@article{75748ee6e296471c88074ebee99dcb07,
title = "Discovery, design and synthesis of Y-shaped peroxisome proliferator- activated receptor δ agonists as potent anti-obesity agents in vivo",
abstract = "We have discovered and demonstrated the in vitro and in vivo PPARδ-selective activity of novel Y-shaped agonists. These compounds activated hPPARδ with EC50 values between 1 and 523 nM. Surprisingly, compounds 10a, 11d, 11e and 11f were the most potent and most selective hPPARδ agonists with 104-fold selectivity over the other two subtypes, namely, hPPARα and hPPARγ. The PPARδ ligands 10a, 11e and 11f showed good bioavailability and in vivo efficacy.",
keywords = "Anti-obesity, GW501516, Marine natural products, Nuclear receptors, PPARδ",
author = "Jungyeob Ham and Hoosang Hwang and Euno Kim and Kim, {Jeong Ah} and Cho, {Sung Jin} and Jaeyoung Ko and Woojin Lee and Jaehwan Lee and Harish Holla and Joydeep Banerjee and Seokho Kim and Inho Yang and Lee, {Hyun Joo} and Kyoungjin Shin and Hyukjae Choi and Nam, {Sang Jip} and Jungae Tak and Dongyup Hahn and Taekyung Oh and Won, {Dong Hwan} and Lee, {Tae Gu} and Jihye Choi and Park, {Mi Sun} and Chaok Seok and Jungwook Chin and Heonjoong Kang",
note = "Funding Information: We are grateful to members of our laboratory. This work was supported by the Marine Biotechnology Program, Ministry of Land, Transport and Maritime Affairs . H. H., J.H., E. K., J. K., I. Y. and J. C. were in part supported by the BK21 program, Ministry of Education, Science and Technology, Korea. ",
year = "2012",
month = jul,
doi = "10.1016/j.ejmech.2012.03.055",
language = "English",
volume = "53",
pages = "190--202",
journal = "European Journal of Medicinal Chemistry",
issn = "0223-5234",
publisher = "Elsevier Masson s.r.l.",
}