The VICC.ORG Directory of Doctors, Healthcare Providers & Researchers
Stephen W. Fesik, Ph.D.
Orrin H. Ingram, II Chair in Cancer Research
Professor of Biochemistry, Pharmacology and Chemistry
VICC Member
Researcher
Contact Information:
Vanderbilt University Medical Center
634 RRB, 2200 Pierce Ave
Nashville, TN 37232-0146
615-322-6303
Profile
Stephen W. Fesik, Ph.D. is the Orrin H. Ingram, II Chair in Cancer Research and a Professor of Biochemistry, Pharmacology, and Chemistry in Vanderbilt University School of Medicine. He is also a member of the Vanderbilt Ingram Cancer Center (VICC), the Vanderbilt Institute of Chemical Biology (VICB) and the Center for Structural Biology (CSB).
The focus of his research is on cancer drug discovery using fragment-based approaches and structure-based drug design.
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Stephen W. Fesik, Ph.D. is the Orrin H. Ingram, II Chair in Cancer Research and a Professor of Biochemistry, Pharmacology, and Chemistry in Vanderbilt University School of Medicine. He is also a member of the Vanderbilt Ingram Cancer Center (VICC), the Vanderbilt Institute of Chemical Biology (VICB) and the Center for Structural Biology (CSB).
The focus of his research is on cancer drug discovery using fragment-based approaches and structure-based drug design. Prior to joining Vanderbilt in May, 2009, Dr. Fesik was the Divisional Vice President of Cancer Research at Abbott (2000-2009) where he built a pipeline of compounds that are showing promising anti-cancer activities in early stage clinical trials. In addition, while he was at Abbott, he developed several new NMR methods, determined the three-dimensional structures of several proteins and protein/ligand complexes, pioneered a method for drug discovery called SAR by NMR, and applied this method to identify and optimize ligands for binding to many protein drug targets.
His research has also involved the use of siRNA for target identification and target validation. Dr. Fesik has published more than 240 papers, trained 36 postdoctoral fellows, has been a reviewer for the NIH Biophysical Chemistry Study Section, and has served as a member of the Editorial Boards of the Journal of Medicinal Chemistry, Journal of Biomolecular NMR, Biophysical Journal, Molecular Cell, Chemical Biology & Drug Design, ChemMedChem, Molecular Cancer Therapeutics, Oncogene, Combinatorial Chemistry and High Throughput Screening, and the Highlights Advisory Panel for Nature Reviews Cancer. He has served on the Keystone Scientific Advisory Board and Board of Directors and currently is a member of the Scientific Advisory Board of the UPenn Abramson Cancer Center, Aileron Therapeutics, and the Bruker Board of Directors. He has obtained several awards, including the Chairman’s Award (1996), Outstanding Researcher of the Year Award (1997) , and the Researcher of the Year Team Award (2008) from Abbott, the Servier Lecturer Award (1998) from the University of Montreal, the ASBMB-Fritz Lipmann Lectureship Award (1999), the Lifetime Achievement Award in Nuclear Magnetic Resonance from EAS (2003), the SBS Technology Innovation Award (2010), and the NIH Director's Pioneer Award (2010). Recently he has been elected Fellow of the American Association for the Advancement of Science (AAAS).
Research Description
The focus of our lab is on cancer drug discovery using fragment-based approaches and structure-based design. To accomplish this goal, we have assembled a multidisciplinary team that includes structural biologists, medicinal chemists, and cell biologists. Among them are five research professors and several research assistants, postdoctoral fellows, and graduate students. In our lab, we clone, express, and purify proteins, conduct fragment-based screens, determine the three-dimensional structures of protein/ligand complexes using NMR and/or X-ray crystallography, design and synthesize compounds, and test compounds in primary and secondary biological assays. The cancer drug targets that we are pursuing are highly validated but technically challenging such as K-Ras and c-Myc.
Publications
- Lin, X, David, CA, Donnelly, JB, Michaelides, M, Chandel, NS, Huang, X, Warrior, U, Weinberg, F, Tormos, KV, Fesik, SW, Shen, Y A chemical genomics screen highlights the essential role of mitochondria in HIF-1 regulation. Proc Natl Acad Sci U S A, 105(1), 174-9, 2008.
- Ackler, S, Xiao, Y, Mitten, MJ, Foster, K, Oleksijew, A, Refici, M, Schlessinger, S, Wang, B, Chemburkar, SR, Bauch, J, Tse, C, Frost, DJ, Fesik, SW, Rosenberg, SH, Elmore, SW, Shoemaker, AR ABT-263 and rapamycin act cooperatively to kill lymphoma cells in vitro and in vivo. Mol Cancer Ther, 7(10), 3265-74, 2008.
