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Fesik Lab

Stephen W. Fesik, Ph.D.

Orrin H. Ingram, II Chair in Cancer Research
Professor of Biochemistry, Pharmacology, and Chemistry

Mailing Address:  2215 Garland Ave., 607 Light Hall
City:                         Nashville, TN 37232-0146
Office:                      634-A  Robinson Research Building
Laboratory:             802/804  Robinson Research Building
Office Phone:          615-322-6303
Email:                       stephen.fesik@vanderbilt.edu

Faculty Profile

Principal Investigator (BRET Faculty Member)
Member, Vanderbilt Institute of Chemical Biology (VICB)
Member, Vanderbilt Ingram Cancer Center (VICC)
Member, Center for Structural Biology (CSB)

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 anti-cancer compounds. 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.

Dr. Fesik has published more than 270 papers, trained aver 55 postdoctoral fellows, has been a reviewer for the NIH Biophysical Chemistry Study Section, the NCI Experimental Therapeutics (NExT) Program, and CPRIT. He has also 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, Cancer Research, Cell Death and Differentiation,and the Highlights Advisory Panel for Nature Reviews Cancer. Dr. Fesik has served on the Keystone Scientific Advisory Board, Board of Directors and the Scientific Advisory Board of the UPenn Abramson Cancer Center, the Bruker Board of Directors, and the Scientific Advisory Board of Aileron Therapeutics.

Dr. Fesik 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), the NIH Director’s Pioneer Award (2010), the Fellow of the American Association for the Advancement of Science (AAAS) (2010), the AACR Award for Outstanding Achievement in Chemistry in Cancer Research (2012), and The Lustgarten Foundation Research Investigator Award (2015).

Click here to view a current list of Dr. Fesik’s PubMed publications.

Selected Publications (from over 270)

  • Fesik, S.W.  Isotope-edited NMR spectroscopy.  Nature, 232, 865-866 (1988).
  • Fesik, S.W. and E.R.P. Zuiderweg.  Heteronuclear three dimensional NMR spectroscopy.  A strategy for the simplification of homonuclear two dimensional NMR spectra.  J. Magn. Reson., 78, 588-593 (1988).
  • Fesik, S.W., R.T. Gampe, Jr., T.F. Holzman, D.A. Egan, R. Edalji, J.R. Luly, R. Simmer, and R. Helfrich. Isotope-edited NMR of cyclosporin A bound to cyclophilin:  Evidence for a trans 9,10 amide bond.  Science, 250, 1406-1409 (1990).
  • Zuiderweg, E.R.P., A.M. Petros, S.W. Fesik, and E.T. Olejniczak. Four-dimensional [13C,1H,13C,1H]HMQC-NOE-HMQC NMR spectroscopy:  Resolving tertiary NOE distance constraints in the spectra of larger proteins.  J. Am. Chem. Soc., 113,  370-372 (1991).
  • Theriault, Y., T.M. Logan, R. Meadows, L. Yu, E. T. Olejniczak, T.F. Holzman, R.L. Simmer, and S.W. Fesik.  Solution structure of the cyclosporin A/cyclophilin complex by NMR.  Nature, 361, 88-91 (1993).
  • Yoon, H.S., P.J. Hajduk, A.M. Petros, E.T. Olejniczak, R.P. Meadows, and S.W. Fesik. Solution structure of a pleckstrin homology domain. Nature, 369, 672-675 (1994).
  • Harlan, J.E., P.J. Hajduk, H.S. Yoon, and S.W. Fesik.  Pleckstrin homology domains bind to phosphatidylinositol 4,5-bisphosphate. Nature, 371, 167-170 (1994).
  • Zhou, M.-M., K.S. Ravichandran, E.T. Olejniczak, A.M. Petros, R.P. Meadows, M. Sattler, J.E. Harlan, W.S. Wade, S.J. Burakoff, and S.W. Fesik.  Structure and ligand recognition of the phosphotyrosine binding domain of Shc.  Nature, 378, 584-592 (1995).
