi BR, Ahn YH, Cole PA, Zhu H, Tao SC. YcgC represents a new protein deacetylase family in prokaryotes. Elife. 2015 Dec 30; 4. PMID: 26716769; PMCID: PMC4709262.
  24. Philip P, Boija A, Vaid R, Churcher AM, Meyers DJ, Cole PA, Mannervik M, Stenberg P. CBP binding outside of promoters and enhancers in Drosophila melanogaster. Epigenetics Chromatin. 2015; 8:48. PMID: 26604986; PMCID: PMC4657240.
  25. Chen Z, Cole PA. Synthetic approaches to protein phosphorylation. Curr Opin Chem Biol. 2015 Oct; 28:115-22. PMID: 26196731; PMCID: PMC4624483 [Available on 10/01/16].
  26. Taylor MS, Dempsey DR, Hwang Y, Chen Z, Chu N, Boeke JD, Cole PA. Mechanistic analysis of ghrelin-O-acyltransferase using substrate analogs. Bioorg Chem. 2015 Oct; 62:64-73. PMID: 26246082; PMCID: PMC4567917 [Available on 10/01/16].
  27. Giotopoulos G, Chan WI, Horton SJ, Ruau D, Gallipoli P, Fowler A, Crawley C, Papaemmanuil E, Campbell PJ, Göttgens B, Van Deursen JM, Cole PA, Huntly BJ. The epigenetic regulators CBP and p300 facilitate leukemogenesis and represent therapeutic targets in acute myeloid leukemia. Oncogene. 2016 Jan 21; 35(3):279-89. PMID: 25893291; PMCID: PMC4729186.
  28. Chu N, Cole PA. Switching immune signals on and off. Elife. 2015 Apr 02; 4. PMID: 25838130; PMCID: PMC4384531.
  29. He C, Cole P. Introduction: epigenetics. Chem Rev. 2015 Mar 25; 115(6):2223-4. PMID: 25804907; PMCID: PMC4729185.
  30. Müller TD, Nogueiras R, Andermann ML, Andrews ZB, Anker SD, Argente J, Batterham RL, Benoit SC, Bowers CY, Broglio F, Casanueva FF, D'Alessio D, Depoortere I, Geliebter A, Ghigo E, Cole PA, Cowley M, Cummings DE, Dagher A, Diano S, Dickson SL, Diéguez C, Granata R, Grill HJ, Grove K, Habegger KM, Heppner K, Heiman ML, Holsen L, Holst B, Inui A, Jansson JO, Kirchner H, Korbonits M, Laferrère B, LeRoux CW, Lopez M, Morin S, Nakazato M, Nass R, Perez-Tilve D, Pfluger PT, Schwartz TW, Seeley RJ, Sleeman M, Sun Y, Sussel L, Tong J, Thorner MO, van der Lely AJ, van der Ploeg LH, Zigman JM, Kojima M, Kangawa K, Smith RG, Horvath T, Tschöp MH. Ghrelin. Mol Metab. 2015 Jun; 4(6):437-60. PMID: 26042199; PMCID: PMC4443295.
  31. Dancy BM, Cole PA. Protein lysine acetylation by p300/CBP. Chem Rev. 2015 Mar 25; 115(6):2419-52. PMID: 25594381; PMCID: PMC4378506.
  32. Leurs U, Lohse B, Ming S, Cole PA, Clausen RP, Kristensen JL, Rand KD. Dissecting the binding mode of low affinity phage display peptide ligands to protein targets by hydrogen/deuterium exchange coupled to mass spectrometry. Anal Chem. 2014 Dec 02; 86(23):11734-41. PMID: 25325890; PMCID: PMC4255673.
  33. Kavran JM, McCabe JM, Byrne PO, Connacher MK, Wang Z, Ramek A, Sarabipour S, Shan Y, Shaw DE, Hristova K, Cole PA, Leahy DJ. How IGF-1 activates its receptor. Elife. 2014 Sep 25; 3. PMID: 25255214.
    View in: PubMed
  34. Wang Y, Kavran JM, Chen Z, Karukurichi KR, Leahy DJ, Cole PA. Regulation of S-adenosylhomocysteine hydrolase by lysine acetylation. J Biol Chem. 2014 Nov 07; 289(45):31361-72. PMID: 25248746; PMCID: PMC4223336.
  35. Brown LJ, Baranowski M, Wang Y, Schrey AK, Lenz T, Taverna SD, Cole PA, Sefkow M. Using S-adenosyl-L-homocysteine capture compounds to characterize S-adenosyl-L-methionine and S-adenosyl-L-homocysteine binding proteins. Anal Biochem. 2014 Dec 15; 467:14-21. PMID: 25172130; PMCID: PMC4315328.
  36. Liu Y, Wang L, Han R, Beier UH, Akimova T, Bhatti T, Xiao H, Cole PA, Brindle PK, Hancock WW. Two histone/protein acetyltransferases, CBP and p300, are indispensable for Foxp3+ T-regulatory cell development and function. Mol Cell Biol. 2014 Nov; 34(21):3993-4007. PMID: 25154413; PMCID: PMC4386456.
  37. Miller MS, Schmidt-Kittler O, Bolduc DM, Brower ET, Chaves-Moreira D, Allaire M, Kinzler KW, Jennings IG, Thompson PE, Cole PA, Amzel LM, Vogelstein B, Gabelli SB. Structural basis of nSH2 regulation and lipid binding in PI3Ka. Oncotarget. 2014 Jul 30; 5(14):5198-208. PMID: 25105564; PMCID: PMC4170646.
  38. Leurs U, Lohse B, Rand KD, Ming S, Riise ES, Cole PA, Kristensen JL, Clausen RP. Substrate- and cofactor-independent inhibition of histone demethylase KDM4C. ACS Chem Biol. 2014 Sep 19; 9(9):2131-8. PMID: 25014588; PMCID: PMC4168794.
  39. Maksimoska J, Segura-Peña D, Cole PA, Marmorstein R. Structure of the p300 histone acetyltransferase bound to acetyl-coenzyme A and its analogues. Biochemistry. 2014 Jun 03; 53(21):3415-22. PMID: 24819397; PMCID: PMC4045318.
  40. Prusevich P, Kalin JH, Ming SA, Basso M, Givens J, Li X, Hu J, Taylor MS, Cieniewicz AM, Hsiao PY, Huang R, Roberson H, Adejola N, Avery LB, Casero RA, Taverna SD, Qian J, Tackett AJ, Ratan RR, McDonald OG, Feinberg AP, Cole PA. A selective phenelzine analogue inhibitor of histone demethylase LSD1. ACS Chem Biol. 2014 Jun 20; 9(6):1284-93. PMID: 24707965; PMCID: PMC4076021.
  41. Chiang MJ, Holbert MA, Kalin JH, Ahn YH, Giddens J, Amin MN, Taylor MS, Collins SL, Chan-Li Y, Waickman A, Hsiao PY, Bolduc D, Leahy DJ, Horton MR, Wang LX, Powell JD, Cole PA. An Fc domain protein-small molecule conjugate as an enhanced immunomodulator. J Am Chem Soc. 2014 Mar 05; 136(9):3370-3. PMID: 24533830; PMCID: PMC3954559.
  42. Wang Z, Cole PA. Catalytic mechanisms and regulation of protein kinases. Methods Enzymol. 2014; 548:1-21. PMID: 25399640; PMCID: PMC4373616.
  43. Wondisford AR, Xiong L, Chang E, Meng S, Meyers DJ, Li M, Cole PA, He L. Control of Foxo1 gene expression by co-activator P300. J Biol Chem. 2014 Feb 14; 289(7):4326-33. PMID: 24379407; PMCID: PMC3924295.