- Tse, C, Shoemaker, AR, Adickes, J, Anderson, MG, Chen, J, Jin, S, Johnson, EF, Marsh, KC, Mitten, MJ, Nimmer, P, Roberts, L, Tahir, SK, Xiao, Y, Yang, X, Zhang, H, Fesik, S, Rosenberg, SH, Elmore, SW ABT-263: a potent and orally bioavailable Bcl-2 family inhibitor. Cancer Res, 68(9), 3421-8, 2008.
- Shoemaker, AR, Mitten, MJ, Adickes, J, Ackler, S, Refici, M, Ferguson, D, Oleksijew, A, O''Connor, JM, Wang, B, Frost, DJ, Bauch, J, Marsh, K, Tahir, SK, Yang, X, Tse, C, Fesik, SW, Rosenberg, SH, Elmore, SW Activity of the Bcl-2 family inhibitor ABT-263 in a panel of small cell lung cancer xenograft models. Clin Cancer Res, 14(11), 3268-77, 2008.
- Park, CM, Bruncko, M, Adickes, J, Bauch, J, Ding, H, Kunzer, A, Marsh, KC, Nimmer, P, Shoemaker, AR, Song, X, Tahir, SK, Tse, C, Wang, X, Wendt, MD, Yang, X, Zhang, H, Fesik, SW, Rosenberg, SH, Elmore, SW Discovery of an orally bioavailable small molecule inhibitor of prosurvival B-cell lymphoma 2 proteins. J Med Chem, 51(21), 6902-15, 2008.
- Zheng, M, Morgan-Lappe, SE, Yang, J, Bockbrader, KM, Pamarthy, D, Thomas, D, Fesik, SW, Sun, Y Growth inhibition and radiosensitization of glioblastoma and lung cancer cells by small interfering RNA silencing of tumor necrosis factor receptor-associated factor 2. Cancer Res, 68(18), 7570-8, 2008.
- Lin, X, Morgan-Lappe, S, Huang, X, Li, L, Zakula, DM, Vernetti, LA, Fesik, SW, Shen, Y ''Seed'' analysis of off-target siRNAs reveals an essential role of Mcl-1 in resistance to the small-molecule Bcl-2/Bcl-XL inhibitor ABT-737. Oncogene, 26(27), 3972-9, 2007.
- Li, L, Lin, X, Khvorova, A, Fesik, SW, Shen, Y Defining the optimal parameters for hairpin-based knockdown constructs. RNA, 13(10), 1765-74, 2007.
- Huth, JR, Park, C, Petros, AM, Kunzer, AR, Wendt, MD, Wang, X, Lynch, CL, Mack, JC, Swift, KM, Judge, RA, Chen, J, Richardson, PL, Jin, S, Tahir, SK, Matayoshi, ED, Dorwin, SA, Ladror, US, Severin, JM, Walter, KA, Bartley, DM, Fesik, SW, Elmore, SW, Hajduk, PJ Discovery and design of novel HSP90 inhibitors using multiple fragment-based design strategies. Chem Biol Drug Des, 70(1), 1-12, 2007.
- Lerner, CG, Hajduk, PJ, Wagner, R, Wagenaar, FL, Woodall, C, Gu, YG, Searle, XB, Florjancic, AS, Zhang, T, Clark, RF, Cooper, CS, Mack, JC, Yu, L, Cai, M, Betz, SF, Chovan, LE, McCall, JO, Black-Schaefer, CL, Kakavas, SJ, Schurdak, ME, Comess, KM, Walter, KA, Edalji, R, Dorwin, SA, Smith, RA, Hebert, EJ, Harlan, JE, Metzger, RE, Merta, PJ, Baranowski, JL, Coen, ML, Thornewell, SJ, Shivakumar, AG, Saiki, AY, Soni, N, Bui, M, Balli, DJ, Sanders, WJ, Nilius, AM, Holzman, TF, Fesik, SW, Beutel, BA From bacterial genomes to novel antibacterial agents: discovery, characterization, and antibacterial activity of compounds that bind to HI0065 (YjeE) from Haemophilus influenzae. Chem Biol Drug Des, 69(6), 395-404, 2007.
- Morgan-Lappe, SE, Tucker, LA, Huang, X, Zhang, Q, Sarthy, AV, Zakula, D, Vernetti, L, Schurdak, M, Wang, J, Fesik, SW Identification of Ras-related nuclear protein, targeting protein for xenopus kinesin-like protein 2, and stearoyl-CoA desaturase 1 as promising cancer targets from an RNAi-based screen. Cancer Res, 67(9), 4390-8, 2007.
