Publications

2018

Shaw S, Bian Z, Zhao B, Tarr JC, Veerasamy N, Jeon KO, Belmar J, Arnold AL, Fogarty SA, Perry E, Sensintaffar JL, Camper DV, Rossanese OW, Lee T, Olejniczak ET, Fesik SW, Optimization of Potent and Selective Tricyclic Indole Diazepinone Myeloid Cell Leukemia-1 Inhibitors… Journal of medicinal chemistry. 2018 Mar 22; 61 (6) 2410-2421
Howes JE, Akan DT, Burns MC, Rossanese OW, Waterson AG, Fesik SW, Small molecule-mediated activation of RAS elicits biphasic modulation of phospho ERK levels that are… Molecular cancer therapeutics. 2018 Feb 13;
Burns MC, Howes JE, Sun Q, Little AJ, Camper DV, Abbott JR, Phan J, Lee T, Waterson AG, Rossanese OW, Fesik SW, High-throughput screening identifies small molecules that bind to the RAS:SOS:RAS complex and pertur… Analytical biochemistry. 2018 Feb 11; 548 44-52

2017

Zhao B, Sensintaffar J, Bian Z, Belmar J, Lee T, Olejniczak ET, Fesik SW, Structure of a Myeloid cell leukemia-1 (Mcl-1) inhibitor bound to drug site 3 of Human Serum Albumin… Bioorganic & medicinal chemistry. 2017 Dec 15; 25 (12) 3087-3092
Lee KM, Giltnane JM, Balko JM, Schwarz LJ, Guerrero-Zotano AL, Hutchinson KE, Nixon MJ, Estrada MV, Sánchez V, Sanders ME, Lee T, Gómez H, Lluch A, Pérez-Fidalgo JA, Wolf MM, Andrejeva G, Rathmell JC, Fesik SW, Arteaga CL, MYC and MCL1 Cooperatively Promote Chemotherapy-Resistant Breast Cancer Stem Cells via Regulation of… Cell metabolism. 2017 Oct 3; 26 (4) 633-647.e7
Lee T, Bian Z, Zhao B, Hogdal LJ, Sensintaffar JL, Goodwin CM, Belmar J, Shaw S, Tarr JC, Veerasamy N, Matulis SM, Koss B, Fischer MA, Arnold AL, Camper DV, Browning CF, Rossanese OW, Budhraja A, Opferman J, Boise LH, Savona MR, Letai A, Olejniczak ET, Fesik SW, Discovery and biological characterization of potent myeloid cell leukemia-1 inhibitors. FEBS letters. 2017 Jan 591 (1) 240-251

2016

Erlanson DA, Fesik SW, Hubbard RE, Jahnke W, Jhoti H, Twenty years on: the impact of fragments on drug discovery. Nature reviews. Drug discovery. 2016 Dec 15 (9) 605-19
Patrone JD, Pelz NF, Bates BS, Souza-Fagundes EM, Vangamudi B, Camper DV, Kuznetsov AG, Browning CF, Feldkamp MD, Frank AO, Gilston BA, Olejniczak ET, Rossanese OW, Waterson AG, Chazin WJ, Fesik SW, Identification and Optimization of Anthranilic Acid Based Inhibitors of Replication Protein A. ChemMedChem. 2016 Jan 8;
Pelz NF, Bian Z, Zhao B, Shaw S, Tarr JC, Belmar J, Gregg C, Camper DV, Goodwin CM, Arnold AL, Sensintaffar JL, Friberg A, Rossanese OW, Lee T, Olejniczak ET, Fesik SW, Discovery of 2-Indole-acylsulfonamide Myeloid Cell Leukemia 1 (Mcl-1) Inhibitors Using Fragment-Base… Journal of medicinal chemistry. 2016 Mar 10; 59 (5) 2054-66

2015

Belmar J, Fesik SW, Small molecule Mcl-1 inhibitors for the treatment of cancer. Pharmacology & therapeutics. 2015 Jan 145 76-84
Goodwin CM, Rossanese OW, Olejniczak ET, Fesik SW, Myeloid cell leukemia-1 is an important apoptotic survival factor in triple-negative breast cancer. Cell death and differentiation. 2015 Dec 22 (12) 2098-106
Burke JP, Bian Z, Shaw S, Zhao B, Goodwin CM, Belmar J, Browning CF, Vigil D, Friberg A, Camper DV, Rossanese OW, Lee T, Olejniczak ET, Fesik SW, Discovery of tricyclic indoles that potently inhibit Mcl-1 using fragment-based methods and structur… Journal of medicinal chemistry. 2015 May 14; 58 (9) 3794-805
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. Molecular cell. 2015 May 7; 58 (3) 440-52
Waterson AG, Kennedy JP, Patrone JD, Pelz NF, Feldkamp MD, Frank AO, Vangamudi B, Souza-Fagundes EM, Rossanese OW, Chazin WJ, Fesik SW, Diphenylpyrazoles as replication protein a inhibitors. ACS medicinal chemistry letters. 2015 Feb 12; 6 (2) 140-5

2014

Sun Q, Phan J, Friberg AR, Camper DV, Olejniczak ET, Fesik SW, A method for the second-site screening of K-Ras in the presence of a covalently attached first-site … Journal of biomolecular NMR. 2014 Sep 60 (1) 11-4
Cox AD, Fesik SW, Kimmelman AC, Luo J, Der CJ, Drugging the undruggable RAS: Mission possible? Nature reviews. Drug discovery. 2014 Nov 13 (11) 828-51
Harner MJ, Chauder BA, Phan J, Fesik SW, Fragment-based screening of the bromodomain of ATAD2. Journal of medicinal chemistry. 2014 Nov 26; 57 (22) 9687-92
Frank AO, Vangamudi B, Feldkamp MD, Souza-Fagundes EM, Luzwick JW, Cortez D, Olejniczak ET, Waterson AG, Rossanese OW, Chazin WJ, Fesik SW, Discovery of a potent stapled helix peptide that binds to the 70N domain of replication protein A. Journal of medicinal chemistry. 2014 Mar 27; 57 (6) 2455-61
Burns MC, Sun Q, Daniels RN, Camper D, Kennedy JP, Phan J, Olejniczak ET, Lee T, Waterson AG, Rossanese OW, Fesik SW, Approach for targeting Ras with small molecules that activate SOS-mediated nucleotide exchange. Proceedings of the National Academy of Sciences of the United States of America. 2014 Mar 4; 111 (9) 3401-6

