Philip A. Cole

Department Affiliation: Pharmacology
Degree: M.D., Ph.D., Johns Hopkins University
Rank:  Director and E.K. Marshall and Thomas H. Maren Professor
Telephone Number: 410-614-8849
Fax Number: 410-614-7717
E-mail address: pcole@jhmi.edu
School of Medicine Address: 316 Hunterian, Johns Hopkins School of Medicine, 725 N. Wolfe St., Baltimore, MD, 21205          

Staff

Chemical and biochemical approaches in the study of signal transduction, circadian rhythm, and gene regulation.

We use chemical approaches to study cell signal transduction hormonal control of circadian rhythm and gene regulation. We are interested in understanding the basis for molecular recognition of protein kinases. We employ substrate analogs, site-directed mutagenesis, and kinetic methods to elucidate protein kinase-substrate relationships. We are also pursuing the mechanism and inhibition of melatonin production. A new protein engineering method called expressed protein ligation, which allows for the ligation of synthetic peptides to recombinant proteins developed by us in collaboration with Tom Muir's laboratory, is being applied to these systems and others to elucidate protein function.  We have also developed selective HAT (histone acetyltransferase) inhibitors to investigate the role of the protein acetylation. 

Representative Publications: 

• DeAngelis, J., Gastel, J., Klein, D.C., and Cole, P.A.  Kinetic analysis of the catalytic mechanism of serotonin N-acetyltransferase, J. Biol. Chem., 273:3045-3050, 1998. Pub Med Reference
  
  
• Muir, T.W., Sondhi, D., and Cole, P.A.  Expressed protein ligation:  A general method for protein engineering, Proc. Natl. Acad. Sci. USA, 95:6705-6710, 1998. [Commentary: Science (1998) 281, 367-368]  Pub Med Reference
  
  
• Khalil, E. and Cole, P.A.  A potent inhibitor of the melatonin rhythm enzyme, J. Am. Chem. Soc., 120:6195-6196, 1998. [Commentary: Science News (1998) 154, 6-7]   Pub Med Abstract not available.
  
  
• Kim, K. and Cole, P.A.  Kinetic analysis of a protein tyrosine kinase transition state in the forward and reverse directions, J. Am. Chem. Soc., 120:6851-6858, 1998.  Pub Med Abstract not available.
  
  
• Khalil, E., DeAngelis, J., and Cole, P.A.  Indole-amine analogs as probes of the substrate selectivity and catalytic mechanism of serotonin N-acetyltransferase, J. Biol. Chem., 273:30321-30327, 1998.  Pub Med Reference
  
  
• Cole, P.A., Sondhi, D., and Kim, K.  Chemical approaches to the study of protein kinases and their implications for mechanism and inhibitor design, Pharmacology and Therapeutics, 82:219-229, 1999.  Pub Med Reference
  
  
• Kim, K. and Cole, P.A.  Synthesis of (2S, 3R)-beta-methyltyrosine catalyzed by tyrosine phenol-lyase bioorg, Med. Chem. Lett., 9:1205-1208, 1999.  Pub Med Reference
  
  
• Sondhi, D. and Cole, P.A.  Domain interactions in protein tyrosine kinase Csk, Biochemistry, 38:11147-11155, 1999.  Pub Med Reference
  
  
• Khalil, E.M., De Angelis, J., Ishii, M., and Cole, P.A. (1999) Mechanism-based inhibition of the melatonin rhythm enzyme: Pharmacologic exploitation of active site functional plasticity, Proc. Nat. Acad. Sci. USA, 96:12418-12423.  Pub Med Reference
  
  
• Lau, O.D., Kundu, T.K., Soccio, R.E., Ait-Si-Ali, S., Khalil, E., Vassilev, A., Wolffe, A.P., Nakatani, Y., Roeder, R.G., and Cole, P.A.  HATs off: Selective synthetic inhibitors of the histone acetyltransferases p300 and PCAF, Molecular Cell, 5:589-595, 2000.  Pub Med Reference
  
  
• Blaustein, R.O., Cole, P.A., Williams, C., and Miller, C.  Mapping K+ channels with molecular tape-measures, Nature Structural Biology, 7:309-311, 2000.  Pub Med Reference
  