  44. Zhang Y, Dayalan Naidu S, Samarasinghe K, Van Hecke GC, Pheely A, Boronina TN, Cole RN, Benjamin IJ, Cole PA, Ahn YH, Dinkova-Kostova AT. Sulphoxythiocarbamates modify cysteine residues in HSP90 causing degradation of client proteins and inhibition of cancer cell proliferation. Br J Cancer. 2014 Jan 07; 110(1):71-82. PMID: 24322890; PMCID: PMC3887302.
  45. Schröder S, Herker E, Itzen F, He D, Thomas S, Gilchrist DA, Kaehlcke K, Cho S, Pollard KS, Capra JA, Schnölzer M, Cole PA, Geyer M, Bruneau BG, Adelman K, Ott M. Acetylation of RNA polymerase II regulates growth-factor-induced gene transcription in mammalian cells. Mol Cell. 2013 Nov 07; 52(3):314-24. PMID: 24207025; PMCID: PMC3936344.
  46. Taylor MS, Ruch TR, Hsiao PY, Hwang Y, Zhang P, Dai L, Huang CR, Berndsen CE, Kim MS, Pandey A, Wolberger C, Marmorstein R, Machamer C, Boeke JD, Cole PA. Architectural organization of the metabolic regulatory enzyme ghrelin O-acyltransferase. J Biol Chem. 2013 Nov 08; 288(45):32211-28. PMID: 24045953; PMCID: PMC3820860.
  47. Wang Z, Raines LL, Hooy RM, Roberson H, Leahy DJ, Cole PA. Tyrosine phosphorylation of mig6 reduces its inhibition of the epidermal growth factor receptor. ACS Chem Biol. 2013 Nov 15; 8(11):2372-6. PMID: 24004111; PMCID: PMC3830645.
  48. Liu Y, Wang L, Predina J, Han R, Beier UH, Wang LC, Kapoor V, Bhatti TR, Akimova T, Singhal S, Brindle PK, Cole PA, Albelda SM, Hancock WW. Inhibition of p300 impairs Foxp3? T regulatory cell function and promotes antitumor immunity. Nat Med. 2013 Sep; 19(9):1173-7. PMID: 23955711; PMCID: PMC3793393.
  49. Cole PA. Open questions: two challenges in chemical biology--chemical engineering and the science of diet. BMC Biol. 2013 Jul 30; 11:87. PMID: 23899134; PMCID: PMC3728078.
  50. Sugar JG, Chu QD, Cole PA, Li BD, Kim RH. Effect of January vacations and prior night call status on resident ABSITE performance. J Surg Educ. 2013 Nov-Dec; 70(6):720-4. PMID: 24209647.
    View in: PubMed
  51. Bolduc D, Rahdar M, Tu-Sekine B, Sivakumaren SC, Raben D, Amzel LM, Devreotes P, Gabelli SB, Cole P. Phosphorylation-mediated PTEN conformational closure and deactivation revealed with protein semisynthesis. Elife. 2013 Jul 09; 2:e00691. PMID: 23853711; PMCID: PMC3707082.
  52. Yan G, Eller MS, Elm C, Larocca CA, Ryu B, Panova IP, Dancy BM, Bowers EM, Meyers D, Lareau L, Cole PA, Taverna SD, Alani RM. Selective inhibition of p300 HAT blocks cell cycle progression, induces cellular senescence, and inhibits the DNA damage response in melanoma cells. J Invest Dermatol. 2013 Oct; 133(10):2444-2452. PMID: 23698071; PMCID: PMC4380234.
  53. Teubner BJ, Garretson JT, Hwang Y, Cole PA, Bartness TJ. Inhibition of ghrelin O-acyltransferase attenuates food deprivation-induced increases in ingestive behavior. Horm Behav. 2013 Apr; 63(4):667-73. PMID: 23399323; PMCID: PMC3633643.
  54. Newman RH, Hu J, Rho HS, Xie Z, Woodard C, Neiswinger J, Cooper C, Shirley M, Clark HM, Hu S, Hwang W, Jeong JS, Wu G, Lin J, Gao X, Ni Q, Goel R, Xia S, Ji H, Dalby KN, Birnbaum MJ, Cole PA, Knapp S, Ryazanov AG, Zack DJ, Blackshaw S, Pawson T, Gingras AC, Desiderio S, Pandey A, Turk BE, Zhang J, Zhu H, Qian J. Construction of human activity-based phosphorylation networks. Mol Syst Biol. 2013; 9:655. PMID: 23549483; PMCID: PMC3658267.
  55. Dancy BM, Crump NT, Peterson DJ, Mukherjee C, Bowers EM, Ahn YH, Yoshida M, Zhang J, Mahadevan LC, Meyers DJ, Boeke JD, Cole PA. Live-cell studies of p300/CBP histone acetyltransferase activity and inhibition. Chembiochem. 2012 Sep 24; 13(14):2113-21. PMID: 22961914; PMCID: PMC3517098.
  56. Wei W, Coelho CM, Li X, Marek R, Yan S, Anderson S, Meyers D, Mukherjee C, Sbardella G, Castellano S, Milite C, Rotili D, Mai A, Cole PA, Sah P, Kobor MS, Bredy TW. p300/CBP-associated factor selectively regulates the extinction of conditioned fear. J Neurosci. 2012 Aug 29; 32(35):11930-41. PMID: 22933779; PMCID: PMC3466419.
  57. Ferrando IM, Chaerkady R, Zhong J, Molina H, Jacob HK, Herbst-Robinson K, Dancy BM, Katju V, Bose R, Zhang J, Pandey A, Cole PA. Identification of targets of c-Src tyrosine kinase by chemical complementation and phosphoproteomics. Mol Cell Proteomics. 2012 Aug; 11(8):355-69. PMID: 22499769; PMCID: PMC3412967.
  58. Wang Y, Toh HC, Chow P, Chung AY, Meyers DJ, Cole PA, Ooi LL, Lee CG. MicroRNA-224 is up-regulated in hepatocellular carcinoma through epigenetic mechanisms. FASEB J. 2012 Jul; 26(7):3032-41. PMID: 22459148; PMCID: PMC3382089.
  59. Francetic T, Le May M, Hamed M, Mach H, Meyers D, Cole PA, Chen J, Li Q. Regulation of Myf5 Early Enhancer by Histone Acetyltransferase p300 during Stem Cell Differentiation. Mol Biol. 2012 Mar 17; 1. PMID: 25382872.
    View in: PubMed
  60. Dancy BC, Ming SA, Papazyan R, Jelinek CA, Majumdar A, Sun Y, Dancy BM, Drury WJ, Cotter RJ, Taverna SD, Cole PA. Azalysine analogues as probes for protein lysine deacetylation and demethylation. J Am Chem Soc. 2012 Mar 21; 134(11):5138-48. PMID: 22352831; PMCID: PMC3313494.
  61. Tarrant MK, Rho HS, Xie Z, Jiang YL, Gross C, Culhane JC, Yan G, Qian J, Ichikawa Y, Matsuoka T, Zachara N, Etzkorn FA, Hart GW, Jeong JS, Blackshaw S, Zhu H, Cole PA. Regulation of CK2 by phosphorylation and O-GlcNAcylation revealed by semisynthesis. Nat Chem Biol. 2012 Jan 22; 8(3):262-9. PMID: 22267120; PMCID: PMC3288285.
  62. Taylor MS, Hwang Y, Hsiao PY, Boeke JD, Cole PA. Ghrelin O-acyltransferase assays and inhibition. Methods Enzymol. 2012; 514:205-28. PMID: 22975055; PMCID: PMC3763810.