2013

Harner MJ, Frank AO, Fesik SW, Fragment-based drug discovery using NMR spectroscopy. Journal of biomolecular NMR. 2013 Jun 56 (2) 65-75
Patrone JD, Kennedy JP, Frank AO, Feldkamp MD, Vangamudi B, Pelz NF, Rossanese OW, Waterson AG, Chazin WJ, Fesik SW, Discovery of Protein-Protein Interaction Inhibitors of Replication Protein A. ACS medicinal chemistry letters. 2013 Jul 11; 4 (7) 601-605
Li L, Wang R, Wilcox D, Sarthy A, Lin X, Huang X, Tian L, Dande P, Hubbard RD, Hansen TM, Wada C, Zhao X, Kohlbrenner WM, Fesik SW, Shen Y, Developing lipid nanoparticle-based siRNA therapeutics for hepatocellular carcinoma using an integra… Molecular cancer therapeutics. 2013 Nov 12 (11) 2308-18
Feldkamp MD, Frank AO, Kennedy JP, Patrone JD, Vangamudi B, Waterson AG, Fesik SW, Chazin WJ, Surface reengineering of RPA70N enables cocrystallization with an inhibitor of the replication prote… Biochemistry. 2013 Sep 17; 52 (37) 6515-24
Frank AO, Feldkamp MD, Kennedy JP, Waterson AG, Pelz NF, Patrone JD, Vangamudi B, Camper DV, Rossanese OW, Chazin WJ, Fesik SW, Discovery of a potent inhibitor of replication protein a protein-protein interactions using a fragme… Journal of medicinal chemistry. 2013 Nov 27; 56 (22) 9242-50
Friberg A, Vigil D, Zhao B, Daniels RN, Burke JP, Garcia-Barrantes PM, Camper D, Chauder BA, Lee T, Olejniczak ET, Fesik SW, Discovery of potent myeloid cell leukemia 1 (Mcl-1) inhibitors using fragment-based methods and stru… Journal of medicinal chemistry. 2013 Jan 10; 56 (1) 15-30

2012

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. Angewandte Chemie (International ed. in English). 2012 Jun 18; 51 (25) 6140-3
Souza-Fagundes EM, Frank AO, Feldkamp MD, Dorset DC, Chazin WJ, Rossanese OW, Olejniczak ET, Fesik SW, A high-throughput fluorescence polarization anisotropy assay for the 70N domain of replication prote… Analytical biochemistry. 2012 Feb 15; 421 (2) 742-9

1997

Olejniczak ET, Hajduk PJ, Marcotte PA, Nettesheim D, Meadows RP, Edalji R, Holzman TF, Fesik SW, Stromelysin inhibitors designed from weakly bound fragments: Effects of linking and cooperativity Journal of the American Chemical Society. 1997 Jun 25; 25 (119) 5828-5832
Hadjuk PJ, Sheppard G, Nettesheim D, Olejniczak ET, Shuker SB, Meadows RP, Steinman DH, Carrera GM, Marcotte PA, Severin J, Walter K, Smith H, Gubbins E, Simmer R, Holzman TF, Morgan DW, Davidsen SK, Summers JB, Fesik SW, Discovery of potent nonpeptide inhibitors of stromelysin using SAR by NMR Journal of the American Chemical Society. 1997 Jun 25; 25 (119) 5818-5827
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. 1997 Feb 14; 275 (5302) 983-986
Minn AJ, Velez 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. 1997 Jan 23; 385 (6614) 353-357

1996

Huang B, Eberstadt M, Olejniczak ET, Meadows RP, Fesik SW, NMR structure and mutagenesis of the Fas (APO-1/CD95) death domain Nature. 1996 Dec 19; 384 (6610) 638-641
Shuker SB, Hadjuk PJ, Meadows RP, Fesik SW, Discovering high-affinity ligands for proteins: SAR by NMR Science. 1996 Nov 29; 274 (5292) 1531-1534
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. 1996 May 23; 381 (6580) 335-341

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. 1995 Dec 7; 378 (6557) 584-592

1994

Harlan JE, Hajduk PJ, Yoon HS, Fesik SW, Pleckstrin homology domains bind to phosphatidylinositol 4,5-bisphosphate Nature. 1994 Sep 8; 271 (6493) 168-170
Yoon HS, Hajduk PJ, Petros AM, Olejniczak ET, Meadows RP, Fesik SW, Solution structure of a pleckstrin homology domain Nature. 1994 Jun 23; (369) 672–675

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. 1993 Jan 7; 361 (6407) 88-91

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. 1990 Dec 7; 250 (4986) 1406-1409
Fesik SW, Eaton HL, Olejniczak ET, Zuiderweg ERP, McIntosh LP, Dahlquist FW, 2D and 3D NMR Spectroscopy employing 13C-13C magnetization transfer by isotropic mixing. Spin system identification in large proteins Journal of the American Chemical Society. 1990 Jan 1; 112 (2) 886-888

1988

Fesik SW, Isotope-edited NMR spectroscopy Nature. 1988 Apr 28; (332) 865-866