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Discovery of Potent Myeloid Cell Leukemia-1 (Mcl-1) Inhibitors That Demonstrate in Vivo Activity in Mouse Xenograft Models of Human Cancer.

Lee T, Christov PP, Shaw S, Tarr JC, Zhao B, Veerasamy N, Jeon KO, Mills JJ, Bian Z, Sensintaffar JL, Arnold AL, Fogarty SA, Perry E, Ramsey HE, Cook RS, Hollingshead M, Davis Millin M, Lee KM, Koss B, Budhraja A, Opferman JT, Kim K, Arteaga CL, Moore WJ, Olejniczak ET, Savona MR, Fesik SW.

J Med Chem. 2019 Apr 25;62(8):3971-3988. doi: 10.1021/acs.jmedchem.8b01991. Epub 2019 Apr 16.


Displacement of WDR5 from Chromatin by a WIN Site Inhibitor with Picomolar Affinity.

Aho ER, Wang J, Gogliotti RD, Howard GC, Phan J, Acharya P, Macdonald JD, Cheng K, Lorey SL, Lu B, Wenzel S, Foshage AM, Alvarado J, Wang F, Shaw JG, Zhao B, Weissmiller AM, Thomas LR, Vakoc CR, Hall MD, Hiebert SW, Liu Q, Stauffer SR, Fesik SW, Tansey WP.

Cell Rep. 2019 Mar 12;26(11):2916-2928.e13. doi: 10.1016/j.celrep.2019.02.047.


Small Molecule SOS1 Agonists Modulate MAPK and PI3K Signaling via Independent Cellular Responses.

Akan DT, Howes JE, Sai J, Arnold AL, Beesetty Y, Phan J, Olejniczak ET, Waterson AG, Fesik SW.

ACS Chem Biol. 2019 Mar 15;14(3):325-331. doi: 10.1021/acschembio.8b00869. Epub 2019 Feb 18.


Discovery of Quinazolines That Activate SOS1-Mediated Nucleotide Exchange on RAS.

Abbott JR, Patel PA, Howes JE, Akan DT, Kennedy JP, Burns MC, Browning CF, Sun Q, Rossanese OW, Phan J, Waterson AG, Fesik SW.

ACS Med Chem Lett. 2018 Aug 8;9(9):941-946. doi: 10.1021/acsmedchemlett.8b00296. eCollection 2018 Sep 13.


Discovery and Structure-Based Optimization of Benzimidazole-Derived Activators of SOS1-Mediated Nucleotide Exchange on RAS.

Hodges TR, Abbott JR, Little AJ, Sarkar D, Salovich JM, Howes JE, Akan DT, Sai J, Arnold AL, Browning C, Burns MC, Sobolik T, Sun Q, Beesetty Y, Coker JA, Scharn D, Stadtmueller H, Rossanese OW, Phan J, Waterson AG, McConnell DB, Fesik SW.

J Med Chem. 2018 Oct 11;61(19):8875-8894. doi: 10.1021/acs.jmedchem.8b01108. Epub 2018 Sep 28.


A Novel MCL1 Inhibitor Combined with Venetoclax Rescues Venetoclax-Resistant Acute Myelogenous Leukemia.

Ramsey HE, Fischer MA, Lee T, Gorska AE, Arrate MP, Fuller L, Boyd KL, Strickland SA, Sensintaffar J, Hogdal LJ, Ayers GD, Olejniczak ET, Fesik SW, Savona MR.

Cancer Discov. 2018 Dec;8(12):1566-1581. doi: 10.1158/2159-8290.CD-18-0140. Epub 2018 Sep 5.


Understanding the Species Selectivity of Myeloid Cell Leukemia-1 (Mcl-1) Inhibitors.

Zhao B, Arnold AL, Coronel MA, Lee JH, Lee T, Olejniczak ET, Fesik SW.

Biochemistry. 2018 Aug 14;57(32):4952-4958. doi: 10.1021/acs.biochem.8b00626. Epub 2018 Jul 31.