  63. Zhang Y, Ahn YH, Benjamin IJ, Honda T, Hicks RJ, Calabrese V, Cole PA, Dinkova-Kostova AT. HSF1-dependent upregulation of Hsp70 by sulfhydryl-reactive inducers of the KEAP1/NRF2/ARE pathway. Chem Biol. 2011 Nov 23; 18(11):1355-61. PMID: 22118669; PMCID: PMC3302153.
  64. Wang Z, Longo PA, Tarrant MK, Kim K, Head S, Leahy DJ, Cole PA. Mechanistic insights into the activation of oncogenic forms of EGF receptor. Nat Struct Mol Biol. 2011 Nov 20; 18(12):1388-93. PMID: 22101934; PMCID: PMC3230693.
  65. Wang L, Gural A, Sun XJ, Zhao X, Perna F, Huang G, Hatlen MA, Vu L, Liu F, Xu H, Asai T, Xu H, Deblasio T, Menendez S, Voza F, Jiang Y, Cole PA, Zhang J, Melnick A, Roeder RG, Nimer SD. The leukemogenicity of AML1-ETO is dependent on site-specific lysine acetylation. Science. 2011 Aug 05; 333(6043):765-9. PMID: 21764752; PMCID: PMC3251012.
  66. Santer FR, Höschele PP, Oh SJ, Erb HH, Bouchal J, Cavarretta IT, Parson W, Meyers DJ, Cole PA, Culig Z. Inhibition of the acetyltransferases p300 and CBP reveals a targetable function for p300 in the survival and invasion pathways of prostate cancer cell lines. Mol Cancer Ther. 2011 Sep; 10(9):1644-55. PMID: 21709130.
    View in: PubMed
  67. Smirnova NA, Haskew-Layton RE, Basso M, Hushpulian DM, Payappilly JB, Speer RE, Ahn YH, Rakhman I, Cole PA, Pinto JT, Ratan RR, Gazaryan IG. Development of Neh2-luciferase reporter and its application for high throughput screening and real-time monitoring of Nrf2 activators. Chem Biol. 2011 Jun 24; 18(6):752-65. PMID: 21700211; PMCID: PMC3251032.
  68. Wirdefeldt K, Adami HO, Cole P, Trichopoulos D, Mandel J. Epidemiology and etiology of Parkinson's disease: a review of the evidence. Eur J Epidemiol. 2011 Jun; 26 Suppl 1:S1-58. PMID: 21626386.
    View in: PubMed
  69. Xu CR, Cole PA, Meyers DJ, Kormish J, Dent S, Zaret KS. Chromatin "prepattern" and histone modifiers in a fate choice for liver and pancreas. Science. 2011 May 20; 332(6032):963-6. PMID: 21596989; PMCID: PMC3128430.
  70. Marek R, Coelho CM, Sullivan RK, Baker-Andresen D, Li X, Ratnu V, Dudley KJ, Meyers D, Mukherjee C, Cole PA, Sah P, Bredy TW. Paradoxical enhancement of fear extinction memory and synaptic plasticity by inhibition of the histone acetyltransferase p300. J Neurosci. 2011 May 18; 31(20):7486-91. PMID: 21593332; PMCID: PMC3458795.
  71. Crump NT, Hazzalin CA, Bowers EM, Alani RM, Cole PA, Mahadevan LC. Dynamic acetylation of all lysine-4 trimethylated histone H3 is evolutionarily conserved and mediated by p300/CBP. Proc Natl Acad Sci U S A. 2011 May 10; 108(19):7814-9. PMID: 21518915; PMCID: PMC3093510.
  72. Collins SL, Black KE, Chan-Li Y, Ahn YH, Cole PA, Powell JD, Horton MR. Hyaluronan fragments promote inflammation by down-regulating the anti-inflammatory A2a receptor. Am J Respir Cell Mol Biol. 2011 Oct; 45(4):675-83. PMID: 21257926; PMCID: PMC3208614.
  73. Tang Y, Holbert MA, Delgoshaie N, Wurtele H, Guillemette B, Meeth K, Yuan H, Drogaris P, Lee EH, Durette C, Thibault P, Verreault A, Cole PA, Marmorstein R. Structure of the Rtt109-AcCoA/Vps75 complex and implications for chaperone-mediated histone acetylation. Structure. 2011 Feb 09; 19(2):221-31. PMID: 21256037; PMCID: PMC3050538.
  74. Taverna SD, Cole PA. Drug discovery: Reader's block. Nature. 2010 Dec 23; 468(7327):1050-1. PMID: 21179160.
    View in: PubMed
  75. Barnett BP, Hwang Y, Taylor MS, Kirchner H, Pfluger PT, Bernard V, Lin YY, Bowers EM, Mukherjee C, Song WJ, Longo PA, Leahy DJ, Hussain MA, Tschöp MH, Boeke JD, Cole PA. Glucose and weight control in mice with a designed ghrelin O-acyltransferase inhibitor. Science. 2010 Dec 17; 330(6011):1689-92. PMID: 21097901; PMCID: PMC3068526.
  76. Bellows ML, Taylor MS, Cole PA, Shen L, Siliciano RF, Fung HK, Floudas CA. Discovery of entry inhibitors for HIV-1 via a new de novo protein design framework. Biophys J. 2010 Nov 17; 99(10):3445-53. PMID: 21081094; PMCID: PMC2980751.
  77. Cerchietti LC, Hatzi K, Caldas-Lopes E, Yang SN, Figueroa ME, Morin RD, Hirst M, Mendez L, Shaknovich R, Cole PA, Bhalla K, Gascoyne RD, Marra M, Chiosis G, Melnick A. BCL6 repression of EP300 in human diffuse large B cell lymphoma cells provides a basis for rational combinatorial therapy. J Clin Invest. 2010 Dec 01; 120(12):4569-82. PMID: 21041953.
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  78. Karukurichi KR, Cole PA. Probing the reaction coordinate of the p300/CBP histone acetyltransferase with bisubstrate analogs. Bioorg Chem. 2011 Feb; 39(1):42-7. PMID: 21111442; PMCID: PMC3076313.
  79. Min SW, Cho SH, Zhou Y, Schroeder S, Haroutunian V, Seeley WW, Huang EJ, Shen Y, Masliah E, Mukherjee C, Meyers D, Cole PA, Ott M, Gan L. Acetylation of tau inhibits its degradation and contributes to tauopathy. Neuron. 2010 Sep 23; 67(6):953-66. PMID: 20869593; PMCID: PMC3035103.
  80. Reynoird N, Schwartz BE, Delvecchio M, Sadoul K, Meyers D, Mukherjee C, Caron C, Kimura H, Rousseaux S, Cole PA, Panne D, French CA, Khochbin S. Oncogenesis by sequestration of CBP/p300 in transcriptionally inactive hyperacetylated chromatin domains. EMBO J. 2010 Sep 01; 29(17):2943-52. PMID: 20676058; PMCID: PMC2944051.
  81. Huang R, Holbert MA, Tarrant MK, Curtet S, Colquhoun DR, Dancy BM, Dancy BC, Hwang Y, Tang Y, Meeth K, Marmorstein R, Cole RN, Khochbin S, Cole PA. Site-specific introduction of an acetyl-lysine mimic into peptides and proteins by cysteine alkylation. J Am Chem Soc. 2010 Jul 28; 132(29):9986-7. PMID: 20608637; PMCID: PMC2912447.
  82. Huang R, Martinez-Ferrando I, Cole PA. Enhanced interrogation: emerging strategies for cell signaling inhibition. Nat Struct Mol Biol. 2010 Jun; 17(6):646-9. PMID: 20520657; PMCID: PMC3160762.