  
• Kim, K., Parang, K., Lau, O.D., and Cole, P.A.  Tyrosine analogs as alternative substrates for protein tyrosine kinase Csk: Insights into substrate selectivity and catalytic mechanism, Bioorganic and Medicinal Chemistry, 8:1263-1268, 2000.  Pub Med Reference
  
  
• Lau, O.D., Courtney, A.D., Vassilev, A., Marzilli, L.A., Cotter, R.J., Nakatani, Y., and Cole, P.A.  PCAF histone acetyltransferase processing of a peptide substrate: Kinetic analysis of the catalytic mechanism, J. Biol. Chem., 275:21953-21959, 2000.  Pub Med Reference
  
  
• Kundu, T.K., Palhan, V.B., Wang, Z.Y., An, W., Cole, P.A., and Roeder, R.G.  Activator-dependent transcription from chromatin in vitro involving targeted histone acetylation by p300, Molecular Cell, 6:551-561, 2000.  Pub Med Reference
  
  
• Ablooglu, A.J., Till, J.H., Kim, K., Parang, K., Cole, P.A., Hubbard, S.R., and Kohanski, R.A.  Probing the catalytic mechanism of the insulin receptor kinase with a tetrafluorotyrosine-containing peptide substrate, J. Biol. Chem., 275:30394-30398, 2000.  Pub Med Reference
  
  
• Williams D.M., Wang, D., and Cole, P.A.  Chemical rescue of a mutant protein tyrosine kinase, J. Biol. Chem., 275:38127-38130, 2000.  Pub Med Reference
  
  
• Parang, K., Till, J.H., Ablooglu, A.J., Kohanski, R.A., Hubbard, S. R., and Cole, P.A. (2001) Mechanism-based design of a protein kinase inhibitor, Nature Structural Biology, 8:37-41, 2001.  [Commentary: Double Trouble, Nature Structural Biology, 8:16-18 (2001)]  Pub Med Reference
  
  
• Wang, D., Huang, X.-Y., and Cole, P.A.  Molecular determinants for Csk-catalyzed tyrosine phosphorylation of the Src tail, Biochemistry, 40:2004-2010, 2001.  Pub Med Reference
  
  
• Zheng, W., Scheibner, K.A., Ho, A.K., and Cole, P.A.  Mechanistic studies on the alkyltransferase activity of serotonin N-acetyltransferase, Chemistry and Biology, 8:379-389, 2001.  Pub Med Reference
  
  
• Williams, D.M. and Cole, P.A.  Kinase chips hit the proteomics era Trends in Biochem. Soc., 26:271-273, 2001.  Pub Med Reference
  
  
• Thompson, P.R. and Cole, P.A.  Probing the mechanism of enzymatic phosphoryl transfer with a chemical trick, Proc. Natl. Acad. Sci. USA, 98:8170-8171, 2001.  Pub Med Reference
  
  
• Kim, C.M. and Cole, P.A.  Bisubstrate ketone analogs as serotonin N-acetyltransferase inhibitors, J. Med. Chem., 44:2479-2485, 2001.  Pub Med Reference
  
  
• Thompson, P.R., Kurooka, H., Nakatani, Y., Cole, P.A.  Transcriptional coactivator protein p300: Kinetic characterization of its histone acetyltransferase activity, J. Biol. Chem., 276:33721-33729, 2001.  Pub Med Reference
  
  
• Wang, D. and Cole, P.A.  Protein tyrosine kinase Csk-catalyzed phosphorylation of Src containing unnatural tyrosine analogs, J. Am. Chem. Soc., 123:8883-8886, 2001.  Pub Med Reference
  
  
• Lu, W., Gong, D., Bar-Sagi, D., and Cole, P.A.  Site-specific incorporation of a phosphotyrosine mimetic reveals a role for tyrosine phosphorylation of SHP-2 in cell signaling, Mol. Cell, 8:759-769, 2001.  Pub Med Reference
  
  
• Asahara, H., Santoso, B., Du, K., Cole, P.A., Davidson, I., and Montminy, M.  Chromatin dependent cooperativity between constitutive and inducible activation domains in CREB, Mol. Cell. Biol., 21:7892-7900, 2001.  Pub Med Reference
  
