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Page 1
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. Pelz NF, et al. Among authors: sensintaffar jl. J Med Chem. 2016 Mar 10;59(5):2054-66. doi: 10.1021/acs.jmedchem.5b01660. Epub 2016 Feb 24. J Med Chem. 2016. PMID: 26878343 Free PMC article.
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. Lee T, et al. Among authors: sensintaffar jl. FEBS Lett. 2017 Jan;591(1):240-251. doi: 10.1002/1873-3468.12497. Epub 2016 Dec 19. FEBS Lett. 2017. PMID: 27878989 Free PMC article.
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. Shaw S, et al. Among authors: sensintaffar jl. J Med Chem. 2018 Mar 22;61(6):2410-2421. doi: 10.1021/acs.jmedchem.7b01155. Epub 2018 Mar 9. J Med Chem. 2018. PMID: 29323899
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. Lee T, et al. Among authors: sensintaffar jl. J Med Chem. 2019 Apr 25;62(8):3971-3988. doi: 10.1021/acs.jmedchem.8b01991. Epub 2019 Apr 16. J Med Chem. 2019. PMID: 30929420
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. Ramsey HE, et al. Among authors: sensintaffar j. Cancer Discov. 2018 Dec;8(12):1566-1581. doi: 10.1158/2159-8290.CD-18-0140. Epub 2018 Sep 5. Cancer Discov. 2018. PMID: 30185627 Free PMC article.
Discovery and Structure-Based Optimization of Potent and Selective WD Repeat Domain 5 (WDR5) Inhibitors Containing a Dihydroisoquinolinone Bicyclic Core.
Tian J, Teuscher KB, Aho ER, Alvarado JR, Mills JJ, Meyers KM, Gogliotti RD, Han C, Macdonald JD, Sai J, Shaw JG, Sensintaffar JL, Zhao B, Rietz TA, Thomas LR, Payne WG, Moore WJ, Stott GM, Kondo J, Inoue M, Coffey RJ, Tansey WP, Stauffer SR, Lee T, Fesik SW. Tian J, et al. Among authors: sensintaffar jl. J Med Chem. 2020 Jan 23;63(2):656-675. doi: 10.1021/acs.jmedchem.9b01608. Epub 2020 Jan 7. J Med Chem. 2020. PMID: 31858797 Free PMC article.
Selective estrogen receptor degraders with novel structural motifs induce regression in a tamoxifen-resistant breast cancer xenograft.
Govek SP, Bonnefous C, Julien JD, Nagasawa JY, Kahraman M, Lai AG, Douglas KL, Aparicio AM, Darimont BD, Grillot KL, Joseph JD, Kaufman JA, Lee KJ, Lu N, Moon MJ, Prudente RY, Sensintaffar J, Rix PJ, Hager JH, Smith ND. Govek SP, et al. Among authors: sensintaffar j. Bioorg Med Chem Lett. 2019 Feb 1;29(3):367-372. doi: 10.1016/j.bmcl.2018.12.042. Epub 2018 Dec 19. Bioorg Med Chem Lett. 2019. PMID: 30587451
7'-substituted benzothiazolothio- and pyridinothiazolothio-purines as potent heat shock protein 90 inhibitors.
Zhang L, Fan J, Vu K, Hong K, Le Brazidec JY, Shi J, Biamonte M, Busch DJ, Lough RE, Grecko R, Ran Y, Sensintaffar JL, Kamal A, Lundgren K, Burrows FJ, Mansfield R, Timony GA, Ulm EH, Kasibhatla SR, Boehm MF. Zhang L, et al. Among authors: sensintaffar jl. J Med Chem. 2006 Aug 24;49(17):5352-62. doi: 10.1021/jm051146h. J Med Chem. 2006. PMID: 16913725
Optimization of an indazole series of selective estrogen receptor degraders: Tumor regression in a tamoxifen-resistant breast cancer xenograft.
Govek SP, Nagasawa JY, Douglas KL, Lai AG, Kahraman M, Bonnefous C, Aparicio AM, Darimont BD, Grillot KL, Joseph JD, Kaufman JA, Lee KJ, Lu N, Moon MJ, Prudente RY, Sensintaffar J, Rix PJ, Hager JH, Smith ND. Govek SP, et al. Among authors: sensintaffar j. Bioorg Med Chem Lett. 2015 Nov 15;25(22):5163-7. doi: 10.1016/j.bmcl.2015.09.074. Epub 2015 Oct 3. Bioorg Med Chem Lett. 2015. PMID: 26463130
30 results