  83. Bowers EM, Yan G, Mukherjee C, Orry A, Wang L, Holbert MA, Crump NT, Hazzalin CA, Liszczak G, Yuan H, Larocca C, Saldanha SA, Abagyan R, Sun Y, Meyers DJ, Marmorstein R, Mahadevan LC, Alani RM, Cole PA. Virtual ligand screening of the p300/CBP histone acetyltransferase: identification of a selective small molecule inhibitor. Chem Biol. 2010 May 28; 17(5):471-82. PMID: 20534345; PMCID: PMC2884008.
  84. Ahn YH, Hwang Y, Liu H, Wang XJ, Zhang Y, Stephenson KK, Boronina TN, Cole RN, Dinkova-Kostova AT, Talalay P, Cole PA. Electrophilic tuning of the chemoprotective natural product sulforaphane. Proc Natl Acad Sci U S A. 2010 May 25; 107(21):9590-5. PMID: 20439747; PMCID: PMC2906893.
  85. Mali P, Chou BK, Yen J, Ye Z, Zou J, Dowey S, Brodsky RA, Ohm JE, Yu W, Baylin SB, Yusa K, Bradley A, Meyers DJ, Mukherjee C, Cole PA, Cheng L. Butyrate greatly enhances derivation of human induced pluripotent stem cells by promoting epigenetic remodeling and the expression of pluripotency-associated genes. Stem Cells. 2010 Apr; 28(4):713-20. PMID: 20201064; PMCID: PMC3015217.
  86. Culhane JC, Wang D, Yen PM, Cole PA. Comparative analysis of small molecules and histone substrate analogues as LSD1 lysine demethylase inhibitors. J Am Chem Soc. 2010 Mar 10; 132(9):3164-76. PMID: 20148560; PMCID: PMC2843942.
  87. Karukurichi KR, Wang L, Uzasci L, Manlandro CM, Wang Q, Cole PA. Analysis of p300/CBP histone acetyltransferase regulation using circular permutation and semisynthesis. J Am Chem Soc. 2010 Feb 03; 132(4):1222-3. PMID: 20063892; PMCID: PMC2811879.
  88. Qiu C, Tarrant MK, Boronina T, Longo PA, Kavran JM, Cole RN, Cole PA, Leahy DJ. In vitro enzymatic characterization of near full length EGFR in activated and inhibited states. Biochemistry. 2009 Jul 21; 48(28):6624-32. PMID: 19518076; PMCID: PMC2747374.
  89. Oussaief L, Hippocrate A, Ramirez V, Rampanou A, Zhang W, Meyers D, Cole P, Khelifa R, Joab I. Phosphatidylinositol 3-kinase/Akt pathway targets acetylation of Smad3 through Smad3/CREB-binding protein interaction: contribution to transforming growth factor beta1-induced Epstein-Barr virus reactivation. J Biol Chem. 2009 Sep 04; 284(36):23912-24. PMID: 19589780; PMCID: PMC2781985.
  90. Muratore KE, Seeliger MA, Wang Z, Fomina D, Neiswinger J, Havranek JJ, Baker D, Kuriyan J, Cole PA. Comparative analysis of mutant tyrosine kinase chemical rescue. Biochemistry. 2009 Apr 21; 48(15):3378-86. PMID: 19260709; PMCID: PMC2714740.
  91. Hansson ML, Popko-Scibor AE, Saint Just Ribeiro M, Dancy BM, Lindberg MJ, Cole PA, Wallberg AE. The transcriptional coactivator MAML1 regulates p300 autoacetylation and HAT activity. Nucleic Acids Res. 2009 May; 37(9):2996-3006. PMID: 19304754; PMCID: PMC2685096.
  92. Wang D, Xia X, Liu Y, Oetting A, Walker RL, Zhu Y, Meltzer P, Cole PA, Shi YB, Yen PM. Negative regulation of TSHalpha target gene by thyroid hormone involves histone acetylation and corepressor complex dissociation. Mol Endocrinol. 2009 May; 23(5):600-9. PMID: 19196836; PMCID: PMC2675953.
  93. Szewczuk LM, Tarrant MK, Cole PA. Protein phosphorylation by semisynthesis: from paper to practice. Methods Enzymol. 2009; 462:1-24. PMID: 19632467; PMCID: PMC3074177.
  94. Tarrant MK, Cole PA. The chemical biology of protein phosphorylation. Annu Rev Biochem. 2009; 78:797-825. PMID: 19489734; PMCID: PMC3074175.
  95. Wang L, Tang Y, Cole PA, Marmorstein R. Structure and chemistry of the p300/CBP and Rtt109 histone acetyltransferases: implications for histone acetyltransferase evolution and function. Curr Opin Struct Biol. 2008 Dec; 18(6):741-7. PMID: 18845255; PMCID: PMC2643075.
  96. Cole PA. Chemical probes for histone-modifying enzymes. Nat Chem Biol. 2008 Oct; 4(10):590-7. PMID: 18800048; PMCID: PMC2908280.
  97. Szewczuk LM, Tarrant MK, Sample V, Drury WJ, Zhang J, Cole PA. Analysis of serotonin N-acetyltransferase regulation in vitro and in live cells using protein semisynthesis. Biochemistry. 2008 Sep 30; 47(39):10407-19. PMID: 18771288; PMCID: PMC2682328.
  98. Levinson NM, Seeliger MA, Cole PA, Kuriyan J. Structural basis for the recognition of c-Src by its inactivator Csk. Cell. 2008 Jul 11; 134(1):124-34. PMID: 18614016; PMCID: PMC2494536.
  99. Tang Y, Holbert MA, Wurtele H, Meeth K, Rocha W, Gharib M, Jiang E, Thibault P, Verreault A, Verrault A, Cole PA, Marmorstein R. Fungal Rtt109 histone acetyltransferase is an unexpected structural homolog of metazoan p300/CBP. Nat Struct Mol Biol. 2008 Jul; 15(7):738-45. PMID: 18568037; PMCID: PMC2574607.
  100. Pickin KA, Chaudhury S, Dancy BC, Gray JJ, Cole PA. Analysis of protein kinase autophosphorylation using expressed protein ligation and computational modeling. J Am Chem Soc. 2008 Apr 30; 130(17):5667-9. PMID: 18396877; PMCID: PMC2654778.
  101. Qiu C, Tarrant MK, Choi SH, Sathyamurthy A, Bose R, Banjade S, Pal A, Bornmann WG, Lemmon MA, Cole PA, Leahy DJ. Mechanism of activation and inhibition of the HER4/ErbB4 kinase. Structure. 2008 Mar; 16(3):460-7. PMID: 18334220; PMCID: PMC2858219.
  102. MacMahon B, Cole P. Is the incidence of breast cancer declining? Epidemiology. 2008 Mar; 19(2):268-9. PMID: 18277162.
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  103. Liu X, Wang L, Zhao K, Thompson PR, Hwang Y, Marmorstein R, Cole PA. The structural basis of protein acetylation by the p300/CBP transcriptional coactivator. Nature. 2008 Feb 14; 451(7180):846-50. PMID: 18273021.