  • Muchmore, S.W., M. Sattler, H. Liang, R.P. Meadows, J.E. Harlan, H.S. Yoon, D. Nettesheim, B.S. Chang, C.B. Thompson, S.-L. Wang, S.-C. Ng, and S.W. Fesik.  X-ray and NMR structure of human Bcl-XL, an inhibitor of programmed cell death.  Nature, 381, 335-341 (1996).
  • Shuker, S.B., P.J. Hajduk, R.P. Meadows, and S.W. Fesik.  Discovering high-affinity ligands for proteins:  SAR by NMR.  Science, 274, 1531-1534 (1996).
  • Huang, B., M. Eberstadt, E.T. Olejniczak, R.P. Meadows, and S.W. Fesik.  NMR structure and mutagenesis of the Fas (APO-1/CD95) death domain.  Nature, 384, 638-641 (1996).
  • Minn, A. J., P. Velez, S. L. Schendel, H. Liang, S. W. Muchmore, S. W. Fesik, M. Fill, and C. B. Thompson. Bcl-xL forms an ion channel in synthetic lipid membranes.  Nature, 385, 353-357 (1997).
    Sattler, M., H. Liang, D. Nettesheim, R.P. Meadows, J.E. Harlan, M. Eberstadt, H. Yoon, S.B. Shuker, B. Chang, A.J. Minn, C.B. Thompson, and S.W. Fesik.  Structure of Bcl-xL/Bak peptide complex: Recognition between regulators of apoptosis.  Science, 275, 983-986 (1997).
  • Hajduk, P. J., G. Sheppard, D. G. Nettesheim, E. T. Olejniczak, S. B. Shuker, R. P. Meadows, D. H. Steinman, G. M. Carrera, Jr., P. A. Marcotte, J. Severin, K. Walter, H. Smith, E. Gubbins, T. F. Holzman, D. W. Morgan, S. K. Davidsen, J. B. Summers, and S. W. Fesik.  Discovery of potent nonpeptide inhibitors of stromelysin using SAR by NMR.  J. Am. Chem. Soc., 119, 5818-5827 (1997).
  • Olejniczak, E. T., P. J. Hajduk, P. A. Marcotte, D. G. Nettesheim, R. P. Meadows, R. Edalji, T. F. Holzman, and S. W. Fesik.  Stromelysin inhibitors designed from weakly bound fragments:  Effects of linking and cooperativity.  J. Am. Chem. Soc., 119, 5828-5832 (1997).
  • Hajduk, P.J., J. Dinges, G.F. Miknis, M. Merlock, T. Middleton, D.J. Kempf, D.A. Egan, K.A. Walter, T. Robbins, S.B. Shuker, T.F. Holzman, and S.W. Fesik. NMR-based discovery of lead inhibitors that block DNA-binding of the human papillomavirus E2 protein.  J. Med. Chem., 40, 3144-3150 (1997).
  • Hajduk, P.J., E.T. Olejniczak,  and S.W. Fesik.  One dimensional relaxation- and diffusion-edited NMR methods for screening compounds that bind to macromolecules.  J. Am. Chem. Soc., 119, 12257-12261 (1997).
  • Hajduk, P.J., R.P. Meadows, and S.W. Fesik.  Discovering high-affinity ligands for proteins.  Science, 278, 497-499 (1997).
  • Eberstadt, M., B. Huang, Z. Chen, R. P. Meadows, S. Ng, L. Zheng, and S. W. Fesik.  NMR structure and mutagenesis of the FADD (Mort1) death-effector domain.  Nature, 392, 941-945 (1998).
  • Betz, S.F., A. Schnuchel, H. Wang, E.T. Olejniczak, R.P. Meadows, B.P. Lipsky, E.A.S. Harris, D.E. Staunton, and S.W. Fesik.  Solution structure of the cytohesin-1 (B2-1) Sec7 domain and its interaction with the GTPase ADP ribosylation factor 1.  Proc. Natl. Acad. Sci., USA, 95, 7909-7914 (1998).