  
• Shekhtman, A., Ghose, R., Wang, D., Cole, P.A., Cowburn, D.  Novel mechanism of the non-receptor protein tyrosine kinase Csk: Insights from NMR mapping studies and site-directed mutagenesis, J. Mol. Biol., 314:129-138, 2001.  Pub Med Reference
  
  
• Polesskaya, A., Naguibneva, I., Duquet, A., Ait-Si-Ali, S., Robin, P., Vervish, A., Cole, P., and Harel-Bellan, A  CBP/p300 and muscle differentiation: no HAT, no muscle EMBO J.,. 20:6816-6825, 2001.  Pub Med Reference
  
  
• Costanzo, A., Merlo, P., Pediconi, N., Fulco, M., Sartorelli, V., Cole, P.A., Fontemaggi, G., Fanciulli, M., Schiltz, L., Blandino, G., Balsano, and C., Levrero, M.  DNA damage-dependent acetylation of p73 dictates the selective activation of apoptotic target genes, Mol. Cell., 9:175-186, 2002.   Pub Med Reference
  
  
• Wolf, E., De Angelis, J., Khalil, E.M., Cole, P.A., and Burley, S.K.  X-ray crystallographic studies of serotonin N-acetyltransferase catalysis and inhibition, J. Mol. Biol., 317:215-224, 2002.   Pub Med Reference
  
  
• Zheng, W. and Cole, P.A.  Serotonin N-acetyltransferase: Mechanism and inhibition, Current Medicinal Chemistry, 9:1187-1199, 2002.  Pub Med Reference
  
  
• Parang, K. and Cole P.A.  Design of bisubstrate analog inhibitors for protein kinases, Pharmacology & Therapeutics, 93:145-157, 2002.  Pub Med Reference
  
  
• Scheibner, K.A., DeAngelis, J., Burley, S.K., and Cole, P.A.  Investigation of the roles of catalytic residues in serotonin N-acetyltransferase, J. Biol. Chem., 277:18118-18126, 2002.  Pub Med Reference
  
  
• Subbaramaiah, K., Cole, P.A., and Dannenberg, A. J.  Retinoids and carnosol suppress cyclooxygenase-2 transcription by CBP/p300-dependent and independent mechanisms, Cancer Research, 62:2522-2530, 2002.  Pub Med Reference
  
  
• Lowry, W.E., Huang, J.J., Ma, Y.-C., Ali, S., Wang, D., Williams, D.M., Okada, M., Cole, P.A., Huang, X.Y.  Csk, A critical link of G protein signals to actin cytoskeletal reorganization, Developmental Cell, 2:733-734, 2002.  Pub Med Reference
  
  
• Lu, H., Pise-Masison, C.A., Fletcher, T.M., Schiltz, R.L., Nagaich, A., Radonovich, M., Hager, G., Cole, P.A., Brady, J.N.  The HAT activity of p300 is required for tax-mediated HTLV-I LTR transcription from a chromatin template, Mol. Cell. Biol., 22:4450-4462, 2002.  Pub Med Reference
  
  
• Williams, D.M. and Cole, P.A. (2002) Proton demand inversion in a mutant protein kinase reaction, J. Am. Chem. Soc., 124:5956-5957, 2002.  Pub Med Reference
  
  
• Parang, K., Kohn, J., Saldanha, A., and Cole, P.A.  Development of photo-cross-linking reagents for protein kinase-substrate interactions, FEBS Letters, 520:156-160, 2002.   Pub Med Reference
  
  
• Wang, D., Esselman, W. J., and Cole, P. A. Substrate conformational restriction and CD45-catalyzed dephosphorylation of tail tyrosine-phosphorylated Src protein, J. Biol. Chem. 277: 40428-40433, 2002.  Pub Med Reference
  
  
• Bandyopadhyay, D., Okan, N. A., Bales, E., Nascimento, L., Cole, P. A., and Medrano, E. E.  Down-regulation of p300/CBP HAT activates a senescence checkpoint in human melanocytes, Cancer Research 62: 6231-6239, 2002.  Pub Med Reference
  
  
• Poux, A. N., Cebrat, M., Kim, C. M., Cole, P. A., and Marmorstein, R.  Structure of the GCN5 histone acetyltransferase bound to a bisubstrate inhibitor, Proc. Natl Acad. Sci. USA 99: 14065-14070, 2002.  Pub Med Reference
  