- Tahir, SK, Yang, X, Anderson, MG, Morgan-Lappe, SE, Sarthy, AV, Chen, J, Warner, RB, Ng, SC, Fesik, SW, Elmore, SW, Rosenberg, SH, Tse, C Influence of Bcl-2 family members on the cellular response of small-cell lung cancer cell lines to ABT-737. Cancer Res, 67(3), 1176-83, 2007.
- Bruncko, M, Oost, TK, Belli, BA, Ding, H, Joseph, MK, Kunzer, A, Martineau, D, McClellan, WJ, Mitten, M, Ng, SC, Nimmer, PM, Oltersdorf, T, Park, CM, Petros, AM, Shoemaker, AR, Song, X, Wang, X, Wendt, MD, Zhang, H, Fesik, SW, Rosenberg, SH, Elmore, SW Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL. J Med Chem, 50(4), 641-62, 2007.
- Sarthy, AV, Morgan-Lappe, SE, Zakula, D, Vernetti, L, Schurdak, M, Packer, JC, Anderson, MG, Shirasawa, S, Sasazuki, T, Fesik, SW Survivin depletion preferentially reduces the survival of activated K-Ras-transformed cells. Mol Cancer Ther, 6(1), 269-76, 2007.
- Shoemaker, AR, Oleksijew, A, Bauch, J, Belli, BA, Borre, T, Bruncko, M, Deckwirth, T, Frost, DJ, Jarvis, K, Joseph, MK, Marsh, K, McClellan, W, Nellans, H, Ng, S, Nimmer, P, O''Connor, JM, Oltersdorf, T, Qing, W, Shen, W, Stavropoulos, J, Tahir, SK, Wang, B, Warner, R, Zhang, H, Fesik, SW, Rosenberg, SH, Elmore, SW A small-molecule inhibitor of Bcl-XL potentiates the activity of cytotoxic drugs in vitro and in vivo. Cancer Res, 66(17), 8731-9, 2006.
- Wendt, MD, Shen, W, Kunzer, A, McClellan, WJ, Bruncko, M, Oost, TK, Ding, H, Joseph, MK, Zhang, H, Nimmer, PM, Ng, SC, Shoemaker, AR, Petros, AM, Oleksijew, A, Marsh, K, Bauch, J, Oltersdorf, T, Belli, BA, Martineau, D, Fesik, SW, Rosenberg, SH, Elmore, SW Discovery and structure-activity relationship of antagonists of B-cell lymphoma 2 family proteins with chemopotentiation activity in vitro and in vivo. J Med Chem, 49(3), 1165-81, 2006.
- Petros, AM, Dinges, J, Augeri, DJ, Baumeister, SA, Betebenner, DA, Bures, MG, Elmore, SW, Hajduk, PJ, Joseph, MK, Landis, SK, Nettesheim, DG, Rosenberg, SH, Shen, W, Thomas, S, Wang, X, Zanze, I, Zhang, H, Fesik, SW Discovery of a potent inhibitor of the antiapoptotic protein Bcl-xL from NMR and parallel synthesis. J Med Chem, 49(2), 656-63, 2006.
- Li, L, Lin, X, Shoemaker, AR, Albert, DH, Fesik, SW, Shen, Y Hypoxia-inducible factor-1 inhibition in combination with temozolomide treatment exhibits robust antitumor efficacy in vivo. Clin Cancer Res, 12(15), 4747-54, 2006.
- Morgan-Lappe, S, Woods, KW, Li, Q, Anderson, MG, Schurdak, ME, Luo, Y, Giranda, VL, Fesik, SW, Leverson, JD RNAi-based screening of the human kinome identifies Akt-cooperating kinases: a new approach to designing efficacious multitargeted kinase inhibitors. Oncogene, 25(9), 1340-8, 2006.
- Oltersdorf, T, Elmore, SW, Shoemaker, AR, Armstrong, RC, Augeri, DJ, Belli, BA, Bruncko, M, Deckwerth, TL, Dinges, J, Hajduk, PJ, Joseph, MK, Kitada, S, Korsmeyer, SJ, Kunzer, AR, Letai, A, Li, C, Mitten, MJ, Nettesheim, DG, Ng, S, Nimmer, PM, O''Connor, JM, Oleksijew, A, Petros, AM, Reed, JC, Shen, W, Tahir, SK, Thompson, CB, Tomaselli, KJ, Wang, B, Wendt, MD, Zhang, H, Fesik, SW, Rosenberg, SH An inhibitor of Bcl-2 family proteins induces regression of solid tumours. Nature, 435(7042), 677-81, 2005.