  • Liu, X., H. Wang, M. Eberstadt, A. Schnuchel, E.T. Olejniczak, R.P. Meadows, J.M. Schkeryantz, D.A. Janowick, J.E. Harlan, E.A.S. Harris, D.E. Staunton, S.W. Fesik.  NMR structure and mutagenesis of the N-terminal Dbl homology domain of the nucleotide exchange factor Trio.  Cell, 95, 269-277 (1998).
  • Hajduk, P.J., J. Dinges, J. M. Schkeryantz, D. Janowick, M. Kaminski, M. Tufano, D. J. Augeri, A. Petros. V.  Nienaber, P. Zhong, R. Hammond, M. Coen, B. Beutel, L. Katz, and S. W. Fesik. Novel inhibitors of Erm methyltransferases from NMR and parallel synthesis.  J.   Med. Chem., 42, 3852-3859 (1999).
  • Sun, C., M. Cai, A. H. Gunasekera, R. P. Meadows, H. Wang, J. Chen, H. Zhang, W. Wu,  N. Xu, S.-C. Ng, and S. W. Fesik.  NMR structure and mutagenesis of the inhibitor of apoptosis protein XIAP.  Nature, 401,818-822 (1999).
  • Huth, J. R., E. T. Olejniczak, R. Mendoza, H. Liang, E. A. S. Harris, M. L. Lupher Jr., A. E. Wilson, S. W. Fesik, and D. E. Staunton.  NMR and mutagenesis evidence for an I domain allosteric site that regulates lymphocyte function-associated antigen 1 ligand binding. Proc. Natl. Acad. Sci., USA, 97, 5231-5236 (2000).
  • Hajduk, P. J., D. J. Augeri, J.Mack, R.  Mendoza, J. Yang, S. F. Betz,  and S. W. Fesik.  NMR-based screening of proteins containing 13C-labeled methyl groups. J. Am. Chem. Soc., 122, 7898-7904 (2000).
  • Fesik, S. W.  Insights into Programmed Cell Death through Structural Biology.  Cell, 103, 273-282 (2000).
  • Hajduk, P. J., S. Boyd, D.  Nettesheim, A. Rueter, V.  Nienaber, J.  Severin, R.  Smith,   D. Davidson, T.  Rockway, and S. W. Fesik.  The identification of novel inhibitors of urokinase  using NMR-based screening.  J. Med. Chem., 43, 3862-3866 (2000).
  • Hajduk, P. J., M. Bures, J.  Praestgaard, and S. W. Fesik.  Priviledged molecules for protein binding identified from NMR-based screening.  J. Med. Chem., 43, 3443-3447 (2000).
  • H. Albert, Y. Guo, R. P. Meadows, M. Michaelides, S. K. Davidsen, and S. W. Fesik. NMR- Hajduk, P. J., A. Gomstyan, S. Didomenico, M. Cowart, E. K. Bayburt, L. Solomon, J. Severin, R. Smith, K. Walter, T. F. Holzman, A. Stewart, S. McGaraughty, M. F. Jarvis, E. Kowaluk, and S. W. Fesik.  Design of adenosine kinase inhibitors from the NMR-based screening of fragments.  J. Med. Chem., 43, 4781-4786 (2000).
  • Liu, Z., C. Sun, E. T. Olejniczak, R. P. Meadows, S. F. Betz, T. Oost, J. Herrman, J. C. Wu, and S. W. Fesik.  Structural basis for binding of Smac/DIABLO to the XIAP Bir3 domain.  Nature, 408, 1004-1008 (2000).
  • Petros, A. M., A. Medek, D. G. Netthesheim, D. H. Kim, H. Yoon, R. P. Meadows, K. Swift, E.D. Matayoshi, T. Oltersdorf, and S.W. Fesik.  Solution structure of the anti-apoptotic protein Bcl-2.  Proceed. Natl. Acad. Sci., USA, 98, 3012-3017 (2001).