  
• Zhang, Z., Shen, K., Lu, W., and Cole, P. A.  The role of c-terminal tyrosine phosphorylation in the regulation of SHP-1 explored via expressed protein ligation, J. Biol. Chem. 278: 4668-4674, 2003.  Pub Med Reference
  
  
• Li, J., Lee, K. C. Cole, P. A., Wong, J., and Kraus, W. L.  Transcriptional activation by thyroid hormone receptor beta involves chromatin remodeling, tistone acetylation, and synergistic stimulation by p300 and SRC coactivators, Molecular Endocrinology 17: 908-922, 2003.    Pub Med Reference
  
  
• Scheibner, K. A., Zhang, Z., and Cole, P. A.  Merging FRET and expressed protein ligation to analyze protein-protein interactions, Anal. Biochem. 317: 226-232, 2003. Pub Med Reference
  
  
• Cole, P. A., Courtney, A. D., Zhang, Z., Qiao, Y., Lu, W., and Williams, D. M.  Chemical approaches to reversible protein phosphorylation, Accounts of Chemical Research 36: 444-452, 2003. Pub Med Reference
  
  
• Georges, S. A., Giebler, H. A., Cole, P. A., Luger, K., Laybourn, P. J., and Nyborg, J. K.  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. 23: 3392-3404, 2003.  Pub Med Reference
  
  
• Huang, Z.-Q., Li, J., Sachs, L. M., Cole, P. A., and Wong, J.  A role for cofactor-cofactor and -histone interactions in targeting p300, SWI/SNF and mediator for transcription, EMBO J. 22: 2146-2155, 2003.  Pub Med Reference
  
  
• Lu, W., Shen, K., and Cole, P. A.  Chemical dissection of the effects of tyrosine phosphorylation of SHP-2, Biochemistry 42: 5461-5468, 2003.  Pub Med Reference
  
  
• Cebrat, M., Kim, C. M., Thompson, P. R., Daugherty, M., and Cole, P. A.  Synthesis and analysis of potential prodrugs of coenzyme A analogs for the inhibition of histone acetyltransferase p300, Bioorg. Med. Chem., 11:3307-13, 2003.  Pub Med Reference
  
  
• Kaehlcke, K.; Dorr, A.; Hetzer-Egger, C., Kiermer, V., Henklein, P., Schnoelzer, M., Loret, E., Cole, P. A., and Verdin, E., Ott, M.  Acetylation of Tat defines a cyclin T1-independent step in HIV transactivation, Mol. Cell 12:167-76, 2003.  Pub Med Reference
  
  
• Zheng, W. and Cole, P.A.  Novel bisubstrate analog inhibitors of serotonin N-acetyltransferase: The importance of being neutral, Bioorg. Chem., 31: 398-411, 2003.   Pub Med Reference
  
  
• Cole, P.A., Shen, K., Qiao, Y., and Wang, D.  Protein tyrosine kinases Src and Csk: A tail's tale, Curr. Opin. Chem., Biol. 7:580-585, 2003.  Pub Med Reference
  
  
• Zheng, W., Zhang, Z., Ganguly, S., Weller, J.L., Klein, D., and Cole, P.A.  Cellular stabilization of the melatonin rhythm enzyme induced by non-hydrolyzable phosphonate incorporation, Nature Struct. Biol., 10:1054-1057, 2003.  [Commentary: Baltimore Sun October, 27, 2003, p. 3]  Pub Med Reference
  
  
• Shen, K. and Cole, P.A.  Conversion of a tyrosine kinase protein substrate to a high affinity ligand by ATP linkage, J. Am. Chem. Soc., 125:16172-16173, 2003.  Pub Med Reference
  
  
• Zheng, Y., Thompson, P.R., Cebrat, M., Wang, L., Devlin, M.K., Alani, R.M., and Cole, P.A.  Selective HAT inhibitors as mechanistic tools for protein acetylation, Meth. Enz., 376:188-199, 2004.  Pub Med Reference
  
  
• Thompson, P.R., Wang, D., Wang, L., Fulco, M., Pediconi, N., Zhang, D., An, W., Ge, Q., Roeder, R.G., Wong, J., Levrero, M., Sartorelli, V., Cotter, R.J., and Cole, P.A.  Regulation of p300 HAT domain via a novel activation loop, Nature Struct. Mol. Biol., 11:308-315, 2004.  [Commentary: Nature Struct. Mol. Biol. 10, 298-300].  Pub Med Reference
  
  
• Farrell, C.J., Lee, J.M., Shin, E.-C., Cebrat, M., Cole, P.A. and Hayward, S.D.  Inhibition of Epstein-Barr Virus induced growth proliferation by an EBNA2-TAT peptide, Proc. Natl. Acad. Sci. USA, 101:4625-4630, 2004.  Pub Med Reference.
  