- Hajduk, PJ, Huth, JR, Fesik, SW Druggability indices for protein targets derived from NMR-based screening data. J Med Chem, 48(7), 2518-25, 2005.
- Park, CM, Sun, C, Olejniczak, ET, Wilson, AE, Meadows, RP, Betz, SF, Elmore, SW, Fesik, SW Non-peptidic small molecule inhibitors of XIAP. Bioorg Med Chem Lett, 15(3), 771-5, 2005.
- Fesik, SW Promoting apoptosis as a strategy for cancer drug discovery. Nat Rev Cancer, 5(11), 876-85, 2005.
- Petros, AM, Gunasekera, A, Xu, N, Olejniczak, ET, Fesik, SW Defining the p53 DNA-binding domain/Bcl-x(L)-binding interface using NMR. FEBS Lett, 559(1-3), 171-4, 2004.
- Oost, TK, Sun, C, Armstrong, RC, Al-Assaad, AS, Betz, SF, Deckwerth, TL, Ding, H, Elmore, SW, Meadows, RP, Olejniczak, ET, Oleksijew, A, Oltersdorf, T, Rosenberg, SH, Shoemaker, AR, Tomaselli, KJ, Zou, H, Fesik, SW Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer. J Med Chem, 47(18), 4417-26, 2004.
- Huth, JR, Yu, L, Collins, I, Mack, J, Mendoza, R, Isaac, B, Braddock, DT, Muchmore, SW, Comess, KM, Fesik, SW, Clore, GM, Levens, D, Hajduk, PJ NMR-driven discovery of benzoylanthranilic acid inhibitors of far upstream element binding protein binding to the human oncogene c-myc promoter. J Med Chem, 47(20), 4851-7, 2004.
- Petros, AM, Olejniczak, ET, Fesik, SW Structural biology of the Bcl-2 family of proteins. Biochim Biophys Acta, 1644(2-3), 83-94, 2004.
- Xiao, Z, Chen, Z, Gunasekera, AH, Sowin, TJ, Rosenberg, SH, Fesik, S, Zhang, H Chk1 mediates S and G2 arrests through Cdc25A degradation in response to DNA-damaging agents. J Biol Chem, 278(24), 21767-73, 2003.
- Liu, G, Szczepankiewicz, BG, Pei, Z, Janowick, DA, Xin, Z, Hajduk, PJ, Abad-Zapatero, C, Liang, H, Hutchins, CW, Fesik, SW, Ballaron, SJ, Stashko, MA, Lubben, T, Mika, AK, Zinker, BA, Trevillyan, JM, Jirousek, MR Discovery and structure-activity relationship of oxalylarylaminobenzoic acids as inhibitors of protein tyrosine phosphatase 1B. J Med Chem, 46(11), 2093-103, 2003.
- Szczepankiewicz, BG, Liu, G, Hajduk, PJ, Abad-Zapatero, C, Pei, Z, Xin, Z, Lubben, TH, Trevillyan, JM, Stashko, MA, Ballaron, SJ, Liang, H, Huang, F, Hutchins, CW, Fesik, SW, Jirousek, MR Discovery of a potent, selective protein tyrosine phosphatase 1B inhibitor using a linked-fragment strategy. J Am Chem Soc, 125(14), 4087-96, 2003.
- Yu, L, Oost, TK, Schkeryantz, JM, Yang, J, Janowick, D, Fesik, SW Discovery of aminoglycoside mimetics by NMR-based screening of Escherichia coli A-site RNA. J Am Chem Soc, 125(15), 4444-50, 2003.
- Hajduk, PJ, Mendoza, R, Petros, AM, Huth, JR, Bures, M, Fesik, SW, Martin, YC Ligand binding to domain-3 of human serum albumin: a chemometric analysis. J Comput Aided Mol Des, 17(2-4), 93-102, 2003.
- Huang, Q, Petros, AM, Virgin, HW, Fesik, SW, Olejniczak, ET Solution structure of the BHRF1 protein from Epstein-Barr virus, a homolog of human Bcl-2. J Mol Biol, 332(5), 1123-30, 2003.
- Hajduk, PJ, Shuker, SB, Nettesheim, DG, Craig, R, Augeri, DJ, Betebenner, D, Albert, DH, Guo, Y, Meadows, RP, Xu, L, Michaelides, M, Davidsen, SK, Fesik, SW NMR-based modification of matrix metalloproteinase inhibitors with improved bioavailability. J Med Chem, 45(26), 5628-39, 2002.