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  104. Mathivanan S, Ahmed M, Ahn NG, Alexandre H, Amanchy R, Andrews PC, Bader JS, Balgley BM, Bantscheff M, Bennett KL, Björling E, Blagoev B, Bose R, Brahmachari SK, Burlingame AS, Bustelo XR, Cagney G, Cantin GT, Cardasis HL, Celis JE, Chaerkady R, Chu F, Cole PA, Costello CE, Cotter RJ, Crockett D, DeLany JP, De Marzo AM, DeSouza LV, Deutsch EW, Dransfield E, Drewes G, Droit A, Dunn MJ, Elenitoba-Johnson K, Ewing RM, Van Eyk J, Faca V, Falkner J, Fang X, Fenselau C, Figeys D, Gagné P, Gelfi C, Gevaert K, Gimble JM, Gnad F, Goel R, Gromov P, Hanash SM, Hancock WS, Harsha HC, Hart G, Hays F, He F, Hebbar P, Helsens K, Hermeking H, Hide W, Hjernø K, Hochstrasser DF, Hofmann O, Horn DM, Hruban RH, Ibarrola N, James P, Jensen ON, Jensen PH, Jung P, Kandasamy K, Kheterpal I, Kikuno RF, Korf U, Körner R, Kuster B, Kwon MS, Lee HJ, Lee YJ, Lefevre M, Lehvaslaiho M, Lescuyer P, Levander F, Lim MS, Löbke C, Loo JA, Mann M, Martens L, Martinez-Heredia J, McComb M, McRedmond J, Mehrle A, Menon R, Miller CA, Mischak H, Mohan SS, Mohmood R, Molina H, Moran MF, Morgan JD, Moritz R, Morzel M, Muddiman DC, Nalli A, Navarro JD, Neubert TA, Ohara O, Oliva R, Omenn GS, Oyama M, Paik YK, Pennington K, Pepperkok R, Periaswamy B, Petricoin EF, Poirier GG, Prasad TS, Purvine SO, Rahiman BA, Ramachandran P, Ramachandra YL, Rice RH, Rick J, Ronnholm RH, Salonen J, Sanchez JC, Sayd T, Seshi B, Shankari K, Sheng SJ, Shetty V, Shivakumar K, Simpson RJ, Sirdeshmukh R, Siu KW, Smith JC, Smith RD, States DJ, Sugano S, Sullivan M, Superti-Furga G, Takatalo M, Thongboonkerd V, Trinidad JC, Uhlen M, Vandekerckhove J, Vasilescu J, Veenstra TD, Vidal-Taboada JM, Vihinen M, Wait R, Wang X, Wiemann S, Wu B, Xu T, Yates JR, Zhong J, Zhou M, Zhu Y, Zurbig P, Pandey A. Human Proteinpedia enables sharing of human protein data. Nat Biotechnol. 2008 Feb; 26(2):164-7. PMID: 18259167.
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  105. Zhang X, Pickin KA, Bose R, Jura N, Cole PA, Kuriyan J. Inhibition of the EGF receptor by binding of MIG6 to an activating kinase domain interface. Nature. 2007 Nov 29; 450(7170):741-4. PMID: 18046415; PMCID: PMC3561764.
  106. Szewczuk LM, Saldanha SA, Ganguly S, Bowers EM, Javoroncov M, Karanam B, Culhane JC, Holbert MA, Klein DC, Abagyan R, Cole PA. De novo discovery of serotonin N-acetyltransferase inhibitors. J Med Chem. 2007 Nov 01; 50(22):5330-8. PMID: 17924613; PMCID: PMC2531295.
  107. Culhane JC, Cole PA. LSD1 and the chemistry of histone demethylation. Curr Opin Chem Biol. 2007 Oct; 11(5):561-8. PMID: 17851108; PMCID: PMC2112775.
  108. Kenneth NS, Ramsbottom BA, Gomez-Roman N, Marshall L, Cole PA, White RJ. TRRAP and GCN5 are used by c-Myc to activate RNA polymerase III transcription. Proc Natl Acad Sci U S A. 2007 Sep 18; 104(38):14917-22. PMID: 17848523; PMCID: PMC1986588.
  109. Muratore KE, Cole PA. A lock on phosphotyrosine signaling. ACS Chem Biol. 2007 Jul 20; 2(7):454-6. PMID: 17649969.
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  110. Hu X, Dang Y, Tenney K, Crews P, Tsai CW, Sixt KM, Cole PA, Liu JO. Regulation of c-Src nonreceptor tyrosine kinase activity by bengamide A through inhibition of methionine aminopeptidases. Chem Biol. 2007 Jul; 14(7):764-74. PMID: 17656313; PMCID: PMC3165037.
  111. Karanam B, Wang L, Wang D, Liu X, Marmorstein R, Cotter R, Cole PA. Multiple roles for acetylation in the interaction of p300 HAT with ATF-2. Biochemistry. 2007 Jul 17; 46(28):8207-16. PMID: 17590016; PMCID: PMC2532843.
  112. Yang M, Culhane JC, Szewczuk LM, Jalili P, Ball HL, Machius M, Cole PA, Yu H. Structural basis for the inhibition of the LSD1 histone demethylase by the antidepressant trans-2-phenylcyclopropylamine. Biochemistry. 2007 Jul 10; 46(27):8058-65. PMID: 17569509.
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  113. Yang M, Culhane JC, Szewczuk LM, Gocke CB, Brautigam CA, Tomchick DR, Machius M, Cole PA, Yu H. Structural basis of histone demethylation by LSD1 revealed by suicide inactivation. Nat Struct Mol Biol. 2007 Jun; 14(6):535-9. PMID: 17529991.
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  114. Szewczuk LM, Culhane JC, Yang M, Majumdar A, Yu H, Cole PA. Mechanistic analysis of a suicide inactivator of histone demethylase LSD1. Biochemistry. 2007 Jun 12; 46(23):6892-902. PMID: 17511474; PMCID: PMC2531293.
  115. Hwang Y, Thompson PR, Wang L, Jiang L, Kelleher NL, Cole PA. A selective chemical probe for coenzyme A-requiring enzymes. Angew Chem Int Ed Engl. 2007; 46(40):7621-4. PMID: 17768748.
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  116. Hwang Y, Ganguly S, Ho AK, Klein DC, Cole PA. Enzymatic and cellular study of a serotonin N-acetyltransferase phosphopantetheine-based prodrug. Bioorg Med Chem. 2007 Mar 01; 15(5):2147-55. PMID: 17258461; PMCID: PMC1831523.
  117. Bose R, Holbert MA, Pickin KA, Cole PA. Protein tyrosine kinase-substrate interactions. Curr Opin Struct Biol. 2006 Dec; 16(6):668-75. PMID: 17085043.
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  118. Karanam B, Jiang L, Wang L, Kelleher NL, Cole PA. Kinetic and mass spectrometric analysis of p300 histone acetyltransferase domain autoacetylation. J Biol Chem. 2006 Dec 29; 281(52):40292-301. PMID: 17065153.
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  119. Bose R, Molina H, Patterson AS, Bitok JK, Periaswamy B, Bader JS, Pandey A, Cole PA. Phosphoproteomic analysis of Her2/neu signaling and inhibition. Proc Natl Acad Sci U S A. 2006 Jun 27; 103(26):9773-8. PMID: 16785428; PMCID: PMC1502529.
  120. Zhang X, Gureasko J, Shen K, Cole PA, Kuriyan J. An allosteric mechanism for activation of the kinase domain of epidermal growth factor receptor. Cell. 2006 Jun 16; 125(6):1137-49. PMID: 16777603.
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  121. Cheng KY, Noble ME, Skamnaki V, Brown NR, Lowe ED, Kontogiannis L, Shen K, Cole PA, Siligardi G, Johnson LN. The role of the phospho-CDK2/cyclin A recruitment site in substrate recognition. J Biol Chem. 2006 Aug 11; 281(32):23167-79. PMID: 16707497.
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  122. Levinson NM, Kuchment O, Shen K, Young MA, Koldobskiy M, Karplus M, Cole PA, Kuriyan J. A Src-like inactive conformation in the abl tyrosine kinase domain. PLoS Biol. 2006 May; 4(5):e144. PMID: 16640460; PMCID: PMC1450098.
