Ham, Jungyeob Hwang, Hoosang Kim, Euno Kim, Jeong-ah Cho, Sung Jin Ko, Jaeyoung Lee, Woojin Lee, Jaehwan Holla, Harish Banerjee, Joydeep Kim, Seokho Yang, Inho Lee, Hyun Joo Shin, Kyoungjin Choi, Hyukjae Nam, Sang-Jip Tak, Jungae Hahn, Dongyup Oh, Taekyung Won, Dong Hwan Lee, Tae Gu Choi, Jihye Park, Mi Sun Seok, Chaok Chin, Jungwook Kang, Heonjoong 2024-01-20T14:32:27Z 2024-01-20T14:32:27Z 2021-08-31 2012-07 0223-5234 https://pubs.kist.re.kr/handle/201004/129133 We have discovered and demonstrated the in vitro and in vivo PPAR delta-selective activity of novel Y-shaped agonists. These compounds activated hPPAR delta with EC50 values between 1 and 523 nM. Surprisingly, compounds 10a, 11d, 11e and 11f were the most potent and most selective hPPAR delta agonists with 10(4)-fold selectivity over the other two subtypes, namely, hPPAR alpha and hPPAR gamma. The PPAR delta ligands 10a, 11e and 11f showed good bioavailability and in vivo efficacy. (C) 2012 Elsevier Masson SAS. All rights reserved. English ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER BETA-OXIDATION PATHWAY PPAR-DELTA FATTY-ACIDS ALPHA GAMMA IDENTIFICATION METABOLISM EXPRESSION SULFIDES LIGANDS Discovery, design and synthesis of Y-shaped peroxisome proliferator-activated receptor delta agonists as potent anti-obesity agents in vivo Article 10.1016/j.ejmech.2012.03.055 1 EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, v.53, pp.190 - 202 EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 53 190 202 scie scopus 000305863100020 Chemistry, Medicinal Pharmacology & Pharmacy Article BETA-OXIDATION PATHWAY PPAR-DELTA FATTY-ACIDS ALPHA GAMMA IDENTIFICATION METABOLISM EXPRESSION SULFIDES LIGANDS PPAR delta Nuclear receptors Marine natural products Anti-obesity GW501516