- Huang, Q, Petros, AM, Virgin, HW, Fesik, SW, Olejniczak, ET Solution structure of a Bcl-2 homolog from Kaposi sarcoma virus. Proc Natl Acad Sci U S A, 99(6), 3428-33, 2002.
- Liu, G, Huth, JR, Olejniczak, ET, Mendoza, R, DeVries, P, Leitza, S, Reilly, EB, Okasinski, GF, Fesik, SW, von Geldern, TW Novel p-arylthio cinnamides as antagonists of leukocyte function-associated antigen-1/intracellular adhesion molecule-1 interaction. 2. Mechanism of inhibition and structure-based improvement of pharmaceutical properties. J Med Chem, 44(8), 1202-10, 2001.
- Mao, H, Hajduk, PJ, Craig, R, Bell, R, Borre, T, Fesik, SW Rational design of diflunisal analogues with reduced affinity for human serum albumin. J Am Chem Soc, 123(43), 10429-35, 2001.
- Petros, AM, Medek, A, Nettesheim, DG, Kim, DH, Yoon, HS, Swift, K, Matayoshi, ED, Oltersdorf, T, Fesik, SW Solution structure of the antiapoptotic protein bcl-2. Proc Natl Acad Sci U S A, 98(6), 3012-7, 2001.
- Liu, Z, Sun, C, Olejniczak, ET, Meadows, RP, Betz, SF, Oost, T, Herrmann, J, Wu, JC, Fesik, SW Structural basis for binding of Smac/DIABLO to the XIAP BIR3 domain. Nature, 408(6815), 1004-8, 2001.
- Riedl, SJ, Renatus, M, Schwarzenbacher, R, Zhou, Q, Sun, C, Fesik, SW, Liddington, RC, Salvesen, GS Structural basis for the inhibition of caspase-3 by XIAP. Cell, 104(5), 791-800, 2001.
- Fesik, SW, Shi, Y Structural biology. Controlling the caspases. Science, 294(5546), 1477-8, 2001.
- Hajduk, PJ, Gomtsyan, A, Didomenico, S, Cowart, M, Bayburt, EK, Solomon, L, Severin, J, Smith, R, Walter, K, Holzman, TF, Stewart, A, McGaraughty, S, Jarvis, MF, Kowaluk, EA, Fesik, SW Design of adenosine kinase inhibitors from the NMR-based screening of fragments. J Med Chem, 43(25), 4781-6, 2000.
- Hajduk, PJ, Boyd, S, Nettesheim, D, Nienaber, V, Severin, J, Smith, R, Davidson, D, Rockway, T, Fesik, SW Identification of novel inhibitors of urokinase via NMR-based screening. J Med Chem, 43(21), 3862-6, 2000.
- Fesik, SW Insights into programmed cell death through structural biology. Cell, 103(2), 273-82, 2000.
- Huth, JR, Olejniczak, ET, Mendoza, R, Liang, H, Harris, EA, Lupher, ML, Wilson, AE, Fesik, SW, Staunton, DE NMR and mutagenesis evidence for an I domain allosteric site that regulates lymphocyte function-associated antigen 1 ligand binding. Proc Natl Acad Sci U S A, 97(10), 5231-6, 2000.
- Sun, C, Cai, M, Meadows, RP, Xu, N, Gunasekera, AH, Herrmann, J, Wu, JC, Fesik, SW NMR structure and mutagenesis of the third Bir domain of the inhibitor of apoptosis protein XIAP. J Biol Chem, 275(43), 33777-81, 2000.
- Losonczi, JA, Olejniczak, ET, Betz, SF, Harlan, JE, Mack, J, Fesik, SW NMR studies of the anti-apoptotic protein Bcl-xL in micelles. Biochemistry, 39(36), 11024-33, 2000.
- Hajduk, PJ, Bures, M, Praestgaard, J, Fesik, SW Privileged molecules for protein binding identified from NMR-based screening. J Med Chem, 43(18), 3443-7, 2000.
- Cai, M, Wang, H, Olejniczak, ET, Meadows, RP, Gunasekera, AH, Xu, N, Fesik, SW Accurate measurement of H(N)-H(alpha) residual dipolar couplings in proteins. J Magn Reson, 139(2), 451-3, 1999.
- Martin, DA, Zheng, L, Siegel, RM, Huang, B, Fisher, GH, Wang, J, Jackson, CE, Puck, JM, Dale, J, Straus, SE, Peter, ME, Krammer, PH, Fesik, S, Lenardo, MJ Defective CD95/APO-1/Fas signal complex formation in the human autoimmune lymphoproliferative syndrome, type Ia. Proc Natl Acad Sci U S A, 96(8), 4552-7, 1999.