  • Fesik, S. W., and Y. Shi.  Controlling the caspases.  Science, 294, 1477-1478 (2001).
  • Riedl S. J., M. Renatus, R. Schwarzenbacher, Q. Zhou, C. Sun, S. W. Fesik, R. C. Liddington, and G. S. Salvesen.  Structural basis for the inhibition of caspase-3 by XIAP.  Cell, 104, 791-800 (2001).
  • Hajduk, P. J., S. B. Shuker, D. G. Nettesheim, L. Xu, D. J. Augeri, D. Betebenner, R. Craig, D. based modification of matrix metalloproteinase inhibitors with improved bioavailability. J. Med. Chem., 45, 5628-5639 (2002).
  • Yu, L., T. K. Oost, J. M. Schkeryantz, J. Yang, D. Janowick, and S. W. Fesik.  Discovery of aminoglycoside mimetics by NMR-based screening of Escherichia coli A-site RNA.  J. Am. Chem. Soc., 125, 4444-4450 (2003).
  • Oost, T., C. Sun, R.C. Armstrong, A. Al-Assaad, S.F. Betz, T.L. Deckwerth, H. Ding, S.W. Elmore, R.P. Meadows, E.T. Olejniczak, A. Oleksijew, T. Oltersdorf, S.H. Rosenberg, A.R. Shoemaker, K.J. Tomaselli, H. Zou and S.W. Fesik.  Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.  J. Med. Chem. 47, 4417-4426 (2004).
  • Oltersdorf, T., S.W. Elmore, A.R. Shoemaker, R.C. Armstrong, D.J. Augeri, B.A. Belli, M. Bruncko, T.L. Deckwerth, J. Dinges, P.J. Hajduk, M.K. Joseph, S. Kitada, S.J. Korsmeyer, A.R. Kunzer, A. Letai, C. Li, M.J. Mitten, D.G. Nettesheim, S. Ng, P.M. Nimmer, J.M. O’Connor, A. Oleksijew, A.M. Petros, J.C. Reed, W. Shen, S.K. Tahir, C.B. Thompson, K.J. Tomaselli, B. Wang, M.D. Wendt, H. Zhang, S.W. Fesik and S.H. Rosenberg.  An inhibitor of Bcl-2 family proteins induces regression of solid tumors.  Nature 435, 677-681 (2005).
  • Li, L., X. Lin, M. Staver, A. Shoemaker, D. Semizarov, S.W. Fesik and Y. Shen.  Evaluating hypoxia-inducible factor-1α as a cancer therapeutic target via inducible RNA interference in vivo.  Cancer Res. 65, 7249-7258 (2005).
  • Morgan-Lappe, S., K.W. Woods, Q. Li, M.G. Anderson, M. Schurdak, Y. Luo, V.L. Giranda, S.W. Fesik and J.D. Leverson.  RNAi-based screening of the human kinome identifies Akt-cooperating kinases:  A new approach to designing efficacious multi-targeted kinase inhibitors.  Oncogene 25, 1340-1348 (2006).
  • Fesik, S.W.  Promoting apoptosis as a strategy for cancer drug discovery.  Nature Rev. Cancer 5, 876-885 (2005).
  • Petros, A.M., J. Dinges, D.J. Augeri, S.A. Baumeister, D.A. Betebenner, M.G. Bures, S.W. Elmore, P.J. Hajduk, M.K. Joseph, S.K. Landis, D.G. Nettesheim, S.H. Rosenberg, W. Shen, S. Thomas, X. Wang, I. Zanze, H. Zhang and S.W. Fesik.  Discovery of a potent inhibitor of the antiapoptotic protein Bcl-XL from NMR and parallel synthesis.  J. Med Chem. 49, 656-663 (2006).