  
• Sagar, V., Zheng, W., Thompson, P.R., and Cole, P.A.  Bisubstrate analog structure-activity-relationships for p300 histone acetyltransferase inhibitors, Bioorg. Med. Chem.,  12:3383-3390, 2004.  Pub Med Reference
  
  
• Hines (Courtney), A. and Cole, P.A.  Design, synthesis and characterization of an ATP-peptide conjugate inhibitor of protein kinase A, Bioorg. Med. Chem. Lett., 14:2951-2954, 2004. Pub Med Reference
  
  
• Hwang, Y. and Cole, P.A.  Efficient synthesis of phosphorylated prodrugs with bis(POM)-phosphoryl chloride, Org. Letters, 6:1555-1556, 2004.  Pub Med Reference

• Shi, Y., Lan, F., Matson, C., Mulligan, P., Whetstine, J.R., Cole, P. A., Casero, R.A., and Shi, Y.  Histone demethylation mediated by the nuclear amine oxidase homolog LSD1, Cell, 119:941-953, 2004.  Pub Med Reference
  
  
• Yoon, H.G., Choi, Y., Cole, P.A., and Wong, J.  Reading and function of a histone code involved in targeting corepressor complexes for repression, Mol. Cell. Biol., 25:324-335, 2005.  Pub Med Reference
  
  
• Cheung, E., Acevedo, M.L., Cole, P.A., and Kraus, W.L.  Altered pharmacology and distinct coactivator usage for estrogen receptor-dependent transcription through activating protein-1, Proc. Natl. Acad. Sci. USA, 102:559-564, 2005.  Pub Med Reference
  
  
• Wang, D., Thompson, P.R., Cole, P.A., and Cotter, R.J.  Post-source decay analysis of a highly acetylated protein using a curved-field reflectron mass spectrometer, Proteomics 5:2288-2295, 2005.  Pub Med Reference
  
  
• Zheng, W., Schwarzer, D., LeBeau, A., Weller, J.L., Klein, D.C., and Cole, P.A.  Cellular stability of serotonin N-acetyltransferase conferred by Phosphono-difluoromethylene Alanine (Pfa) substitution for Ser205, J. Biol. Chem. 280:10462-10467, 2005.  Pub Med Reference
  
  
• Hines, A.C., Parang, K., Kohanski, R.A., Hubbard, S.R., and Cole, P.A. Bisubstrate Analog Probes for the Insulin Receptor Protein Tyrosine Kinase: Molecular Yardsticks for Analyzing Catalytic Mechanism and Inhibitor Design, Bioorg. Chem. 33:285-297, 2005.  Pub Med Reference
  
  

• Zheng, Y., Mamdani, F., Toptygin, D., Brand, L. Stivers, J. T., and Cole, P.A.  Fluorescence analysis of a dynamic loop in the PCAF/GCN5 histone acetyltransferase, Biochemistry 44:10501-10509, 2005.  Pub Med Reference
  

• Schwarzer, D. and Cole, P.A.  Protein semisynthesis and expressed protein ligation: Chasing a protein’s tail, Curr. Opin. Chem. Biol. 9:561-569, 2005.  Pub Med Reference

• Guidez, F., Howell, L., Islam, M., Cebrat, M., Alani, R. M., Ivins, S., Hormaeche, I., McConnell, M. J., Pierce, S., Cole, P. A., Licht, J., Zelent, A. Histone acetyltransferase activity of p300 is required for transcriptional repression by the promyelocytic zinc finger protein, Mol. Cell. Biol. 25:5552-5566, 2005.  Pub Med Reference

