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Benzimidazole-2-pyrazole HIF Prolyl 4-Hydroxylase Inhibitors as Oral Erythropoietin Secretagogues.
Rosen MD, Venkatesan H, Peltier HM, Bembenek SD, Kanelakis KC, Zhao LX, Leonard BE, Hocutt FM, Wu X, Palomino HL, Brondstetter TI, Haugh PV, Cagnon L, Yan W, Liotta LA, Young A, Mirzadegan T, Shankley NP, Barrett TD, Rabinowitz MH. Rosen MD, et al. Among authors: brondstetter ti. ACS Med Chem Lett. 2010 Oct 5;1(9):526-9. doi: 10.1021/ml100198y. eCollection 2010 Dec 9. ACS Med Chem Lett. 2010. PMID: 24900242 Free PMC article.
Prolyl hydroxylase inhibition corrects functional iron deficiency and inflammation-induced anaemia in rats.
Barrett TD, Palomino HL, Brondstetter TI, Kanelakis KC, Wu X, Yan W, Merton KP, Schoetens F, Ma JY, Skaptason J, Gao J, Tran DT, Venkatesan H, Rosen MD, Shankley NP, Rabinowitz MH. Barrett TD, et al. Among authors: brondstetter ti. Br J Pharmacol. 2015 Aug;172(16):4078-88. doi: 10.1111/bph.13188. Epub 2015 Jun 26. Br J Pharmacol. 2015. PMID: 25988595 Free PMC article.
Beyond Traditional Structure-Based Drug Design: The Role of Iron Complexation, Strain, and Water in the Binding of Inhibitors for Hypoxia-Inducible Factor Prolyl Hydroxylase 2.
Bembenek SD, Venkatesan H, Peltier HM, Rosen MD, Barrett TD, Kanelakis KC, Palomino HL, Brondstetter TI, Mirzadegan T, Rabinowitz MH. Bembenek SD, et al. Among authors: brondstetter ti. ACS Omega. 2019 Apr 30;4(4):6703-6708. doi: 10.1021/acsomega.9b00199. Epub 2019 Apr 12. ACS Omega. 2019. PMID: 31179408 Free PMC article.
Pharmacological characterization of 1-(5-chloro-6-(trifluoromethoxy)-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid (JNJ-42041935), a potent and selective hypoxia-inducible factor prolyl hydroxylase inhibitor.
Barrett TD, Palomino HL, Brondstetter TI, Kanelakis KC, Wu X, Haug PV, Yan W, Young A, Hua H, Hart JC, Tran DT, Venkatesan H, Rosen MD, Peltier HM, Sepassi K, Rizzolio MC, Bembenek SD, Mirzadegan T, Rabinowitz MH, Shankley NP. Barrett TD, et al. Among authors: brondstetter ti. Mol Pharmacol. 2011 Jun;79(6):910-20. doi: 10.1124/mol.110.070508. Epub 2011 Mar 3. Mol Pharmacol. 2011. PMID: 21372172