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Fesik Lab

Fesik Lab Publications

2018

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
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;
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

2017

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
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
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

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
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
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;

2015

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
Belmar J , Fesik SW , Small molecule Mcl-1 inhibitors for the treatment of cancer. Pharmacology & therapeutics. 2015 Jan ; 145 76-84

2014

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
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
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
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

2013

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
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
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
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
Harner MJ , Frank AO , Fesik SW , Fragment-based drug discovery using NMR spectroscopy. Journal of biomolecular NMR. 2013 Jun ; 56 (2). 65-75
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 , Zuiderweg ERP , Heteronuclear three-dimensional NMR spectroscopy. A strategy for the simplification of homonuclear two-dimensional NMR spectra Journal of Magnetic Resonance . 1988 Jul ; 78 (3). 588-593
Fesik SW , Isotope-edited NMR spectroscopy Nature. 1988 Apr 28; (332). 865-866