• Cleary, J., Sitwala, K.V., Khodadoust, M.S., Kwok, R.P.S., Mor-Vaknin, N., Cebrat, M., Cole, P.A., Markovitz, D.M.  Acetylation by P/CAF Drives DEK Into Interchromatin Granule Clusters, J. Biol. Chem. 280:31760-31767. 2005.  Pub Med Reference

• Shen, K., Hines, A.C., Schwarzer, D., Paumi, K., Cole, P.A. Protein Kinase Structure and Function Analysis Using Chemical Tools, Biochim. Biophys. Acta 1754:65-78, 2005.  Pub Med Reference 

• Lewczuk, B., Zheng, W., Prusik, M., Cole, P.A., Przybylska-Gornowicz, B. N-bromoacetyltryptamine strongly and reversibly inhibits melatonin secretion from mammalian pinealocytes, Neuroendocrinology Lett. 26:581-592, 2005.  Pub Med Reference

• Zheng, Y., Karanam, B., Cebrat, M. Buck, D., Guidez, F., Zelent, A., Alani, R. M., Cole, P.A., Synthesis and Evaluation of a Potent and Selective Cell-permeable p300 Histone Acetyltransferase Inhibitor, J. Am. Chem. Soc.127:17182-17183, 2005. Pub Med Reference

• Qiao, Y., Molina, H., Pandey, A., Zhang, J., Cole, P.A., Chemical Rescue of a Mutant Enzyme in Living Cells, Science 311:1293-1297, 2006.  Pub Med Reference

• Levinson, N. M., Kuchmnet, O., Shen, K., Young, M. A., Koldobskiy, M., Karplus, M., Cole, P.A., Kuriyan, J., A Src-like Inactive Conformation in the Abl Tyrosine Kinase Domain, PloSBiology 4:e144, 2006.  Pub Med Reference

• Culhane, J.C., Szewczuk, L.M., Liu, X., Da, G., Marmorstein, R., Cole, P.A., A Mechanism-based Inactivator for Histone Demethylase LSD1, J. Am. Chem. Soc. 128:4356-4357, 2006.  Pub Med Reference

• Schwarzer, D., Zhang, Z., Zheng, W., Cole, P. A., Negative Regulation of a Tyrosine Phosphatase by Tyrosine Phosphorylation, J. Am. Chem. Soc. 128:4192-4193, 2006. Pub Med Reference

• Bose, R., Molina, H., Patterson, A.S., Bitok, J.K., Periaswamy, B., Bader, J.S., Pandey, A., Cole, P.A., Phosphoproteomic analysis of Her2/neu signaling and inhibition, Proc. Natl Acad Sci. USA 103:9773-9778, 2006. Pub Med Reference

• Zhang, X., Gureasko, J., Shen, K., Cole, P.A., Kuriyan, J., An Allosteric Mechanism for the Activation of the Kinase Domain of the Epidermal Growth Factor Receptor, Cell 125:1137-1149, 2006.  Pub Med Reference

• Cheng, K.Y., Noble, M.E.M., Skamnaki, V., Brown, N.R., Lowe, E.D., Kontogiannis, L., Shen, K., Cole, P.A., Siligardi, G., Johnson, L.N., The Role of the Phospho-CDK2/cyclin A Recruitment Site in Substrate Recognition, J. Biol. Chem. 281:23167-23179, 2006. Pub Med Reference

• Bose, R., Holbert, M. A., Pickin, K. A. and Cole, P.A.  Protein Tyrosine Kinase-Substrate Interactions, Curr. Op. Struct. Biol. 16:668-675, 2006.  Pub Med Reference       

• Cole, P. A., (2007) 'Chemical Biology and Enzymology, Protein Phosphorylation as a Case Study' in Chemical Biology, eds. Schreiber, Kapoor, Wess; Wiley-VCH, Weinheim.