  • Tahir, S.K., X. Yang, M.G. Anderson, S.E. Morgan-Lappe, A.Sarthy, J. Chen, R.B. Warner, S-C. Ng, S. Fesik, S. Elmore, S. Rosenberg, and C. Tse.  Influence of Bcl-2 family members on the cellular response of Small Cell Lung Cancer cell lines to ABT-737. Cancer Res. 67, 1176-1183 (2007).
  • Sarthy, A., S. Morgan-Lappe, D. Zakula, L. Vernetti, M. Schurdak, J. C.L. Packer, M. G. Anderson, S. Shirasawa, T. Sasazuki, and S.W. Fesik.  Survivin depletion preferentially reduces the survival of activated k-ras-transformed cells.  Mol. Cancer Ther. 6, 269-276 (2007).
  • Morgan-Lappe, S.E., X. Huang, L. Garcia, C. Zhang, A.V. Sarthy, D. Zakula, L. Vernetti, M. Schurdak, J. Wang, and S.W. Fesik.  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, 4390-4398 (2007).
  • Tse, C., A.R. Shoemaker, J. Adickes, M.G. Anderson, J. Chen, S. Jin, E.F. Johnson, K.C. Marsh, M.J. Mitten, P. Nimmer, L. Roberts, S.K. Tahir, Y. Xiao, X. Yang, H. Zhang, S. Fesik, S.H. Rosenberg, and S.W. Elmore.  ABT-263:  a potent and orally bioavailable Bcl-2 family inhibitor.  Cancer Res.68, 3421-3428 (2008).
  • Shah O.J., Lin X., Li L., Huang X., Li J., Anderson M.G., Tang H., Rodriguez L.E., Warder S.E., McLoughlin S., Chen J., Palma J., Glaser K.B., Donawho C.K., Fesik S.W., Shen Y. Bcl-XL represents a druggable molecular vulnerability during aurora B inhibitor-mediated polyploidization. Proc. Natl. Acad. Sci., USA, 107, 12634-12639 (2010). PMC2906553
  • Petros A.M., Huth J.R., Oost T., Park C.M., Ding H., Wang X., Zhang H., Nimmer P., Mendoza R., Sun C., Mack J., Walter K., Dorwin S., Gramling E., Ladror U., Rosenberg S.H., Elmore S.W., Fesik S.W., Hajduk P.J. Discovery of a potent and selective Bcl-2 inhibitor using SAR by NMR. Bioorg. Med. Chem. Lett., 20, 6587-6591 (2010).
  • Lin X., Li L., Wang R., Wilcox D., Zhao X., Song J., Huang X., Hansen T.M., Dande P., Wada C., Hubbard R.D., Kohlbrenner W.M., Fesik S.W., Shen Y. A robust in vivo positive-readout system for monitoring siRNA delivery to xenograft tumors. RNA, 17, 603-612. (2011).
  • Souza-Fagundes E.M., Frank A.O., Feldkamp M.D., Dorset D.C., Chazin W.J., Rossanese O.W., Olejniczak E.T., Fesik S.W. A high-throughput fluorescence polarization anisotropy assay for the 70N domain of Replication Protein A. Anal. Biochem., 421, 742–749 (2012). PMC3274598
  • Sun Q, Burke JP, Phan J, Burns MC, Olejniczak ET, Waterson AG, Lee T, Rossanese OW, Fesik SW. Discovery of Small Molecules that Bind to K-Ras and Inhibit Sos-Mediated Activation. Angew. Chem. Int. Ed. Engl. 51(25): 6140-3 (2012). PMCID: PMC3620661
  • Friberg A, Vigil D, Zhao B, Daniels RN, Burke JP, Garcia-Barrantes P, Camper D, Chauder B, Lee T, Olejniczak ET, Fesik SW. Discovery of potent myeloid cell leukemia-1 (Mcl-1) inhibitors using fragment-based methods and structure-based design. J. Med. Chem. 56(1): 15-30 (2013). PMCID: PMC3646517
  • Harner M.J., Frank A.O., Fesik S.W. Fragment-Based Drug Discovery Using NMR Spectroscopy. J. Biomol. NMR. 56(2): 65-75 (2013). PMCID: PMC3699969
  • Patrone J.D., Kennedy J.P., Frank A.O., Feldkamp M.D., Vangamudi B., Pelz N.F., Rossanese O.W., Waterson A.G., Chazin W.J., Fesik S.W. Discovery of Protein-Protein Interaction Inhibitors of Replication Protein A. ACS Med. Chem. Lett. 4(7): 601–605 (2013). PMCID: PMC3728914
  • Li L., Wang R., Wilcox D., Sarthy A., Lin X., Huang X., Tian L., Dande P., Hubbard R.D., Hansen T.M., Wada C., Zhao X., Kohlbrenner W.M., Fesik S.W., Shen Y. Developing Lipid Nanoparticle-based siRNA Therapeutics for Hepatocellular Carcinoma Using an Integrated Approach. Mol Cancer Ther. 12(11):2308-18 (2013).