  123. Culhane JC, Szewczuk LM, Liu X, Da G, Marmorstein R, Cole PA. A mechanism-based inactivator for histone demethylase LSD1. J Am Chem Soc. 2006 Apr 12; 128(14):4536-7. PMID: 16594666.
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  124. Schwarzer D, Zhang Z, Zheng W, Cole PA. Negative regulation of a protein tyrosine phosphatase by tyrosine phosphorylation. J Am Chem Soc. 2006 Apr 05; 128(13):4192-3. PMID: 16568970.
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  125. Qiao Y, Molina H, Pandey A, Zhang J, Cole PA. Chemical rescue of a mutant enzyme in living cells. Science. 2006 Mar 03; 311(5765):1293-7. PMID: 16513984.
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  126. Zheng Y, Balasubramanyam K, Cebrat M, Buck D, Guidez F, Zelent A, Alani RM, Cole PA. Synthesis and evaluation of a potent and selective cell-permeable p300 histone acetyltransferase inhibitor. J Am Chem Soc. 2005 Dec 14; 127(49):17182-3. PMID: 16332055.
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  127. Schwarzer D, Cole PA. Protein semisynthesis and expressed protein ligation: chasing a protein's tail. Curr Opin Chem Biol. 2005 Dec; 9(6):561-9. PMID: 16226484.
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  128. Lewczuk B, Zheng W, Prusik M, Cole PA, Przybylska-Gornowicz B. N-bromoacetyltryptamine strongly and reversibly inhibits in vitro melatonin secretion from mammalian pinealocytes. Neuro Endocrinol Lett. 2005 Oct; 26(5):581-92. PMID: 16264397.
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  129. Shen K, Hines AC, Schwarzer D, Pickin KA, Cole PA. Protein kinase structure and function analysis with chemical tools. Biochim Biophys Acta. 2005 Dec 30; 1754(1-2):65-78. PMID: 16213197.
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  130. Zheng Y, Mamdani F, Toptygin D, Brand L, Stivers JT, Cole PA. Fluorescence analysis of a dynamic loop in the PCAF/GCN5 histone acetyltransferase. Biochemistry. 2005 Aug 09; 44(31):10501-9. PMID: 16060659.
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  131. Guidez F, Howell L, Isalan M, Cebrat M, Alani RM, Ivins S, Hormaeche I, McConnell MJ, Pierce S, Cole PA, Licht J, Zelent A. Histone acetyltransferase activity of p300 is required for transcriptional repression by the promyelocytic leukemia zinc finger protein. Mol Cell Biol. 2005 Jul; 25(13):5552-66. PMID: 15964811; PMCID: PMC1156991.
  132. Cleary J, Sitwala KV, Khodadoust MS, Kwok RP, Mor-Vaknin N, Cebrat M, Cole PA, Markovitz DM. p300/CBP-associated factor drives DEK into interchromatin granule clusters. J Biol Chem. 2005 Sep 09; 280(36):31760-7. PMID: 15987677.
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  133. Wang D, Thompson P, Cole PA, Cotter RJ. Structural analysis of a highly acetylated protein using a curved-field reflectron mass spectrometer. Proteomics. 2005 Jun; 5(9):2288-96. PMID: 15887180.
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  134. Hines AC, Parang K, Kohanski RA, Hubbard SR, Cole PA. Bisubstrate analog probes for the insulin receptor protein tyrosine kinase: molecular yardsticks for analyzing catalytic mechanism and inhibitor design. Bioorg Chem. 2005 Aug; 33(4):285-97. PMID: 16023488.
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  135. Cheung E, Acevedo ML, Cole PA, Kraus WL. Altered pharmacology and distinct coactivator usage for estrogen receptor-dependent transcription through activating protein-1. Proc Natl Acad Sci U S A. 2005 Jan 18; 102(3):559-64. PMID: 15642950; PMCID: PMC545529.
  136. Zheng W, Schwarzer D, Lebeau A, Weller JL, Klein DC, Cole PA. Cellular stability of serotonin N-acetyltransferase conferred by phosphonodifluoromethylene alanine (Pfa) substitution for Ser-205. J Biol Chem. 2005 Mar 18; 280(11):10462-7. PMID: 15632116.
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  137. Yoon HG, Choi Y, Cole PA, Wong J. Reading and function of a histone code involved in targeting corepressor complexes for repression. Mol Cell Biol. 2005 Jan; 25(1):324-35. PMID: 15601853; PMCID: PMC538779.
  138. Shi Y, Lan F, Matson C, Mulligan P, Whetstine JR, Cole PA, Casero RA, Shi Y. Histone demethylation mediated by the nuclear amine oxidase homolog LSD1. Cell. 2004 Dec 29; 119(7):941-53. PMID: 15620353.
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  139. Casanova M, Cole P, Collins JJ, Conolly R, Delzell E, Heck Hd Hd, Leonard R, Lewis R, Marsh GM, Ott MG, Sorahan T, Axten CW. Re: Mortality from lymphohematopoietic malignancies among workers in formaldehyde industries. J Natl Cancer Inst. 2004 Jun 16; 96(12):966-7; author reply 967-8. PMID: 15199116.
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  140. Sagar V, Zheng W, Thompson PR, Cole PA. Bisubstrate analogue structure-activity relationships for p300 histone acetyltransferase inhibitors. Bioorg Med Chem. 2004 Jun 15; 12(12):3383-90. PMID: 15158807.
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  141. Hines AC, Cole PA. Design, synthesis, and characterization of an ATP-peptide conjugate inhibitor of protein kinase A. Bioorg Med Chem Lett. 2004 Jun 07; 14(11):2951-4. PMID: 15125966.
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  142. Hwang Y, Cole PA. Efficient synthesis of phosphorylated prodrugs with bis(POM)-phosphoryl chloride. Org Lett. 2004 May 13; 6(10):1555-6. PMID: 15128234.
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  143. Farrell CJ, Lee JM, Shin EC, Cebrat M, Cole PA, Hayward SD. Inhibition of Epstein-Barr virus-induced growth proliferation by a nuclear antigen EBNA2-TAT peptide. Proc Natl Acad Sci U S A. 2004 Mar 30; 101(13):4625-30. PMID: 15070768; PMCID: PMC384797.
  144. Thompson PR, Wang D, Wang L, Fulco M, Pediconi N, Zhang D, An W, Ge Q, Roeder RG, Wong J, Levrero M, Sartorelli V, Cotter RJ, Cole PA. Regulation of the p300 HAT domain via a novel activation loop. Nat Struct Mol Biol. 2004 Apr; 11(4):308-15. PMID: 15004546.
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  145. Zheng Y, Thompson PR, Cebrat M, Wang L, Devlin MK, Alani RM, Cole PA. Selective HAT inhibitors as mechanistic tools for protein acetylation. Methods Enzymol. 2004; 376:188-99. PMID: 14975306.
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  146. Shen K, Cole PA. Conversion of a tyrosine kinase protein substrate to a high affinity ligand by ATP linkage. J Am Chem Soc. 2003 Dec 31; 125(52):16172-3. PMID: 14692742.
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  147. Zheng W, Zhang Z, Ganguly S, Weller JL, Klein DC, Cole PA. Cellular stabilization of the melatonin rhythm enzyme induced by nonhydrolyzable phosphonate incorporation. Nat Struct Biol. 2003 Dec; 10(12):1054-7. PMID: 14578935.
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  148. Zheng W, Cole PA. Novel bisubstrate analog inhibitors of serotonin N-acetyltransferase: the importance of being neutral. Bioorg Chem. 2003 Oct; 31(5):398-411. PMID: 12941292.