- Sun, C, Cai, M, Gunasekera, AH, Meadows, RP, Wang, H, Chen, J, Zhang, H, Wu, W, Xu, N, Ng, SC, Fesik, SW NMR structure and mutagenesis of the inhibitor-of-apoptosis protein XIAP. Nature, 401(6755), 818-22, 1999.
- Hajduk, PJ, Zhou, MM, Fesik, SW NMR-based discovery of phosphotyrosine mimetics that bind to the Lck SH2 domain. Bioorg Med Chem Lett, 9(16), 2403-6, 1999.
- Hajduk, PJ, Meadows, RP, Fesik, SW NMR-based screening in drug discovery. Q Rev Biophys, 32(3), 211-40, 1999.
- Hajduk, PJ, Dinges, J, Schkeryantz, JM, Janowick, D, Kaminski, M, Tufano, M, Augeri, DJ, Petros, A, Nienaber, V, Zhong, P, Hammond, R, Coen, M, Beutel, B, Katz, L, Fesik, SW Novel inhibitors of Erm methyltransferases from NMR and parallel synthesis. J Med Chem, 42(19), 3852-9, 1999.
- Eberstadt, M, Huang, B, Chen, Z, Meadows, RP, Ng, SC, Zheng, L, Lenardo, MJ, Fesik, SW NMR structure and mutagenesis of the FADD (Mort1) death-effector domain. Nature, 392(6679), 941-5, 1998.
- Liu, X, Wang, H, Eberstadt, M, Schnuchel, A, Olejniczak, ET, Meadows, RP, Schkeryantz, JM, Janowick, DA, Harlan, JE, Harris, EA, Staunton, DE, Fesik, SW NMR structure and mutagenesis of the N-terminal Dbl homology domain of the nucleotide exchange factor Trio. Cell, 95(2), 269-77, 1998.
- Betz, SF, Schnuchel, A, Wang, H, Olejniczak, ET, Meadows, RP, Lipsky, BP, Harris, EA, Staunton, DE, Fesik, SW Solution structure of the cytohesin-1 (B2-1) Sec7 domain and its interaction with the GTPase ADP ribosylation factor 1. Proc Natl Acad Sci U S A, 95(14), 7909-14, 1998.
- Minn, AJ, Vélez, P, Schendel, SL, Liang, H, Muchmore, SW, Fesik, SW, Fill, M, Thompson, CB Bcl-x(L) forms an ion channel in synthetic lipid membranes. Nature, 385(6614), 353-7, 1997.
- Hajduk, PJ, Meadows, RP, Fesik, SW Discovering high-affinity ligands for proteins. Science, 278(5337), 497,499, 1997.
- Hajduk, PJ, Dinges, J, Miknis, GF, Merlock, M, Middleton, T, Kempf, DJ, Egan, DA, Walter, KA, Robins, TS, Shuker, SB, Holzman, TF, Fesik, SW NMR-based discovery of lead inhibitors that block DNA binding of the human papillomavirus E2 protein. J Med Chem, 40(20), 3144-50, 1997.
- Yu, L, Petros, AM, Schnuchel, A, Zhong, P, Severin, JM, Walter, K, Holzman, TF, Fesik, SW Solution structure of an rRNA methyltransferase (ErmAM) that confers macrolide-lincosamide-streptogramin antibiotic resistance. Nat Struct Biol, 4(6), 483-9, 1997.
- Sattler, M, Liang, H, Nettesheim, D, Meadows, RP, Harlan, JE, Eberstadt, M, Yoon, HS, Shuker, SB, Chang, BS, Minn, AJ, Thompson, CB, Fesik, SW Structure of Bcl-xL-Bak peptide complex: recognition between regulators of apoptosis. Science, 275(5302), 983-6, 1997.
- Eberstadt, M, Huang, B, Olejniczak, ET, Fesik, SW The lymphoproliferation mutation in Fas locally unfolds the Fas death domain. Nat Struct Biol, 4(12), 983-5, 1997.
- Liang, H, Fesik, SW Three-dimensional structures of proteins involved in programmed cell death. J Mol Biol, 274(3), 291-302, 1997.
- Yu, L, Zhu, CX, Tse-Dinh, YC, Fesik, SW Backbone dynamics of the C-terminal domain of Escherichia coli topoisomerase I in the absence and presence of single-stranded DNA. Biochemistry, 35(30), 9661-6, 1996.
- Shuker, SB, Hajduk, PJ, Meadows, RP, Fesik, SW Discovering high-affinity ligands for proteins: SAR by NMR. Science, 274(5292), 1531-4, 1996.