• Szewczuk, L. M., Tarrant, M. K., Cole, P. A. Protein phosphorylation by semisynthesis: from paper to practice, Meth. Enz. 462:1-24, 2009.   Pub Med Reference

• Hwang, Y., Ganguly, S., Ho, A. K., Klein, D. C., Cole, P. A.  Enzymatic and Cellular Study of a Serotonin N-acetyltransferase Phosphopantetheine-based Prodrug, Bioorg. Med. Chem. 15:2147-2155, 2007. Pub Med Reference

• Kenneth, N. S., Ramsbottom, B. A., Gomez-Roman, N., Marshall, L., Zhang, J.,Cole, P. A., White, R. J.  Activation of Pol III Transcription by c-Myc Involves Selective Acetylation of Histone H3 and Recruitment of TRAPP, GCN5, and TFIIIB, Proc. Natl Acad. Sci. USA 104:14917-14922, 2007. Pub Med Reference

• Karanam, B., Wang, L., Wang, D., Liu, X., Marmorstein, R., Cotter, R., Cole, P. A.  Multiple Roles for Acetylation in the Interaction of p300 HAT with ATF-2, Biochemistry 46: 8207-8216, 2007. Pub Med Reference

• Hu, X., Dang, Y., Tenney, K., Crews, P., Tsai, C. W., Sixt, K. M.,Cole, P. A., Liu, J. O.  Regulation of c-Src Non-receptor Tyrosine Kinase Activity by Bengamide A Through Inhibition of Methionine Aminopeptidases Chemistry and Biology 14: 764-774, 2007.  Pub Med Reference

• Szewczuk, L. M., Culhane, J. C., Yang, M., Majumdar, A., Yu, H., Cole, P. A.  Mechanistic Analysis of a Suicide Inactivator of Histone Demethylase LSD1, Biochemistry 46: 6892-6902, 2007. Pub Med Reference

• Yang, M., Culhane, J. C., Szewczuk, L. M., Gocke, C. B., Brautigam, C. A., Tomchick, D. R., Machius, M., Cole, P. A.*, Yu, H.*  Structural Basis of Histone Demethylation by LSD1 Revealed by Suicide Inactivation Nature Struct. Mol. Biol. 14: 535-539, 2007. (*co-corresponding author) Pub Med Reference

• Yang, M., Culhane, J. C., Szewczuk, L. M., Jalli, P., Ball, H. L., Machius, M.,Cole, P. A., Yu, H.  Structural Basis for Inhibition of the LSD1 Histone Demethylase by the Antidepressant trans-2-Phenylcyclopropylamine Biochemistry 46:8058-8065, 2007. Pub Med Reference

• Muratore, K.,Cole, P. A.  A Lock on Phosphotyrosine Signaling ACS Chemical Biology 2:454-456, 2007. Pub Med Reference

• Zhang, X., Pickin, K. A., Bose, R., Jura, N., Cole, P. A., Kuriyan, J.  Inhibition of the EGF Receptor by Blockage of an Activating Kinase Domain Interface, Nature 450: 741-744, 2007. Pub Med Reference

• Hwang, Y., Thompson, P. R., Wang, L., Jiang, L., Kelleher, N. L., Cole, P. A.  A Selective Chemical Probe for Coenzyme-A Requiring Enzymes Angewandte Chemie Int. Ed. 46:7621-7624, 2007. Pub Med Reference

• Culhane, J. C., Cole, P. A.  LSD1 and the Chemistry of Histone Demethylation Curr. Op. Chem. Biol. 11:561-568, 2007. Pub Med Reference

• Szewczuk, L. M., Saldanha, S. A., Ganguly, S., Bowers, E. M., Javoroncov, M., Karanam, B., Culhane, J. C., Holbert, M. A., Klein, D. C., Abagyan, R.,Cole, P. A.  De novo Discovery of Serotonin N-acetyltransferase Inhibitors J. Med. Chem. 50:5330-5338, 2007. Pub Med Reference

• Liu, X., Wang, L., Zhao, K., Thompson, P. R., Hwang, Y., Marmorstein, R., Cole, P. A. (2008) The Structural Basis of Protein Acetylation by the p300/CBP Transcriptional Coactivator Nature 451: 846-850. Pub Med Reference

• Qiu, Q., Tarrant, M.K., Lee, S.H., Satyamurthy, A., Bose, R., Banjade, S., Pal, A., Bornmann, W. G., Lemmon, M. A., Cole, P. A., Leahy, D. J.  (2008) Mechanism of Activation and Inhibition of the HER4/ErbB4 Kinase Structure 16: 460-467. Pub Med Reference

• Mathivanan, S. et al. (2008) Human Proteinpedia enables sharing of human protein data Nature Biotech. 26:164-167. Pub Med Reference

