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Page 1
Discovery of a highly potent, selective, orally bioavailable inhibitor of KAT6A/B histone acetyltransferases with efficacy against KAT6A-high ER+ breast cancer.
Sharma S, Chung CY, Uryu S, Petrovic J, Cao J, Rickard A, Nady N, Greasley S, Johnson E, Brodsky O, Khan S, Wang H, Wang Z, Zhang Y, Tsaparikos K, Chen L, Mazurek A, Lapek J, Kung PP, Sutton S, Richardson PF, Greenwald EC, Yamazaki S, Jones R, Maegley KA, Bingham P, Lam H, Stupple AE, Kamal A, Chueh A, Cuzzupe A, Morrow BJ, Ren B, Carrasco-Pozo C, Tan CW, Bhuva DD, Allan E, Surgenor E, Vaillant F, Pehlivanoglu H, Falk H, Whittle JR, Newman J, Cursons J, Doherty JP, White KL, MacPherson L, Devlin M, Dennis ML, Hattarki MK, De Silva M, Camerino MA, Butler MS, Dolezal O, Pilling P, Foitzik R, Stupple PA, Lagiakos HR, Walker SR, Hediyeh-Zadeh S, Nuttall S, Spall SK, Charman SA, Connor T, Peat TS, Avery VM, Bozikis YE, Yang Y, Zhang M, Monahan BJ, Voss AK, Thomas T, Street IP, Dawson SJ, Dawson MA, Lindeman GJ, Davis MJ, Visvader JE, Paul TA. Sharma S, et al. Among authors: paul ta. Cell Chem Biol. 2023 Oct 19;30(10):1191-1210.e20. doi: 10.1016/j.chembiol.2023.07.005. Epub 2023 Aug 8. Cell Chem Biol. 2023. PMID: 37557181 Free article.
Characterization of Specific N-α-Acetyltransferase 50 (Naa50) Inhibitors Identified Using a DNA Encoded Library.
Kung PP, Bingham P, Burke BJ, Chen Q, Cheng X, Deng YL, Dou D, Feng J, Gallego GM, Gehring MR, Grant SK, Greasley S, Harris AR, Maegley KA, Meier J, Meng X, Montano JL, Morgan BA, Naughton BS, Palde PB, Paul TA, Richardson P, Sakata S, Shaginian A, Sonnenburg WK, Subramanyam C, Timofeevski S, Wan J, Yan W, Stewart AE. Kung PP, et al. Among authors: paul ta. ACS Med Chem Lett. 2020 Apr 10;11(6):1175-1184. doi: 10.1021/acsmedchemlett.0c00029. eCollection 2020 Jun 11. ACS Med Chem Lett. 2020. PMID: 32550998 Free PMC article.
SAM-Competitive PRMT5 Inhibitor PF-06939999 Demonstrates Antitumor Activity in Splicing Dysregulated NSCLC with Decreased Liability of Drug Resistance.
Jensen-Pergakes K, Tatlock J, Maegley KA, McAlpine IJ, McTigue M, Xie T, Dillon CP, Wang Y, Yamazaki S, Spiegel N, Shi M, Nemeth A, Miller N, Hendrickson E, Lam H, Sherrill J, Chung CY, McMillan EA, Bryant SK, Palde P, Braganza J, Brooun A, Deng YL, Goshtasbi V, Kephart SE, Kumpf RA, Liu W, Patman RL, Rui E, Scales S, Tran-Dube M, Wang F, Wythes M, Paul TA. Jensen-Pergakes K, et al. Among authors: paul ta. Mol Cancer Ther. 2022 Jan;21(1):3-15. doi: 10.1158/1535-7163.MCT-21-0620. Epub 2021 Nov 4. Mol Cancer Ther. 2022. PMID: 34737197
The SMARCA2/4 ATPase Domain Surpasses the Bromodomain as a Drug Target in SWI/SNF-Mutant Cancers: Insights from cDNA Rescue and PFI-3 Inhibitor Studies.
Vangamudi B, Paul TA, Shah PK, Kost-Alimova M, Nottebaum L, Shi X, Zhan Y, Leo E, Mahadeshwar HS, Protopopov A, Futreal A, Tieu TN, Peoples M, Heffernan TP, Marszalek JR, Toniatti C, Petrocchi A, Verhelle D, Owen DR, Draetta G, Jones P, Palmer WS, Sharma S, Andersen JN. Vangamudi B, et al. Among authors: paul ta. Cancer Res. 2015 Sep 15;75(18):3865-3878. doi: 10.1158/0008-5472.CAN-14-3798. Epub 2015 Jul 2. Cancer Res. 2015. PMID: 26139243 Free PMC article.
Chemical Proteomics Identifies Druggable Vulnerabilities in a Genetically Defined Cancer.
Bar-Peled L, Kemper EK, Suciu RM, Vinogradova EV, Backus KM, Horning BD, Paul TA, Ichu TA, Svensson RU, Olucha J, Chang MW, Kok BP, Zhu Z, Ihle NT, Dix MM, Jiang P, Hayward MM, Saez E, Shaw RJ, Cravatt BF. Bar-Peled L, et al. Among authors: paul ta. Cell. 2017 Oct 19;171(3):696-709.e23. doi: 10.1016/j.cell.2017.08.051. Epub 2017 Sep 28. Cell. 2017. PMID: 28965760 Free PMC article.
Use of the dTAG system in vivo to degrade CDK2 and CDK5 in adult mice and explore potential safety liabilities.
Yenerall P, Sung T, Palyada K, Qian J, Arat S, Kumpf SW, Wang SW, Biddle K, Esparza C, Chang S, Scott W, Collette W, Winrow TS, Affolter T, Shirai N, Thibault S, Wang J, Liu L, Bauchmann M, Frey J, Steyn S, Sacaan A, Vitsky A, Ahn Y, Paul T, Lum L, Oyer J, Yang A, Hu W. Yenerall P, et al. Toxicol Sci. 2023 Jun 28;194(1):53-69. doi: 10.1093/toxsci/kfad049. Toxicol Sci. 2023. PMID: 37228089 Free PMC article.
28 results