In This Section      

Philip A. Cole, M.D., Ph.D.

Philip A. Cole, M.D., Ph.D. Philip A. Cole, M.D., Ph.D.

Key Publications

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. (2010).  Glucose and weight control in mice with a designed ghrelin O-acyltransferase inhibitor.  Science. 330, 1689-1692PubMed Link

Karukurichi KR, Cole PA. (2010). Probing the reaction coordinate of the p300/CBP histone acetyltransferase with bisubstrate analogs. [Epub ahead of print].  PubMed Link

Bowers E, 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. (2010). Virtual ligand screening of the p300/CBP histone acetyltransferase:  Identification of a selective small molecule inhibitor. Chem. Biol. 17, 471-482PubMed Link

Ahn YH, Hwang Y, Liu H, Wang XJ, Zhang Y, Stephenson KK, Boronina TN, Cole RN, Dinkova-Kostova AT, Talalay P, Cole PA. (2010). Electrophilic tuning of the chemoprotective natural product sulforaphane. Proc Natl Acad Sci U S A. Epub ahead of print].  PubMed Link

Hansson ML, Popko-Scibor AE, Saint Just Ribeiro M, Dancy BM, Lindberg MJ, Cole PA, Wallberg AE. (2009). The transcriptional coactivator MAML1 regulates p300 autoacetylation and HAT activity. Nucleic Acids Res. 37, 2996-3006.  PubMed Link

Karukurichi KR, Wang L, Uzasci L, Manlandro CM, Wang Q, Cole PA. (2010). Analysis of p300/CBP histone acetyltransferase regulation using circular permutation and semisynthesis. J Am Chem Soc. 132, 1222-1223.  PubMed Link

Culhane JC, Wang D, Yen PM, Cole PA. (2010). Comparative analysis of small molecules and histone substrate analogues as LSD1 lysine demethylase inhibitors. J Am Chem Soc. 132, 3164-3176.  PubMed Link

Cole PA. (2008). Chemical Probes for Histone-Modifying Enzymes. Nature Chem. Biol. 4(10), 590-597.  PubMed Link

Wang L, Tang Y, Cole PA, Marmorstein R. (2008). Structure and Chemistry of the p300/CBP and Rtt109 Histone Acetyltransferases: Implications for Histone Acetyltransferase Evolution and Function. Curr. Op. Struct. Biol.18, 741-747.  PubMed Link

Liu X, Wang L, Zhao K, Thompson PR, Hwang Y, Marmorstein R, Cole PA. (2008). The structural basis of protein acetylation by the p300/CBP transcriptional coactivator. Nature. 451, 846-850.  PubMed Link

Tang Y, Holbert MA, Wurtele H, Meeth K, Rocha W, Gharib M, Jiang E, Thibault P, Verreault A, Cole PA, Marmorstein R. (2008). Fungal Rtt109 histone acetyltransferase is an unexpected structural homolog of metazoan p300/CBP. Nat Struct Mol Biol. 15, 738-745.  PubMed Link

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, et al. (2008). Human Proteinpedia enables sharing of human protein data. Nature Biotechnol. 26, 164-167.  PubMed Link

Culhane JC, Cole PA. (2007). LSD1 and the chemistry of histone demethylation. Curr. Op. Chem. Biol. 11, 561-568.  PubMed Link

Karanam B, Wang L, Wang D, Liu X, Marmorstein R, Cotter R, Cole PA. (2007). Multiple roles for acetylation in the interaction of p300 HAT with ATF-2. Biochemistry. 46(28), 8207-8216.  PubMed Link

Hwang Y, Thompson PR, Wang L, Jiang L, Kelleher NL and Cole PA. (2007). A selective chemical probe for coenzyme-A requiring enzymes. Angewandte Chemie Int. Ed Engl. 46, 7621-7624.  PubMed Link

