PMID- 24900242 OWN - NLM STAT- PubMed-not-MEDLINE DCOM- 20140605 LR - 20240506 IS - 1948-5875 (Print) IS - 1948-5875 (Electronic) IS - 1948-5875 (Linking) VI - 1 IP - 9 DP - 2010 Dec 9 TI - Benzimidazole-2-pyrazole HIF Prolyl 4-Hydroxylase Inhibitors as Oral Erythropoietin Secretagogues. PG - 526-9 LID - 10.1021/ml100198y [doi] AB - HIF prolyl 4-hydroxylases (PHD) are a family of enzymes that mediate key physiological responses to hypoxia by modulating the levels of hypoxia inducible factor 1-alpha (HIF1alpha). Certain benzimidazole-2-pyrazole carboxylates were discovered to be PHD2 inhibitors using ligand- and structure-based methods and found to be potent, orally efficacious stimulators of erythropoietin secretion in vivo. FAU - Rosen, Mark D AU - Rosen MD AD - Johnson & Johnson Pharmaceutical Research and Development, L.L.C, 3210 Merryfield Row, San Diego, California 92121, United States. FAU - Venkatesan, Hariharan AU - Venkatesan H AD - Johnson & Johnson Pharmaceutical Research and Development, L.L.C, 3210 Merryfield Row, San Diego, California 92121, United States. FAU - Peltier, Hillary M AU - Peltier HM AD - Johnson & Johnson Pharmaceutical Research and Development, L.L.C, 3210 Merryfield Row, San Diego, California 92121, United States. FAU - Bembenek, Scott D AU - Bembenek SD AD - Johnson & Johnson Pharmaceutical Research and Development, L.L.C, 3210 Merryfield Row, San Diego, California 92121, United States. FAU - Kanelakis, Kimon C AU - Kanelakis KC AD - Johnson & Johnson Pharmaceutical Research and Development, L.L.C, 3210 Merryfield Row, San Diego, California 92121, United States. FAU - Zhao, Lucy X AU - Zhao LX AD - Johnson & Johnson Pharmaceutical Research and Development, L.L.C, 3210 Merryfield Row, San Diego, California 92121, United States. FAU - Leonard, Barry E AU - Leonard BE AD - Johnson & Johnson Pharmaceutical Research and Development, L.L.C, 3210 Merryfield Row, San Diego, California 92121, United States. FAU - Hocutt, Frances M AU - Hocutt FM AD - Johnson & Johnson Pharmaceutical Research and Development, L.L.C, 3210 Merryfield Row, San Diego, California 92121, United States. FAU - Wu, Xiaodong AU - Wu X AD - Johnson & Johnson Pharmaceutical Research and Development, L.L.C, 3210 Merryfield Row, San Diego, California 92121, United States. FAU - Palomino, Heather L AU - Palomino HL AD - Johnson & Johnson Pharmaceutical Research and Development, L.L.C, 3210 Merryfield Row, San Diego, California 92121, United States. FAU - Brondstetter, Theresa I AU - Brondstetter TI AD - Johnson & Johnson Pharmaceutical Research and Development, L.L.C, 3210 Merryfield Row, San Diego, California 92121, United States. FAU - Haugh, Peter V AU - Haugh PV AD - Johnson & Johnson Pharmaceutical Research and Development, L.L.C, 3210 Merryfield Row, San Diego, California 92121, United States. FAU - Cagnon, Laurence AU - Cagnon L AD - Johnson & Johnson Pharmaceutical Research and Development, L.L.C, 3210 Merryfield Row, San Diego, California 92121, United States. FAU - Yan, Wen AU - Yan W AD - Johnson & Johnson Pharmaceutical Research and Development, L.L.C, 3210 Merryfield Row, San Diego, California 92121, United States. FAU - Liotta, Lisa A AU - Liotta LA AD - Johnson & Johnson Pharmaceutical Research and Development, L.L.C, 3210 Merryfield Row, San Diego, California 92121, United States. FAU - Young, Andrew AU - Young A AD - Johnson & Johnson Pharmaceutical Research and Development, L.L.C, 3210 Merryfield Row, San Diego, California 92121, United States. FAU - Mirzadegan, Tara AU - Mirzadegan T AD - Johnson & Johnson Pharmaceutical Research and Development, L.L.C, 3210 Merryfield Row, San Diego, California 92121, United States. FAU - Shankley, Nigel P AU - Shankley NP AD - Johnson & Johnson Pharmaceutical Research and Development, L.L.C, 3210 Merryfield Row, San Diego, California 92121, United States. FAU - Barrett, Terrance D AU - Barrett TD AD - Johnson & Johnson Pharmaceutical Research and Development, L.L.C, 3210 Merryfield Row, San Diego, California 92121, United States. FAU - Rabinowitz, Michael H AU - Rabinowitz MH AD - Johnson & Johnson Pharmaceutical Research and Development, L.L.C, 3210 Merryfield Row, San Diego, California 92121, United States. LA - eng PT - Journal Article DEP - 20101005 PL - United States TA - ACS Med Chem Lett JT - ACS medicinal chemistry letters JID - 101521073 PMC - PMC4007848 OTO - NOTNLM OT - HIF OT - PHD inhibitors OT - Prolyl 4-hydroxylase inhibitors OT - anemia OT - epo OT - erythropoietin OT - erythropoietin stimulating agents OT - hypoxia inducible factor EDAT- 2010/12/09 00:00 MHDA- 2010/12/09 00:01 PMCR- 2011/12/09 CRDT- 2014/06/06 06:00 PHST- 2010/08/20 00:00 [received] PHST- 2010/09/29 00:00 [accepted] PHST- 2014/06/06 06:00 [entrez] PHST- 2010/12/09 00:00 [pubmed] PHST- 2010/12/09 00:01 [medline] PHST- 2011/12/09 00:00 [pmc-release] AID - 10.1021/ml100198y [doi] PST - epublish SO - ACS Med Chem Lett. 2010 Oct 5;1(9):526-9. doi: 10.1021/ml100198y. eCollection 2010 Dec 9.