• Levinson, N. M., Seeliger, M. A., Cole, P. A., Kuriyan, J.  Structural Basis for the Recognition of c-Src by its Inactivator Csk, Cell 134:124-134, 2008.  Pub Med Reference

• Pickin, K. A., Chaudhury, S., Dancy, B. C. R., Gray, J. J., Cole, P. A. (2008) Analysis of Autophosphorylation of a Protein Kinase by Expressed Protein Ligation J. Am. Chem. Soc. 130:5667-5669. Pub Med Reference

• Tang, Y., Holbert, M. A., Wurtele, H., Meeth, K., Rocha, W., Gharib, M., Jiang, E., Thibault, P., Verrauly, A., Cole, P. A., Marmorstein, R.  Fungal Rtt109/KAT11 Histone Acetyltransferase: an Unexpected Structural Homolog of Metazoan p300/CBP, Nature Struct. Mol. Biol. 15:738-745, 2008.  Pub Med Reference

• Liu, Y., Dentin, R., Chen, D., Hedrick, S., Ravnskaer, K., Schenk, S., Milne, J., Meyers, D. J., Cole, P., Yates, J., Olefsky, J., Guarente, L., Montminy, M.  A fasting inducible acetylase/deacetylase switch modulates gluconeogenesis through activator-coactivator exchange, Nature 456:269-273, 2008.  Pub Med Reference

• Cole, P. A.  Chemical Probes for Histone-Modifying Enzymes. Nature Chem. Biol. 4, 590-597, 2008.  Pub Med Reference

• Szewczuk, L. M., Tarrant, M. K., Sample, V., Drury, W. J. III, Zhang, J., Cole, P. A. Analysis of Serotonin N-Acetyltransferase Regulation In Vitro and in Live Cells Using Protein Semisynthesis. Biochemistry 47:10407-10419, 2008.  Pub Med Reference
  
• Wang, L., Tang, Y., Cole, P. A.,* 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, 2008. (*co-corresponding author).  Pub Med Reference
  
• Tarrant, M. K., Cole, P. A.  The Chemical Biology of Protein Phosphorylation. Ann. Rev. Biochem 78:797-825, 2009.  Pub Med Reference
  
• Hansson, M. L., Popko-Scibor, Saint Just Ribiero, M., Dancy, B. M., Lindberg, M. L., Cole, P. A., Wallberg, A. E.  The Transcriptional Coactivator MAML1 Regulates p300 Autoacetylation and HAT Activity. Nucl. Acids Res. 91:2996-3006, 2009.  Pub Med Reference
  
• Wang, D., Xia, X., Liu, Y., Oetting, A., Walker, R. L., Meltzer, P., Cole, P. A., Zhu, Y., Shi, Y.-B., Yen, P. M.  Negative Regulation of TSHa Target Gen by Thyroid Hormone Involves Histone Acetylation and Corepressor Complex Dissociation.  Mol. Endocrin. 23, 600-609, 2009. Pub Med Reference
  
• Muratore, K. E., Seeliger, M. A., Wang, Z., Fomina, D., Neiswinger, J., Havranek, J. J., Baker, D., Kuriyan, J., Cole, P. A.  Comparative Analysis of Mutant Tyrosine Kinase Chemical Rescue. Biochemistry 48:3378-3386, 2009.  Pub Med Reference
  
• Qiu, C., Tarrant, M.K., Boronina, T., Longo, P. A., Kavran, J. M., Cole, R. N., Cole, P. A.*, Leahy, D. J.*  In vitro Enzymatic Characterization of Near Full Length EGFR in Activated and Inhibited States. Biochemistry 48:6624-6632, 2009. (*co-corresponding).  Pub Med Reference
  
• Oussaief, L., Hippocrate, A., Ramirez, V., Rampanou, A., Zhang, W., Meyers, D., Cole, P., Khelifa, R, Joab, I.  PI3-K/Akt Pathway Targets Acetylation of Smad3 through Smad3/CBP Interaction; Contribution to TGF-¾1-induced EBV Reactivation.  J. Biol. Chem. 284:23912-23924, 2009.  Pub Med Reference

Other graduate programs in which Dr. Cole participates:

BCMB Program 
Anti-Cancer Drug Development Program 
Chemistry-Biology Interface Program (CBI)

Staff