Discovery of Potent 2-Aryl-6,7-dihydro-5 H-pyrrolo[1,2- a]imidazoles as WDR5-WIN-Site Inhibitors Using Fragment-Based Methods and Structure-Based Design.

Wang F, Jeon KO, Salovich JM, Macdonald JD, Alvarado J, Gogliotti RD, Phan J, Olejniczak ET, Sun Q, Wang S, Camper D, Yuh JP, Shaw JG, Sai J, Rossanese OW, Tansey WP, Stauffer SR, Fesik SW.

J Med Chem. 2018 Jul 12;61(13):5623-5642. doi: 10.1021/acs.jmedchem.8b00375. Epub 2018 Jun 29.


Discovery of Aminopiperidine Indoles That Activate the Guanine Nucleotide Exchange Factor SOS1 and Modulate RAS Signaling.

Abbott JR, Hodges TR, Daniels RN, Patel PA, Kennedy JP, Howes JE, Akan DT, Burns MC, Sai J, Sobolik T, Beesetty Y, Lee T, Rossanese OW, Phan J, Waterson AG, Fesik SW.

J Med Chem. 2018 Jul 26;61(14):6002-6017. doi: 10.1021/acs.jmedchem.8b00360. Epub 2018 Jul 11.


High-throughput screening identifies small molecules that bind to the RAS:SOS:RAS complex and perturb RAS signaling.

Burns MC, Howes JE, Sun Q, Little AJ, Camper DV, Abbott JR, Phan J, Lee T, Waterson AG, Rossanese OW, Fesik SW.

Anal Biochem. 2018 May 1;548:44-52. doi: 10.1016/j.ab.2018.01.025. Epub 2018 Feb 11.


Small Molecule-Mediated Activation of RAS Elicits Biphasic Modulation of Phospho-ERK Levels that Are Regulated through Negative Feedback on SOS1.

Howes JE, Akan DT, Burns MC, Rossanese OW, Waterson AG, Fesik SW.

Mol Cancer Ther. 2018 May;17(5):1051-1060. doi: 10.1158/1535-7163.MCT-17-0666. Epub 2018 Feb 13.


Optimization of Potent and Selective Tricyclic Indole Diazepinone Myeloid Cell Leukemia-1 Inhibitors Using Structure-Based Design.

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.

J Med Chem. 2018 Mar 22;61(6):2410-2421. doi: 10.1021/acs.jmedchem.7b01155. Epub 2018 Mar 9.


MYC and MCL1 Cooperatively Promote Chemotherapy-Resistant Breast Cancer Stem Cells via Regulation of Mitochondrial Oxidative Phosphorylation.

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.

Cell Metab. 2017 Oct 3;26(4):633-647.e7. doi: 10.1016/j.cmet.2017.09.009.


Structure of a Myeloid cell leukemia-1 (Mcl-1) inhibitor bound to drug site 3 of Human Serum Albumin.

Zhao B, Sensintaffar J, Bian Z, Belmar J, Lee T, Olejniczak ET, Fesik SW.

Bioorg Med Chem. 2017 Jun 15;25(12):3087-3092. doi: 10.1016/j.bmc.2017.03.060. Epub 2017 Mar 29.


Discovery and biological characterization of potent myeloid cell leukemia-1 inhibitors.

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.

FEBS Lett. 2017 Jan;591(1):240-251. doi: 10.1002/1873-3468.12497. Epub 2016 Dec 19.


Recent advancements in the discovery of protein-protein interaction inhibitors of replication protein A.

Patrone JD, Waterson AG, Fesik SW.

Medchemcomm. 2016 Nov 4;8(2):259-267. doi: 10.1039/c6md00460a. eCollection 2017 Feb 1. Review.


Twenty years on: the impact of fragments on drug discovery.

Erlanson DA, Fesik SW, Hubbard RE, Jahnke W, Jhoti H.

