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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. Among authors: yu ipl. 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
Functional mapping of androgen receptor enhancer activity.
Huang CF, Lingadahalli S, Morova T, Ozturan D, Hu E, Yu IPL, Linder S, Hoogstraat M, Stelloo S, Sar F, van der Poel H, Altintas UB, Saffarzadeh M, Le Bihan S, McConeghy B, Gokbayrak B, Feng FY, Gleave ME, Bergman AM, Collins C, Hach F, Zwart W, Emberly E, Lack NA. Huang CF, et al. Among authors: yu ipl. Genome Biol. 2021 May 11;22(1):149. doi: 10.1186/s13059-021-02339-6. Genome Biol. 2021. PMID: 33975627 Free PMC article.
Extensive androgen receptor enhancer heterogeneity in primary prostate cancers underlies transcriptional diversity and metastatic potential.
Kneppers J, Severson TM, Siefert JC, Schol P, Joosten SEP, Yu IPL, Huang CF, Morova T, Altıntaş UB, Giambartolomei C, Seo JH, Baca SC, Carneiro I, Emberly E, Pasaniuc B, Jerónimo C, Henrique R, Freedman ML, Wessels LFA, Lack NA, Bergman AM, Zwart W. Kneppers J, et al. Among authors: yu ipl. Nat Commun. 2022 Nov 30;13(1):7367. doi: 10.1038/s41467-022-35135-2. Nat Commun. 2022. PMID: 36450752 Free PMC article.
Genomic and transcriptomic features of androgen receptor signaling inhibitor resistance in metastatic castration-resistant prostate cancer.
Zhu X, Farsh T, Vis D, Yu I, Li H, Liu T, Sjöström M, Shrestha R, Kneppers J, Severson T, Zhang M, Lundberg A, Moreno Rodriguez T, Weinstein AS, Foye A, Mehra N, Aggarwal RR, Bergman AM, Small EJ, Lack NA, Zwart W, Quigley DA, van der Heijden MS, Feng FY. Zhu X, et al. J Clin Invest. 2024 Aug 13;134(19):e178604. doi: 10.1172/JCI178604. J Clin Invest. 2024. PMID: 39352383 Free PMC article.