  • Feldkamp M.D., Frank A.O., Kennedy J.P., Patrone J., Vangamudi B., Waterson A.G., Fesik S.W., Chazin W.J. Surface reengineering of RPA70N enables co-crystallization with an inhibitor of the Replication Protein A interaction motif of ATR Interacting Protein. Biochemistry 52(37): 6515-24 (2013). PMCID: PMC3804075
  • Frank A. O., Feldkamp M.D., Kennedy J. P., Waterson A. G., Pelz N. F., Patrone J. D., Vangamudi B., Camper D.V., Rossanese O. W., Chazin W. J., Fesik S.W. Discovery of a Potent Inhibitor of Replication Protein A Protein-Protein Interactions Using a Fragment Linking Approach. J. Med. Chem.56(22):9242-50 (2013). PMCID: PMC3932990
  • Frank, A. O.; Vangamudi, B.; Feldkamp, M.; Souza-Fagundes, E.; Luzwick, J.; Cortez, D.; Olejniczak, E. T.; Waterson, A. G.; Rossanese, O. W.; Chazin, W.; Fesik, S. W. Discovery of a potent stapled helix peptide that binds to the 70N domain of Replication Protein A. J. Med. Chem. 57(6):2455-61 (2014). Epub 2014 Feb 19. PMCID: PMC3969094
  • Burns M.C., Sun Q., Daniels R.N., Camper D.V., Kennedy J. P., Phan, J., Olejniczak E. T., Lee T., Waterson A. G., Rossanese O. W., Fesik S.W. Approach for Targeting Ras with Small Molecules that Activate SOS-Mediated Nucleotide Exchange. Proceed. Natl. Acad. Sci. USA. 111(9):3401-6 (2014). PMCID: PMC3948241
  • Sun Q., Phan J., Friberg A.R., Camper D.V., Olejniczak E.T., Fesik S.W. A method for the second-site screening of K-Ras in the presence of a covalently attached first-site ligand. J. Biomol. NMR 60, 11-14 (2014). Epub 2014 Aug 3. PMCID: PMC4358732
  • Belmar J., Fesik S.W. Small molecule Mcl-1 inhibitors for the treatment of cancer. Pharmacol. Ther. 145C, 76-84 (2015).Epub 2014 Aug 27. PMCID: PMC4340597
    254.   Harner M.J., Chauder B.A., Phan J., Fesik S.W. Fragment-Based Screening of the Bromodomain of ATAD2. J. Med. Chem. 57(22):9687-92 (2014). Epub 2014 Nov 11. PMCID: PMC4255743
  • Cox A.D., Fesik S.W., Kimmelman A.C., Luo J., Der C.J. Drugging the undruggable Ras: Mission Possible? Nat. Rev. Drug Discov. 13(11):828-51 (2014). Epub 2014 Oct 17. PMCID: PMC4355017
  • Waterson A.G., Kennedy J.P., Patrone J.D., Pelz N.F., Feldkamp M.D., Frank A.O., Vangamudi B., Souza-Fagundes E.M., Rossanese O.W., Chazin W.J., Fesik S.W. Diphenylpyrazoles as replication protein A inhibitors. ACS Med Chem Lett. 6(2):140-5(2014). PMCID: PMC4329576