Nat Rev Drug Discov. 2016 Sep;15(9):605-619. doi: 10.1038/nrd.2016.109. Epub 2016 Jul 15. Review.


Discovery of 2-Indole-acylsulfonamide Myeloid Cell Leukemia 1 (Mcl-1) Inhibitors Using Fragment-Based Methods.

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.

J Med Chem. 2016 Mar 10;59(5):2054-66. doi: 10.1021/acs.jmedchem.5b01660. Epub 2016 Feb 24.


Identification and Optimization of Anthranilic Acid Based Inhibitors of Replication Protein A.

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.

ChemMedChem. 2016 Apr 19;11(8):893-9. doi: 10.1002/cmdc.201500479. Epub 2016 Jan 8.


Myeloid cell leukemia-1 is an important apoptotic survival factor in triple-negative breast cancer.

Goodwin CM, Rossanese OW, Olejniczak ET, Fesik SW.

Cell Death Differ. 2015 Dec;22(12):2098-106. doi: 10.1038/cdd.2015.73. Epub 2015 Jun 5.


Discovery of tricyclic indoles that potently inhibit Mcl-1 using fragment-based methods and structure-based design.

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.

J Med Chem. 2015 May 14;58(9):3794-805. doi: 10.1021/jm501984f. Epub 2015 Apr 17.


Interaction with WDR5 promotes target gene recognition and tumorigenesis by MYC.

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.

Mol Cell. 2015 May 7;58(3):440-52. doi: 10.1016/j.molcel.2015.02.028. Epub 2015 Mar 26.


Diphenylpyrazoles as replication protein a inhibitors.

Waterson AG, Kennedy JP, Patrone JD, Pelz NF, Feldkamp MD, Frank AO, Vangamudi B, Souza-Fagundes EM, Rossanese OW, Chazin WJ, Fesik SW.

ACS Med Chem Lett. 2014 Nov 11;6(2):140-5. doi: 10.1021/ml5003629. eCollection 2015 Feb 12.


Drugging the undruggable RAS: Mission possible?

Cox AD, Fesik SW, Kimmelman AC, Luo J, Der CJ.

Nat Rev Drug Discov. 2014 Nov;13(11):828-51. doi: 10.1038/nrd4389. Epub 2014 Oct 17. Review.


Fragment-based screening of the bromodomain of ATAD2.

Harner MJ, Chauder BA, Phan J, Fesik SW.

J Med Chem. 2014 Nov 26;57(22):9687-92. doi: 10.1021/jm501035j. Epub 2014 Nov 11.


Small molecule Mcl-1 inhibitors for the treatment of cancer.

Belmar J, Fesik SW.

Pharmacol Ther. 2015 Jan;145:76-84. doi: 10.1016/j.pharmthera.2014.08.003. Epub 2014 Aug 27. Review.


A method for the second-site screening of K-Ras in the presence of a covalently attached first-site ligand.

Sun Q, Phan J, Friberg AR, Camper DV, Olejniczak ET, Fesik SW.

J Biomol NMR. 2014 Sep;60(1):11-4. doi: 10.1007/s10858-014-9849-8. Epub 2014 Aug 3.


Approach for targeting Ras with small molecules that activate SOS-mediated nucleotide exchange.

Burns MC, Sun Q, Daniels RN, Camper D, Kennedy JP, Phan J, Olejniczak ET, Lee T, Waterson AG, Rossanese OW, Fesik SW.

Proc Natl Acad Sci U S A. 2014 Mar 4;111(9):3401-6. doi: 10.1073/pnas.1315798111. Epub 2014 Feb 18.


Discovery of a potent stapled helix peptide that binds to the 70N domain of replication protein A.

Frank AO, Vangamudi B, Feldkamp MD, Souza-Fagundes EM, Luzwick JW, Cortez D, Olejniczak ET, Waterson AG, Rossanese OW, Chazin WJ, Fesik SW.

