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Crystal structures of AKR1C3 containing an N-(aryl)amino-benzoate inhibitor and a bifunctional AKR1C3 inhibitor and androgen receptor antagonist. Therapeutic leads for castrate resistant prostate cancer.
Chen M, Adeniji AO, Twenter BM, Winkler JD, Christianson DW, Penning TM. Chen M, et al. Bioorg Med Chem Lett. 2012 May 15;22(10):3492-7. doi: 10.1016/j.bmcl.2012.03.085. Epub 2012 Mar 29. Bioorg Med Chem Lett. 2012. PMID: 22507964 Free PMC article.
We have previously developed a series of flufenamic acid analogs as potent and selective AKR1C3 inhibitors [Adeniji, A. O. et al., J. Med. Chem.2012, 55, 2311]. Here we report the X-ray crystal structure of one lead compound 3-((4-(trifluoromethyl)phenyl) ami …
We have previously developed a series of flufenamic acid analogs as potent and selective AKR1C3 inhibitors [Adeniji, A. O
Risk Factor Characterization of Ischemic Stroke Subtypes Among West Africans.
Sarfo FS, Ovbiagele B, Akpa O, Akpalu A, Wahab K, Obiako R, Komolafe M, Owolabi L, Ogbole G, Calys-Tagoe B, Fakunle A, Sanni T, Mulugeta G, Abdul S, Akintunde AA, Olowookere S, Uvere EO, Ibinaiye P, Akinyemi J, Uwanuruochi K, Olayemi B, Odunlami OA, Abunimye E, Arulogun O, Isah SY, Abubakar SA, Oladimeji A, Adebayo P, Shidali V, Chukwuonye II, Akpalu J, Tito-Ilori MM, Asowata OJ, Sanya EO, Amusa G, Onyeonoro U, Ogunmodede JA, Sule AG, Akisanya C, Mensah Y, Oyinloye OI, Appiah L, Agunloye AM, Osaigbovo GO, Olabinri E, Kolo PM, Okeke O, Adeoye AM, Ajose O, Jenkins C, Lackland DT, Egberongbe AA, Adeniji O, Ohifemen Adeleye O, Tiwari HK, Arnett D, Laryea RY, Olunuga T, Akinwande KS, Imoh L, Ogah OS, Melikam ES, Adebolaji A, Oguike W, Ogunronbi O, Adeniyi W, Olugbo OY, Bello AH, Ohagwu KA, Ogunjimi L, Agyekum F, Iheonye H, Adesina J, Diala S, Dambatta HA, Ikubor J, Singh A, Adamu S, Obese V, Adusei N, Owusu D, Ampofo M, Tagge R, Efidi R, Fawale B, Yaria J, Akinyemi R, Owolabi M; SIREN. Sarfo FS, et al. Stroke. 2022 Jan;53(1):134-144. doi: 10.1161/STROKEAHA.120.032072. Epub 2021 Sep 30. Stroke. 2022. PMID: 34587795 Free PMC article.