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  149. Cole PA, Shen K, Qiao Y, Wang D. Protein tyrosine kinases Src and Csk: a tail's tale. Curr Opin Chem Biol. 2003 Oct; 7(5):580-5. PMID: 14580561.
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  150. Cebrat M, Kim CM, Thompson PR, Daugherty M, Cole PA. Synthesis and analysis of potential prodrugs of coenzyme A analogues for the inhibition of the histone acetyltransferase p300. Bioorg Med Chem. 2003 Jul 31; 11(15):3307-13. PMID: 12837541.
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  151. Kaehlcke K, Dorr A, Hetzer-Egger C, Kiermer V, Henklein P, Schnoelzer M, Loret E, Cole PA, Verdin E, Ott M. Acetylation of Tat defines a cyclinT1-independent step in HIV transactivation. Mol Cell. 2003 Jul; 12(1):167-76. PMID: 12887902.
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  152. Scheibner KA, Zhang Z, Cole PA. Merging fluorescence resonance energy transfer and expressed protein ligation to analyze protein-protein interactions. Anal Biochem. 2003 Jun 15; 317(2):226-32. PMID: 12758261.
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  153. Cole PA, Courtney AD, Shen K, Zhang Z, Qiao Y, Lu W, Williams DM. Chemical approaches to reversible protein phosphorylation. Acc Chem Res. 2003 Jun; 36(6):444-52. PMID: 12809531.
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  154. Lu W, Shen K, Cole PA. Chemical dissection of the effects of tyrosine phosphorylation of SHP-2. Biochemistry. 2003 May 13; 42(18):5461-8. PMID: 12731888.
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  155. Huang ZQ, Li J, Sachs LM, Cole PA, Wong J. A role for cofactor-cofactor and cofactor-histone interactions in targeting p300, SWI/SNF and Mediator for transcription. EMBO J. 2003 May 01; 22(9):2146-55. PMID: 12727881; PMCID: PMC156091.
  156. Georges SA, Giebler HA, Cole PA, Luger K, Laybourn PJ, Nyborg JK. Tax recruitment of CBP/p300, via the KIX domain, reveals a potent requirement for acetyltransferase activity that is chromatin dependent and histone tail independent. Mol Cell Biol. 2003 May; 23(10):3392-404. PMID: 12724399; PMCID: PMC164760.
  157. Lee KC, Li J, Cole PA, Wong J, Kraus WL. Transcriptional activation by thyroid hormone receptor-beta involves chromatin remodeling, histone acetylation, and synergistic stimulation by p300 and steroid receptor coactivators. Mol Endocrinol. 2003 May; 17(5):908-22. PMID: 12586842.
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  158. Zhang Z, Shen K, Lu W, Cole PA. The role of C-terminal tyrosine phosphorylation in the regulation of SHP-1 explored via expressed protein ligation. J Biol Chem. 2003 Feb 14; 278(7):4668-74. PMID: 12468540.
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  159. Bandyopadhyay D, Okan NA, Bales E, Nascimento L, Cole PA, Medrano EE. Down-regulation of p300/CBP histone acetyltransferase activates a senescence checkpoint in human melanocytes. Cancer Res. 2002 Nov 01; 62(21):6231-9. PMID: 12414652.
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  160. Poux AN, Cebrat M, Kim CM, Cole PA, Marmorstein R. Structure of the GCN5 histone acetyltransferase bound to a bisubstrate inhibitor. Proc Natl Acad Sci U S A. 2002 Oct 29; 99(22):14065-70. PMID: 12391296; PMCID: PMC137837.
  161. Wang D, Esselman WJ, Cole PA. Substrate conformational restriction and CD45-catalyzed dephosphorylation of tail tyrosine-phosphorylated Src protein. J Biol Chem. 2002 Oct 25; 277(43):40428-33. PMID: 12181320.
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  162. Lu H, Pise-Masison CA, Fletcher TM, Schiltz RL, Nagaich AK, Radonovich M, Hager G, Cole PA, Brady JN. Acetylation of nucleosomal histones by p300 facilitates transcription from tax-responsive human T-cell leukemia virus type 1 chromatin template. Mol Cell Biol. 2002 Jul; 22(13):4450-62. PMID: 12052856; PMCID: PMC133924.
  163. Parang K, Kohn JA, Saldanha SA, Cole PA. Development of photo-crosslinking reagents for protein kinase-substrate interactions. FEBS Lett. 2002 Jun 05; 520(1-3):156-60. PMID: 12044889.
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  164. Lowry WE, Huang J, Ma YC, Ali S, Wang D, Williams DM, Okada M, Cole PA, Huang XY. Csk, a critical link of g protein signals to actin cytoskeletal reorganization. Dev Cell. 2002 Jun; 2(6):733-44. PMID: 12062086.
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  165. Zheng W, Cole PA. Serotonin N-acetyltransferase: mechanism and inhibition. Curr Med Chem. 2002 Jun; 9(12):1187-99. PMID: 12052171.
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  166. Williams DM, Cole PA. Proton demand inversion in a mutant protein tyrosine kinase reaction. J Am Chem Soc. 2002 May 29; 124(21):5956-7. PMID: 12022825.
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  167. Subbaramaiah K, Cole PA, Dannenberg AJ. Retinoids and carnosol suppress cyclooxygenase-2 transcription by CREB-binding protein/p300-dependent and -independent mechanisms. Cancer Res. 2002 May 01; 62(9):2522-30. PMID: 11980644.
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  168. Wolf E, De Angelis J, Khalil EM, Cole PA, Burley SK. X-ray crystallographic studies of serotonin N-acetyltransferase catalysis and inhibition. J Mol Biol. 2002 Mar 22; 317(2):215-24. PMID: 11902838.
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  169. Scheibner KA, De Angelis J, Burley SK, Cole PA. Investigation of the roles of catalytic residues in serotonin N-acetyltransferase. J Biol Chem. 2002 May 17; 277(20):18118-26. PMID: 11884405.
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  170. Rodu B, Cole P. Impact of the American anti-smoking campaign on lung cancer mortality. Int J Cancer. 2002 Feb 20; 97(6):804-6. PMID: 11857358.
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  171. Parang K, Cole PA. Designing bisubstrate analog inhibitors for protein kinases. Pharmacol Ther. 2002 Feb-Mar; 93(2-3):145-57. PMID: 12191607.
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  172. Costanzo A, Merlo P, Pediconi N, Fulco M, Sartorelli V, Cole PA, Fontemaggi G, Fanciulli M, Schiltz L, Blandino G, Balsano C, Levrero M. DNA damage-dependent acetylation of p73 dictates the selective activation of apoptotic target genes. Mol Cell. 2002 Jan; 9(1):175-86. PMID: 11804596.
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  173. Asahara H, Santoso B, Guzman E, Du K, Cole PA, Davidson I, Montminy M. Chromatin-dependent cooperativity between constitutive and inducible activation domains in CREB. Mol Cell Biol. 2001 Dec; 21(23):7892-900. PMID: 11689682; PMCID: PMC99956.
  174. Shekhtman A, Ghose R, Wang D, Cole PA, Cowburn D. Novel mechanism of regulation of the non-receptor protein tyrosine kinase Csk: insights from NMR mapping studies and site-directed mutagenesis. J Mol Biol. 2001 Nov 16; 314(1):129-38. PMID: 11724538.
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  175. Lu W, Gong D, Bar-Sagi D, Cole PA. Site-specific incorporation of a phosphotyrosine mimetic reveals a role for tyrosine phosphorylation of SHP-2 in cell signaling. Mol Cell. 2001 Oct; 8(4):759-69. PMID: 11684012.
