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Philip A. Cole

Dr. 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 proteinâ€™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-Â¾1-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

Research Associate
Dr. David Meyers	dmeyers7@jhmi.edu	410-502-4804
Post-Doctoral Fellows
Dr. Young-Hoon Ahn	yahn3@jhmi.edu	410-614-0322
Dr. Marc Holbert	mholber2@jhmi.edu	410-614-0322
Dr. Rong Huang	rhuang9@jhmi.edu	410-614-0322
Dr. You Sang Hwang	yhwang4@jhmi.edu	410-614-0322
Dr. Kannan Karukurichi	kkaruku1@jhmi.edu	410-614-0322
Dr. Chandrani Mukherjee	chandrani@jhmi.edu	410-614-0322
Dr. Zhihong Wang	zwang37@jhmi.edu	410-614-0322
Dr. Zhaoxiong "Norm" Zheng	zzheng3@jhmi.edu	410-502-4803 410-614-8048 (NMR/MS)
Graduate Students
Erin Bowers	ebowers4@jhu.edu	410-614-0322
Blair Dancy	bcrdancy@jhmi.edu	410-614-0322
Isabel Martinez	mmarti65@jhmi.edu	410-614-0322
Beverly Rabbitts	brabbit1@jhmi.edu	410-614-0322
Mary Katherine Tarrant	mtarran1@jhu.edu	410-614-0322
Martin Taylor	mstaylor@jhmi.edu	410-614-0322
Trainee
Tumajah Jackson	tjacks57@jhmi.edu	410-614-0322
Administrative Assistant
Robin Hart	rhart@jhmi.edu	410-614-8849

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Philip A. Cole