- Ravichandran, KS, Igras, V, Shoelson, SE, Fesik, SW, Burakoff, SJ Evidence for a role for the phosphotyrosine-binding domain of Shc in interleukin 2 signaling. Proc Natl Acad Sci U S A, 93(11), 5275-80, 1996.
- Huang, B, Eberstadt, M, Olejniczak, ET, Meadows, RP, Fesik, SW NMR structure and mutagenesis of the Fas (APO-1/CD95) death domain. Nature, 384(6610), 638-41, 1996.
- Liang, H, Petros, AM, Meadows, RP, Yoon, HS, Egan, DA, Walter, K, Holzman, TF, Robins, T, Fesik, SW Solution structure of the DNA-binding domain of a human papillomavirus E2 protein: evidence for flexible DNA-binding regions. Biochemistry, 35(7), 2095-103, 1996.
- Zhou, MM, Huang, B, Olejniczak, ET, Meadows, RP, Shuker, SB, Miyazaki, M, Trüb, T, Shoelson, SE, Fesik, SW Structural basis for IL-4 receptor phosphopeptide recognition by the IRS-1 PTB domain. Nat Struct Biol, 3(4), 388-93, 1996.
- Sattler, M, Fesik, SW Use of deuterium labeling in NMR: overcoming a sizeable problem. Structure, 4(11), 1245-9, 1996.
- Muchmore, SW, Sattler, M, Liang, H, Meadows, RP, Harlan, JE, Yoon, HS, Nettesheim, D, Chang, BS, Thompson, CB, Wong, SL, Ng, SL, Fesik, SW X-ray and NMR structure of human Bcl-xL, an inhibitor of programmed cell death. Nature, 381(6580), 335-41, 1996.
- Yu, L, Zhu, CX, Tse-Dinh, YC, Fesik, SW Solution structure of the C-terminal single-stranded DNA-binding domain of Escherichia coli topoisomerase I. Biochemistry, 34(23), 7622-8, 1995.
- Zhou, MM, Meadows, RP, Logan, TM, Yoon, HS, Wade, WS, Ravichandran, KS, Burakoff, SJ, Fesik, SW Solution structure of the Shc SH2 domain complexed with a tyrosine-phosphorylated peptide from the T-cell receptor. Proc Natl Acad Sci U S A, 92(17), 7784-8, 1995.
- Harlan, JE, Yoon, HS, Hajduk, PJ, Fesik, SW Structural characterization of the interaction between a pleckstrin homology domain and phosphatidylinositol 4,5-bisphosphate. Biochemistry, 34(31), 9859-64, 1995.
- Zhou, MM, Ravichandran, KS, Olejniczak, EF, Petros, AM, Meadows, RP, Sattler, M, Harlan, JE, Wade, WS, Burakoff, SJ, Fesik, SW Structure and ligand recognition of the phosphotyrosine binding domain of Shc. Nature, 378(6557), 584-92, 1995.
- Meadows, RP, Olejniczak, ET, Fesik, SW A computer-based protocol for semiautomated assignments and 3D structure determination of proteins. J Biomol NMR, 4(1), 79-96, 1994.
- Hansen, AP, Petros, AM, Meadows, RP, Fesik, SW Backbone dynamics of a two-domain protein: 15N relaxation studies of the amino-terminal fragment of urokinase-type plasminogen activator. Biochemistry, 33(51), 15418-24, 1994.
- Petros, AM, Fesik, SW Nuclear magnetic resonance methods for studying protein-ligand complexes. Methods Enzymol, 239717-39, 1994.
- Harlan, JE, Hajduk, PJ, Yoon, HS, Fesik, SW Pleckstrin homology domains bind to phosphatidylinositol-4,5-bisphosphate. Nature, 371(6493), 168-70, 1994.
- Logan, TM, Zhou, MM, Nettesheim, DG, Meadows, RP, Van Etten, RL, Fesik, SW Solution structure of a low molecular weight protein tyrosine phosphatase. Biochemistry, 33(37), 11087-96, 1994.
- Yoon, HS, Hajduk, PJ, Petros, AM, Olejniczak, ET, Meadows, RP, Fesik, SW Solution structure of a pleckstrin-homology domain. Nature, 369(6482), 672-5, 1994.
- Hansen, AP, Petros, AM, Meadows, RP, Nettesheim, DG, Mazar, AP, Olejniczak, ET, Xu, RX, Pederson, TM, Henkin, J, Fesik, SW Solution structure of the amino-terminal fragment of urokinase-type plasminogen activator. Biochemistry, 33(16), 4847-64, 1994.