J Med Chem. 2014 Mar 27;57(6):2455-61. doi: 10.1021/jm401730y. Epub 2014 Feb 19.


Discovery of a potent inhibitor of replication protein a protein-protein interactions using a fragment-linking approach.

Frank AO, Feldkamp MD, Kennedy JP, Waterson AG, Pelz NF, Patrone JD, Vangamudi B, Camper DV, Rossanese OW, Chazin WJ, Fesik SW.

J Med Chem. 2013 Nov 27;56(22):9242-50. doi: 10.1021/jm401333u. Epub 2013 Nov 11.


Surface reengineering of RPA70N enables cocrystallization with an inhibitor of the replication protein A interaction motif of ATR interacting protein.

Feldkamp MD, Frank AO, Kennedy JP, Patrone JD, Vangamudi B, Waterson AG, Fesik SW, Chazin WJ.

Biochemistry. 2013 Sep 17;52(37):6515-24. doi: 10.1021/bi400542z. Epub 2013 Sep 6.


Developing lipid nanoparticle-based siRNA therapeutics for hepatocellular carcinoma using an integrated approach.

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.

Mol Cancer Ther. 2013 Nov;12(11):2308-18. doi: 10.1158/1535-7163.MCT-12-0983-T. Epub 2013 Aug 13.


Discovery of Protein-Protein Interaction Inhibitors of Replication Protein A.

Patrone JD, Kennedy JP, Frank AO, Feldkamp MD, Vangamudi B, Pelz NF, Rossanese OW, Waterson AG, Chazin WJ, Fesik SW.

ACS Med Chem Lett. 2013 Jul 11;4(7):601-605.


Fragment-based drug discovery using NMR spectroscopy.

Harner MJ, Frank AO, Fesik SW.

J Biomol NMR. 2013 Jun;56(2):65-75. doi: 10.1007/s10858-013-9740-z. Epub 2013 May 18. Review.


Discovery of potent myeloid cell leukemia 1 (Mcl-1) inhibitors using fragment-based methods and structure-based design.

Friberg A, Vigil D, Zhao B, Daniels RN, Burke JP, Garcia-Barrantes PM, Camper D, Chauder BA, Lee T, Olejniczak ET, Fesik SW.

J Med Chem. 2013 Jan 10;56(1):15-30. doi: 10.1021/jm301448p. Epub 2012 Dec 17.


Discovery of small molecules that bind to K-Ras and inhibit Sos-mediated activation.

Sun Q, Burke JP, Phan J, Burns MC, Olejniczak ET, Waterson AG, Lee T, Rossanese OW, Fesik SW.

Angew Chem Int Ed Engl. 2012 Jun 18;51(25):6140-3. doi: 10.1002/anie.201201358. Epub 2012 May 8. No abstract available.


A high-throughput fluorescence polarization anisotropy assay for the 70N domain of replication protein A.

Souza-Fagundes EM, Frank AO, Feldkamp MD, Dorset DC, Chazin WJ, Rossanese OW, Olejniczak ET, Fesik SW.

Anal Biochem. 2012 Feb 15;421(2):742-9. doi: 10.1016/j.ab.2011.11.025. Epub 2011 Dec 1.


Tumor vasculature is a key determinant for the efficiency of nanoparticle-mediated siRNA delivery.

Li L, Wang R, Wilcox D, Zhao X, Song J, Lin X, Kohlbrenner WM, Fesik SW, Shen Y.

Gene Ther. 2012 Jul;19(7):775-80. doi: 10.1038/gt.2011.146. Epub 2011 Sep 29.


A robust in vivo positive-readout system for monitoring siRNA delivery to xenograft tumors.

Lin X, Li L, Wang R, Wilcox D, Zhao X, Song J, Huang X, Hansen TM, Dande P, Wada C, Hubbard RD, Kohlbrenner WM, Fesik SW, Shen Y.

RNA. 2011 Apr;17(4):603-12. doi: 10.1261/rna.2546011. Epub 2011 Feb 14.


