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Development of 2-(5,6,7-Trifluoro-1H-Indol-3-yl)-quinoline-5-carboxamide as a Potent, Selective, and Orally Available Inhibitor of Human Androgen Receptor Targeting Its Binding Function-3 for the Treatment of Castration-Resistant Prostate Cancer.
Leblanc E, Ban F, Cavga AD, Lawn S, Huang CF, Mohan S, Chang MEK, Flory MR, Ghaidi F, Lingadahalli S, Chen G, Yu IPL, Morin H, Lallous N, Gleave ME, Mohammed H, Young RN, Rennie PS, Lack NA, Cherkasov A. Leblanc E, et al. J Med Chem. 2021 Oct 28;64(20):14968-14982. doi: 10.1021/acs.jmedchem.1c00681. Epub 2021 Oct 18. J Med Chem. 2021. PMID: 34661404
Targeting Binding Function-3 of the Androgen Receptor Blocks Its Co-Chaperone Interactions, Nuclear Translocation, and Activation.
Lallous N, Leblanc E, Munuganti RS, Hassona MD, Nakouzi NA, Awrey S, Morin H, Roshan-Moniri M, Singh K, Lawn S, Yamazaki T, Adomat HH, Andre C, Daugaard M, Young RN, Guns ES, Rennie PS, Cherkasov A. Lallous N, et al. Mol Cancer Ther. 2016 Dec;15(12):2936-2945. doi: 10.1158/1535-7163.MCT-16-0354. Epub 2016 Oct 7. Mol Cancer Ther. 2016. PMID: 27765852 Free PMC article.