  • Thomas LR, Wang Q, Grieb BC, Phan J, Foshage AM, Sun Q, Olejniczak ET, Clark T, Dey S, Lorey S, Alicie B, Howard GC, Cawthon B, Ess KC, Eischen CM, Zhao Z, Fesik SW, Tansey WP. Interaction with WDR5 Promotes Target Gene Recognition and Tumorigenesis by MYC. Mol Cell. 58(3):440-52 (2015). PMCID: PMC4427524
  • Burke J.P., Bian Z., Shaw S., Zhao B., Goodwin C.M., Belmar J., Browning C.F., Vigil D., Friberg A., Camper D.V., Rossanese O.W., Lee T., Olejniczak E.T., FesikS.W. Discovery of tricyclic indoles that potently inhibit Mcl-1 using fragment-based methods and structure-based design. J. Med. Chem. 58(9):3794-805 (2015). PMCID: PMC5565203
  • Goodwin C.M., Rossanese O.W., Olejniczak E.T., FesikS.W. Myeloid cell leukemia-1 (Mcl-1) is an important apoptotic survival factor in Triple Negative Breast Cancer. Cell Death Differ. 22(12):2098-106 (2015). PMCID: PMC4816117
  • Wang F., Fesik S.W. “Chapter 16: Discovery of Inhibitors of Protein–Protein Interactions Using Fragment-Based Methods.” Fragment-based Drug Discovery: Lessons and Outlook. Ed. Daniel A. Erlanson; Ed. Wolfgang Jahnke. In Methods and Principles in Medicinal Chemistry. Vol. 67, pp. 371-390. Weinheim, Germany: Wiley-VCH, 2016. Print ISBN: 978-3-527-33775-0.
  • Patrone J.D., Pelz N.F., Bates B.S., Souza-Fagundes E.M., Vangamudi B., Camper D.V., Kuznetsov A.G., Browning C.F., Feldkamp M.D., Frank A.O., Gilston B.A., Olejniczak E.T., Rossanese O.W., Waterson A.G., Chazin W.J., Fesik S.W. Identification and Optimization of Anthranilic Acid Based Inhibitors of Replication Protein A. ChemMedChem. 11(8):893-9 (2016). PMCID: PMC4838552
  • Pelz N.F., Bian Z., Zhao B., Shaw S., Tarr J.C., Belmar J., Gregg C., Camper D.V., Goodwin C.M., Arnold A.L., Sensintaffar J.L., Friberg A., Rossanese O.W., Lee T., Olejniczak E.T., Fesik S.W. Discovery of 2-Indole-acylsulfonamide Myeloid Cell Leukemia 1 (Mcl-1) Inhibitors Using Fragment-Based Methods. J. Med. Chem. 59(5):2054-66 (2016). PMCID: PMC5565212
  • Erlanson D.A., Fesik S.W., Hubbard R.E., Jahnke W., Jhoti H. Twenty years on: the impact of fragments on drug discovery. Nat. Rev. Drug Discov. 15(9):605-19 (2016).
  • Lee T., Bian Z., Zhao B., Hogdal L.J., Sensintaffar J.L., Goodwin C.M., Belmar J., Shaw S., Tarr J.C., Veerasamy N., Matulis S.M., Koss B., Fischer M.A., Arnold A.L., Camper D.V., Browning C.F., Rossanese O.W., Budhraja A., Opferman J., Boise L.H., Savona M.R., Letai A., Olejniczak E.T., Fesik S.W. Discovery and Biological Characterization of Potent Myeloid Cell Leukemia-1 (Mcl-1) Inhibitors. FEBS Lett. 591(1):240-251 (2017). PMCID: PMC5381274
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