Discovery of a potent and selective Bcl-2 inhibitor using SAR by NMR.

Petros AM, Huth JR, Oost T, Park CM, Ding H, Wang X, Zhang H, Nimmer P, Mendoza R, Sun C, Mack J, Walter K, Dorwin S, Gramling E, Ladror U, Rosenberg SH, Elmore SW, Fesik SW, Hajduk PJ.

Bioorg Med Chem Lett. 2010 Nov 15;20(22):6587-91. doi: 10.1016/j.bmcl.2010.09.033. Epub 2010 Sep 15.


Bcl-XL represents a druggable molecular vulnerability during aurora B inhibitor-mediated polyploidization.

Shah OJ, Lin X, Li L, Huang X, Li J, Anderson MG, Tang H, Rodriguez LE, Warder SE, McLoughlin S, Chen J, Palma J, Glaser KB, Donawho CK, Fesik SW, Shen Y.

Proc Natl Acad Sci U S A. 2010 Jul 13;107(28):12634-9. doi: 10.1073/pnas.0913615107. Epub 2010 Jun 28.


The Bcl-2 inhibitor ABT-263 enhances the response of multiple chemotherapeutic regimens in hematologic tumors in vivo.

Ackler S, Mitten MJ, Foster K, Oleksijew A, Refici M, Tahir SK, Xiao Y, Tse C, Frost DJ, Fesik SW, Rosenberg SH, Elmore SW, Shoemaker AR.

Cancer Chemother Pharmacol. 2010 Oct;66(5):869-80. doi: 10.1007/s00280-009-1232-1. Epub 2010 Jan 23.


ABT-263 and rapamycin act cooperatively to kill lymphoma cells in vitro and in vivo.

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.

Mol Cancer Ther. 2008 Oct;7(10):3265-74. doi: 10.1158/1535-7163.MCT-08-0268.


Discovery of an orally bioavailable small molecule inhibitor of prosurvival B-cell lymphoma 2 proteins.

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.

J Med Chem. 2008 Nov 13;51(21):6902-15. doi: 10.1021/jm800669s. Epub 2008 Oct 8.


Growth inhibition and radiosensitization of glioblastoma and lung cancer cells by small interfering RNA silencing of tumor necrosis factor receptor-associated factor 2.

Zheng M, Morgan-Lappe SE, Yang J, Bockbrader KM, Pamarthy D, Thomas D, Fesik SW, Sun Y.

Cancer Res. 2008 Sep 15;68(18):7570-8. doi: 10.1158/0008-5472.CAN-08-0632.


Activity of the Bcl-2 family inhibitor ABT-263 in a panel of small cell lung cancer xenograft models.

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.

Clin Cancer Res. 2008 Jun 1;14(11):3268-77. doi: 10.1158/1078-0432.CCR-07-4622.


A chemical genomics screen highlights the essential role of mitochondria in HIF-1 regulation.

Lin X, David CA, Donnelly JB, Michaelides M, Chandel NS, Huang X, Warrior U, Weinberg F, Tormos KV, Fesik SW, Shen Y.

Proc Natl Acad Sci U S A. 2008 Jan 8;105(1):174-9. doi: 10.1073/pnas.0706585104. Epub 2008 Jan 2.


Defining the optimal parameters for hairpin-based knockdown constructs.

Li L, Lin X, Khvorova A, Fesik SW, Shen Y.

RNA. 2007 Oct;13(10):1765-74. Epub 2007 Aug 13.


Discovery and design of novel HSP90 inhibitors using multiple fragment-based design strategies.

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.

Chem Biol Drug Des. 2007 Jul;70(1):1-12.


From bacterial genomes to novel antibacterial agents: discovery, characterization, and antibacterial activity of compounds that bind to HI0065 (YjeE) from Haemophilus influenzae.

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.

Chem Biol Drug Des. 2007 Jun;69(6):395-404.


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