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Page 1
Discovery of Selective Estrogen Receptor Covalent Antagonists for the Treatment of ERαWT and ERαMUT Breast Cancer.
Puyang X, Furman C, Zheng GZ, Wu ZJ, Banka D, Aithal K, Agoulnik S, Bolduc DM, Buonamici S, Caleb B, Das S, Eckley S, Fekkes P, Hao MH, Hart A, Houtman R, Irwin S, Joshi JJ, Karr C, Kim A, Kumar N, Kumar P, Kuznetsov G, Lai WG, Larsen N, Mackenzie C, Martin LA, Melchers D, Moriarty A, Nguyen TV, Norris J, O'Shea M, Pancholi S, Prajapati S, Rajagopalan S, Reynolds DJ, Rimkunas V, Rioux N, Ribas R, Siu A, Sivakumar S, Subramanian V, Thomas M, Vaillancourt FH, Wang J, Wardell S, Wick MJ, Yao S, Yu L, Warmuth M, Smith PG, Zhu P, Korpal M. Puyang X, et al. Cancer Discov. 2018 Sep;8(9):1176-1193. doi: 10.1158/2159-8290.CD-17-1229. Epub 2018 Jul 10. Cancer Discov. 2018. PMID: 29991605
Covalent ERα Antagonist H3B-6545 Demonstrates Encouraging Preclinical Activity in Therapy-Resistant Breast Cancer.
Furman C, Puyang X, Zhang Z, Wu ZJ, Banka D, Aithal KB, Albacker LA, Hao MH, Irwin S, Kim A, Montesion M, Moriarty AD, Murugesan K, Nguyen TV, Rimkunas V, Sahmoud T, Wick MJ, Yao S, Zhang X, Zeng H, Vaillancourt FH, Bolduc DM, Larsen N, Zheng GZ, Prajapati S, Zhu P, Korpal M. Furman C, et al. Among authors: aithal kb. Mol Cancer Ther. 2022 Jun 1;21(6):890-902. doi: 10.1158/1535-7163.MCT-21-0378. Mol Cancer Ther. 2022. PMID: 35642432 Free PMC article.
Discovery of MAP855, an Efficacious and Selective MEK1/2 Inhibitor with an ATP-Competitive Mode of Action.
Poddutoori R, Aardalen K, Aithal K, Barahagar SS, Belliappa C, Bock M, Chelur S, Gerken A, Gopinath S, Gruenenfelder B, Kiffe M, Krishnaswami M, Langowski J, Madapa S, Narayanan K, Pandit C, Panigrahi SK, Perrone M, Potakamuri RK, Ramachandra M, Ramanathan A, Ramos R, Sager E, Samajdar S, Subramanya HS, Thimmasandra DS, Venetsanakos E, Möbitz H. Poddutoori R, et al. J Med Chem. 2022 Mar 10;65(5):4350-4366. doi: 10.1021/acs.jmedchem.1c02192. Epub 2022 Feb 23. J Med Chem. 2022. PMID: 35195996
Targeting SWI/SNF ATPases in enhancer-addicted prostate cancer.
Xiao L, Parolia A, Qiao Y, Bawa P, Eyunni S, Mannan R, Carson SE, Chang Y, Wang X, Zhang Y, Vo JN, Kregel S, Simko SA, Delekta AD, Jaber M, Zheng H, Apel IJ, McMurry L, Su F, Wang R, Zelenka-Wang S, Sasmal S, Khare L, Mukherjee S, Abbineni C, Aithal K, Bhakta MS, Ghurye J, Cao X, Navone NM, Nesvizhskii AI, Mehra R, Vaishampayan U, Blanchette M, Wang Y, Samajdar S, Ramachandra M, Chinnaiyan AM. Xiao L, et al. Nature. 2022 Jan;601(7893):434-439. doi: 10.1038/s41586-021-04246-z. Epub 2021 Dec 22. Nature. 2022. PMID: 34937944 Free PMC article.
Development of an orally bioavailable mSWI/SNF ATPase degrader and acquired mechanisms of resistance in prostate cancer.
He T, Cheng C, Qiao Y, Cho H, Young E, Mannan R, Mahapatra S, Miner SJ, Zheng Y, Kim N, Zeng VZ, Wisniewski JP, Hou S, Jackson B, Cao X, Su F, Wang R, Chang Y, Kuila B, Mukherjee S, Dukare S, Aithal KB, D S S, Abbineni C, Vaishampayan U, Lyssiotis CA, Parolia A, Xiao L, Chinnaiyan AM. He T, et al. Among authors: aithal kb. Proc Natl Acad Sci U S A. 2024 Apr 9;121(15):e2322563121. doi: 10.1073/pnas.2322563121. Epub 2024 Apr 1. Proc Natl Acad Sci U S A. 2024. PMID: 38557192 Free PMC article.
Development of an orally bioavailable mSWI/SNF ATPase degrader and acquired mechanisms of resistance in prostate cancer.
He T, Cheng C, Qiao Y, Cho H, Young E, Mannan R, Mahapatra S, Miner SJ, Zheng Y, Kim N, Zeng VZ, Wisniewski JP, Hou S, Jackson B, Cao X, Su F, Wang R, Chang Y, Kuila B, Mukherjee S, Dukare S, Aithal KB, D S S, Abbineni C, Lyssiotis CA, Parolia A, Xiao L, Chinnaiyan AM. He T, et al. Among authors: aithal kb. bioRxiv [Preprint]. 2024 Mar 2:2024.02.29.582768. doi: 10.1101/2024.02.29.582768. bioRxiv. 2024. Update in: Proc Natl Acad Sci U S A. 2024 Apr 9;121(15):e2322563121. doi: 10.1073/pnas.2322563121 PMID: 38464081 Free PMC article. Updated. Preprint.