TY - JOUR
T1 - Identification of a Potent and Selective GPR4 Antagonist as a Drug Lead for the Treatment of Myocardial Infarction
AU - Fukuda, Hayato
AU - Ito, Saki
AU - Watari, Kenji
AU - Mogi, Chihiro
AU - Arisawa, Mitsuhiro
AU - Okajima, Fumikazu
AU - Kurose, Hitoshi
AU - Shuto, Satoshi
N1 - Publisher Copyright:
© 2016 American Chemical Society.
PY - 2016/5/12
Y1 - 2016/5/12
N2 - GPR4, a pH-sensing G protein-coupled receptor, is highly expressed in endothelial cells and may be activated in myocardial infarction due the decreased tissue pH. We are interested in GPR4 antagonists as potential effective pharmacologic tools and/or drug leads for the treatment of myocardial infarction. We investigated the structure-activity relationship of a known GPR4 antagonist 1 as a lead compound to identify 3b as the first potent and selective GPR4 antagonist, whose effectiveness was demonstrated in a mouse myocardial infarction model.
AB - GPR4, a pH-sensing G protein-coupled receptor, is highly expressed in endothelial cells and may be activated in myocardial infarction due the decreased tissue pH. We are interested in GPR4 antagonists as potential effective pharmacologic tools and/or drug leads for the treatment of myocardial infarction. We investigated the structure-activity relationship of a known GPR4 antagonist 1 as a lead compound to identify 3b as the first potent and selective GPR4 antagonist, whose effectiveness was demonstrated in a mouse myocardial infarction model.
UR - http://www.scopus.com/inward/record.url?scp=84969529128&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84969529128&partnerID=8YFLogxK
U2 - 10.1021/acsmedchemlett.6b00014
DO - 10.1021/acsmedchemlett.6b00014
M3 - Article
AN - SCOPUS:84969529128
SN - 1948-5875
VL - 7
SP - 493
EP - 497
JO - ACS Medicinal Chemistry Letters
JF - ACS Medicinal Chemistry Letters
IS - 5
ER -