- Liang, H, Mao, X, Olejniczak, ET, Nettesheim, DG, Yu, L, Meadows, RP, Thompson, CB, Fesik, SW Solution structure of the ets domain of Fli-1 when bound to DNA. Nat Struct Biol, 1(12), 871-5, 1994.
- Liang, H, Olejniczak, ET, Mao, X, Nettesheim, DG, Yu, L, Thompson, CB, Fesik, SW The secondary structure of the ets domain of human Fli-1 resembles that of the helix-turn-helix DNA-binding motif of the Escherichia coli catabolite gene activator protein. Proc Natl Acad Sci U S A, 91(24), 11655-9, 1994.
- Logan, TM, Olejniczak, ET, Xu, RX, Fesik, SW A general method for assigning NMR spectra of denatured proteins using 3D HC(CO)NH-TOCSY triple resonance experiments. J Biomol NMR, 3(2), 225-31, 1993.
- Xu, RX, Meadows, RP, Fesik, SW Heteronuclear 3D NMR studies of water bound to an FK506 binding protein/immunosuppressant complex. Biochemistry, 32(10), 2473-80, 1993.
- Fesik, SW NMR structure-based drug design. J Biomol NMR, 3(3), 261-9, 1993.
- Thériault, Y, Logan, TM, Meadows, R, Yu, L, Olejniczak, ET, Holzman, TF, Simmer, RL, Fesik, SW Solution structure of the cyclosporin A/cyclophilin complex by NMR. Nature, 361(6407), 88-91, 1993.
- Meadows, RP, Nettesheim, DG, Xu, RX, Olejniczak, ET, Petros, AM, Holzman, TF, Severin, J, Gubbins, E, Smith, H, Fesik, SW Three-dimensional structure of the FK506 binding protein/ascomycin complex in solution by heteronuclear three- and four-dimensional NMR. Biochemistry, 32(3), 754-65, 1993.
- Olejniczak, ET, Xu, RX, Fesik, SW A 4D HCCH-TOCSY experiment for assigning the side chain 1H and 13C resonances of proteins. J Biomol NMR, 2(6), 655-9, 1992.
- Hansen, AP, Petros, AM, Mazar, AP, Pederson, TM, Rueter, A, Fesik, SW A practical method for uniform isotopic labeling of recombinant proteins in mammalian cells. Biochemistry, 31(51), 12713-8, 1992.
- Xu, RX, Olejniczak, ET, Fesik, SW Stereospecific assignments and chi 1 rotamers for FKBP when bound to ascomycin from 3JH alpha,H beta and 3HN,H beta coupling constants. FEBS Lett, 305(2), 137-43, 1992.
- Fesik, SW NMR studies of molecular complexes as a tool in drug design. J Med Chem, 34(10), 2937-45, 1991.
- Fesik, SW, Zuiderweg, ER Heteronuclear three-dimensional NMR spectroscopy of isotopically labelled biological macromolecules. Q Rev Biophys, 23(2), 97-131, 1990.
- Fesik, SW, Gampe, RT, Holzman, TF, Egan, DA, Edalji, R, Luly, JR, Simmer, R, Helfrich, R, Kishore, V, Rich, DH Isotope-edited NMR of cyclosporin A bound to cyclophilin: evidence for a trans 9,10 amide bond. Science, 250(4986), 1406-9, 1990.
- Fesik, SW, Zuiderweg, ER, Olejniczak, ET, Gampe, RT NMR methods for determining the structures of enzyme/inhibitor complexes as an aid in drug design. Biochem Pharmacol, 40(1), 161-7, 1990.
- Zuiderweg, ER, Fesik, SW Heteronuclear three-dimensional NMR spectroscopy of the inflammatory protein C5a. Biochemistry, 28(6), 2387-91, 1989.
- Fesik, SW, Luly, JR, Erickson, JW, Abad-Zapatero, C Isotope-edited proton NMR study on the structure of a pepsin/inhibitor complex. Biochemistry, 27(22), 8297-301, 1988.
- Olejniczak, ET, Gampe, RT, Rockway, TW, Fesik, SW NMR study of the solution conformation of rat atrial natriuretic factor 7-23 in sodium dodecyl sulfate micelles. Biochemistry, 27(18), 7124-31, 1988.
- Fesik, SW, Bolis, G, Sham, HL, Olejniczak, ET Structure refinement of a cyclic peptide from two-dimensional NMR data and molecular modeling. Biochemistry, 26(7), 1851-9, 1987.
- Kohlbrenner, WE, Fesik, SW Determination of the anomeric specificity of the Escherichia coli CTP:CMP-3-deoxy-D-manno-octulosonate cytidylyltransferase by 13C NMR spectroscopy. J Biol Chem, 260(27), 14695-700, 1985.
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