Szewczuk LM, Culhane JC, Yang M, Majumdar A, Yu H and Cole PA. (2007). Mechanistic Analysis of a Suicide Inactivator of Histone Demethylase LSD1. Biochemistry. 46, 6892-6902.  PubMed Link

Yang M, Culhane JC, Szewczuk LM, Jalli P, Ball HL, Machius M, Cole PA and Yu H. (2007). Structural basis for inhibition of the LSD1 histone demethylase by the antidepressant trans-2-phenylcyclopropylamine. Biochemistry. 46, 8058-8065.  PubMed Link

Bose R, Molina H, Patterson, AS, Bitok JK, Periaswamy B, Bader JS, Pandey A, Cole PA. (2006). Phosphoproteomic analysis of Her2/neu signaling and inhibition. Proceedings of the National Academy of Sciences, USA. 103, 9773-9778.  PubMed Link

Culhane JC, Szewczuk LM, Liu X, Da G, Marmorstein R, Cole PA. (2006). A Mechanism-based Inactivator for Histone Demethylase LSD1. J. Am. Chem. Soc. 128, 4356-4357.  PubMed Link

Qiao Y, Molina H, Pandey A, Zhang J, Cole PA. (2006). Chemical rescue of a mutant enzyme in living cells. Science. 311, 1293-1297.  PubMed Link

Zheng W, Schwarzer D, LeBeau A, Weller JL, Klein DC, Cole PA. (2005). Cellular stability of serotonin N-acetyltransferase conferred by phosphono-difluoromethylene alanine (Pfa) substitution for Ser205. J. Biol. Chem. 280, 10462-10467.  PubMed Link

Cheung E, Acevedo ML, Cole PA, Kraus WL. (2005). Altered pharmacology and distinct coactivator usage for estrogen receptor-dependent transcription through Activating Protein-1. Proc. Natl. Acad. Sci. USA. 102, 559-564.  PubMed Link

Hines AC, Parang K, Kohanski RA, Hubbard SR, Cole PA. (2005). Bisubstrate analog probes for the insulin receptor protein tyrosine kinase: Molecular yardsticks for analyzing catalytic mechanism and inhibitor design. Bioorg. Chem. 33, 285-297.  PubMed Link

Wang D, Thompson PR, Cole PA, Cotter RJ. (2005). Structural analysis of a highly acetylated protein using a curved-field reflectron mass spectrometer. Proteomics. 5, 2288-2296.  PubMed Link

Guidez F, Howell L, Islam M, Cebrat M, Alani RM, Ivins S, Hormaeche I, McConnell MJ, Pierce S, Cole PA, Licht J, Zelent A. (2005). Histone acetyltransferase activity of p300 is required for transcriptional repression by the promyelocytic zinc finger protein, Mol. Cell. Biol. 25, 5552-5566.  PubMed Link

Zheng Y, Mamdani F, Toptygin D, Brand L, Stivers JT, Cole PA. (2005). Fluorescence analysis of a dynamic loop in the PCAF/GCN5 histone acetyltransferase. Biochemistry. 44, 10501-10509.  PubMed Link

Zheng Y, Karanam B, Cebrat M, Buck D, Guidez F, Zelent A, Alani RM, Cole PA. (2005). Synthesis and evaluation of a potent and selective cell-permeable p300 histone acetyltransferase inhibitor. J. Am. Chem. Soc. 127, 17182-17183.  PubMed Link

Zheng Y, Thompson PR, Cebrat M, Wang L, Devlin MK, Alani RM, Cole PA. (2004). Selective HAT inhibitors as mechanistic tools for protein acetylation. Meth. Enz. 376, 188-199.  PubMed Link

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. (2004). Regulation of p300 HAT domain via a novel activation loop. Nature Struct. Mol. Biol. 11, 308-315.  PubMed Link

Farrell CJ, Lee JM, Shin E-C, Cebrat M, Cole PA, Hayward SD. (2004). Inhibition of Epstein-Barr virus induced growth proliferation by an EBNA2-TAT peptide. Proc. Natl. Acad. Sci. USA. 101, 4625- 4630.  PubMed Link