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  176. Wang D, Cole PA. Protein tyrosine kinase Csk-catalyzed phosphorylation of Src containing unnatural tyrosine analogues. J Am Chem Soc. 2001 Sep 19; 123(37):8883-6. PMID: 11552794.
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  177. Kim CM, Cole PA. Bisubstrate ketone analogues as serotonin N-acetyltransferase inhibitors. J Med Chem. 2001 Jul 19; 44(15):2479-85. PMID: 11448230.
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  178. Thompson PR, Cole PA. Probing the mechanism of enzymatic phosphoryl transfer with a chemical trick. Proc Natl Acad Sci U S A. 2001 Jul 17; 98(15):8170-1. PMID: 11459948; PMCID: PMC37416.
  179. Thompson PR, Kurooka H, Nakatani Y, Cole PA. Transcriptional coactivator protein p300. Kinetic characterization of its histone acetyltransferase activity. J Biol Chem. 2001 Sep 07; 276(36):33721-9. PMID: 11445580.
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  180. Williams DM, Cole PA. Kinase chips hit the proteomics era. Trends Biochem Sci. 2001 May; 26(5):271-3. PMID: 11343910.
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  181. Zheng W, Scheibner KA, Ho AK, Cole PA. Mechanistic studies on the alkyltransferase activity of serotonin N-acetyltransferase. Chem Biol. 2001 Apr; 8(4):379-89. PMID: 11325593.
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  182. Wang D, Huang XY, Cole PA. Molecular determinants for Csk-catalyzed tyrosine phosphorylation of the Src tail. Biochemistry. 2001 Feb 20; 40(7):2004-10. PMID: 11329267.
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  183. Parang K, Till JH, Ablooglu AJ, Kohanski RA, Hubbard SR, Cole PA. Mechanism-based design of a protein kinase inhibitor. Nat Struct Biol. 2001 Jan; 8(1):37-41. PMID: 11135668.
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  184. Williams DM, Wang D, Cole PA. Chemical rescue of a mutant protein-tyrosine kinase. J Biol Chem. 2000 Dec 08; 275(49):38127-30. PMID: 11006267.
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  185. Ablooglu AJ, Till JH, Kim K, Parang K, Cole PA, Hubbard SR, Kohanski RA. Probing the catalytic mechanism of the insulin receptor kinase with a tetrafluorotyrosine-containing peptide substrate. J Biol Chem. 2000 Sep 29; 275(39):30394-8. PMID: 10869355.
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  186. Kundu TK, Palhan VB, Wang Z, An W, Cole PA, Roeder RG. Activator-dependent transcription from chromatin in vitro involving targeted histone acetylation by p300. Mol Cell. 2000 Sep; 6(3):551-61. PMID: 11030335.
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  187. Lau OD, Courtney AD, Vassilev A, Marzilli LA, Cotter RJ, Nakatani Y, Cole PA. p300/CBP-associated factor histone acetyltransferase processing of a peptide substrate. Kinetic analysis of the catalytic mechanism. J Biol Chem. 2000 Jul 21; 275(29):21953-9. PMID: 10777508.
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  188. Kim K, Parang K, Lau OD, Cole PA. Tyrosine analogues as alternative substrates for protein tyrosine kinase Csk: insights into substrate selectivity and catalytic mechanism. Bioorg Med Chem. 2000 Jun; 8(6):1263-8. PMID: 10896106.
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  189. Blaustein RO, Cole PA, Williams C, Miller C. Tethered blockers as molecular 'tape measures' for a voltage-gated K+ channel. Nat Struct Biol. 2000 Apr; 7(4):309-11. PMID: 10742176.
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  190. Lau OD, Kundu TK, Soccio RE, Ait-Si-Ali S, Khalil EM, Vassilev A, Wolffe AP, Nakatani Y, Roeder RG, Cole PA. HATs off: selective synthetic inhibitors of the histone acetyltransferases p300 and PCAF. Mol Cell. 2000 Mar; 5(3):589-95. PMID: 10882143.
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  191. Khalil EM, De Angelis J, Ishii M, Cole PA. Mechanism-based inhibition of the melatonin rhythm enzyme: pharmacologic exploitation of active site functional plasticity. Proc Natl Acad Sci U S A. 1999 Oct 26; 96(22):12418-23. PMID: 10535937; PMCID: PMC22936.
  192. Sondhi D, Cole PA. Domain interactions in protein tyrosine kinase Csk. Biochemistry. 1999 Aug 24; 38(34):11147-55. PMID: 10460171.
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  193. Cole PA, Sondhi D, Kim K. Chemical approaches to the study of protein tyrosine kinases and their implications for mechanism and inhibitor design. Pharmacol Ther. 1999 May-Jun; 82(2-3):219-29. PMID: 10454199.
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  194. Kim K, Cole PA. Synthesis of (2S,3R)-beta-methyltyrosine catalyzed by tyrosine phenol-lyase. Bioorg Med Chem Lett. 1999 Apr 19; 9(8):1205-8. PMID: 10328314.
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  195. Khalil EM, De Angelis J, Cole PA. Indoleamine analogs as probes of the substrate selectivity and catalytic mechanism of serotonin N-acetyltransferase. J Biol Chem. 1998 Nov 13; 273(46):30321-7. PMID: 9804794.
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  196. Muir TW, Sondhi D, Cole PA. Expressed protein ligation: a general method for protein engineering. Proc Natl Acad Sci U S A. 1998 Jun 09; 95(12):6705-10. PMID: 9618476; PMCID: PMC22605.
  197. De Angelis J, Gastel J, Klein DC, Cole PA. Kinetic analysis of the catalytic mechanism of serotonin N-acetyltransferase (EC 2.3.1.87). J Biol Chem. 1998 Jan 30; 273(5):3045-50. PMID: 9446620.
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  198. Sondhi D, Xu W, Songyang Z, Eck MJ, Cole PA. Peptide and protein phosphorylation by protein tyrosine kinase Csk: insights into specificity and mechanism. Biochemistry. 1998 Jan 06; 37(1):165-72. PMID: 9425036.
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  199. Grace MR, Walsh CT, Cole PA. Divalent ion effects and insights into the catalytic mechanism of protein tyrosine kinase Csk. Biochemistry. 1997 Feb 18; 36(7):1874-81. PMID: 9048573.
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  200. Cole PA. Chaperone-assisted protein expression. Structure. 1996 Mar 15; 4(3):239-42. PMID: 8805540.
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  201. Cole PA, Grace MR, Phillips RS, Burn P, Walsh CT. The role of the catalytic base in the protein tyrosine kinase Csk. J Biol Chem. 1995 Sep 22; 270(38):22105-8. PMID: 7673185.
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  202. Cole PA, Burn P, Takacs B, Walsh CT. Evaluation of the catalytic mechanism of recombinant human Csk (C-terminal Src kinase) using nucleotide analogs and viscosity effects. J Biol Chem. 1994 Dec 09; 269(49):30880-7. PMID: 7527038.
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  203. Cole PA, Robinson CH. Mechanism and inhibition of cytochrome P-450 aromatase. J Med Chem. 1990 Nov; 33(11):2933-42. PMID: 2231592.
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  204. Cole PA, Robinson CH. Conversion of 19-oxo[2 beta-2H]androgens into oestrogens by human placental aromatase. An unexpected stereochemical outcome. Biochem J. 1990 Jun 15; 268(3):553-61. PMID: 2363692; PMCID: PMC1131474.
  205. Cole PA, Bean JM, Robinson CH. Conversion of a 3-desoxysteroid to 3-desoxyestrogen by human placental aromatase. Proc Natl Acad Sci U S A. 1990 Apr; 87(8):2999-3003. PMID: 2326261; PMCID: PMC53821.
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