Sagar V, Zheng W, Thompson PR, Cole PA. (2004). Bisubstrate analog structure-activity-relationships for p300 histone acetyltransferase inhibitors. Bioorg. Med. Chem. 12, 3383-3390.  PubMed Link

Hines AC, Cole PA. (2004). Design, synthesis and characterization of an ATP-peptide conjugate inhibitor of protein kinase A. Bioorg. Med. Chem. Lett. 14, 2951-2954.  PubMed Link

Hwang Y, Cole PA. (2004). Efficient synthesis of phosphorylated prodrugs with bis(POM)-phosphoryl chloride. Org. Letters. 6, 1555-1556.  PubMed Link

Shi Y, Lan F, Matson C, Mulligan P, Whetstine, J R, Cole PA, Casero RA, Shi Y. (2004). Histone demethylation mediated by the nuclear amine oxidase homolog LSD1. Cell. 119, 941-953.  PubMed Link

Zhang Z, Shen K, Lu W, Cole PA. (2003). The role of C-terminal tyrosine phosphorylation in the regulation of SHP-1 explored via expressed protein ligation. J. Biol. Chem. 278, 4668-4674.  PubMed Link

Scheibner KA, Zhang Z, Cole PA. (2003). Merging fluorescence resonance energy transfer and expressed protein ligation to analyze protein-protein interactions. Anal. Biochem. 317, 226-232.  PubMed Link

Lu W, Shen K, Cole PA. (2003). Chemical dissection of the effects of tyrosine phosphorylation of SHP-2. Biochemistry. 42, 5461-5468.  PubMed Link

Kaehlcke K, Dorr A, Hetzer-Egger C, Kiermer V, Henklein P, Schnoelzer M, Loret E, Cole PA, Verdin E, Ott M. (2003). Acetylation of Tat defines a cyclinT1-independent step in HIV transactivation. Mol. Cell. 12, 167-176.  PubMed Link

Zheng W, Zhang Z, Ganguly S, Weller JL, Klein D, Cole PA. (2003). Cellular stabilization of the melatonin rhythm enzyme induced by incorporation of a non-hydrolyzable phosphonate. Nature Struct. Biol. 10, 1054-1057.  PubMed Link

Shen K, Cole PA. (2003). Conversion of a tyrosine kinase protein substrate to a high affinity ligand by ATP linkage. J. Am. Chem. Soc. 125, 16172-16173.  PubMed Link

Williams DM, Cole PA. (2002). Proton demand inversion in a mutant protein kinase reaction. J. Am. Chem. Soc. 124, 5956-5957.  PubMed Link

Lowry WE, Huang JJ, Ma Y-C, Ali S, Wang D, Williams DM, Okada M, Cole PA, Huang XY. (2002). Csk, a critical link of G protein signals to actin cytoskeletal reorganization. Dev. Cell. 2, 733-734.  PubMed Link

Wang D, Esselman WJ, Cole PA. (2002). Substrate conformational restriction and CD45-catalyzed dephosphorylation of tail tyrosine-phosphorylated Src protein. J. Biol. Chem. 277, 40428-40433.  PubMed Link

Poux AN, Cebrat M, Kim CM, Cole PA, Marmorstein R. (2002). Structure of the GCN5 histone acetyltransferase bound to a bisubstrate inhibitor.  Proc. Natl Acad. Sci. USA. 99, 14065-14070.  PubMed Link

Parang K, Till JH, Ablooglu AJ, Kohanski RA, Hubbard SR, Cole PA. (2001). Mechanism-based design of a protein kinase inhibitor. Nature Struct. Biol. 8, 37-41.  PubMed Link

Lu W, Gong D, Bar-Sagi D, Cole PA. (2001). Site-specific incorporation of a phosphotyrosine mimetic reveals a role for tyrosine phosphorylation of SHP-2 in cell signaling. Mol. Cell. 8, 759-769.  PubMed Link

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