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Literature DB >> 31312410

Discovery of a Novel Selective Dual Peroxisome Proliferator-Activated Receptor α/δ Agonist for the Treatment of Primary Biliary Cirrhosis.

Zhigan Jiang¹, Xing Liu², Zhiliang Yuan¹, Haiying He¹, Jing Wang¹, Xiao Zhang¹, Zhen Gong¹, Lijuan Hou¹, Liang Shen¹, Fengxun Guo¹, Jiliang Zhang¹, Jianhua Wang¹, Deming Xu¹, Zhuowei Liu^2,3, Haijun Li^2,3, Xiaoxin Chen^2,3, Chaofeng Long^2,3, Jian Li¹, Shuhui Chen¹.

Abstract

A novel peroxisome proliferator-activated receptor (PPAR) α/δ dual agonist 5c was developed with an EC50 of 8 nM for PPARα, 5 nM for PPARδ, and >300-fold selectivity against PPARγ (EC50 = 2939 nM), respectively. Further ADME and pharmacokinetic studies indicated 5c possessed distinguished in vitro and in vivo profiles. The excellent in vivo efficacy of compound 5c was demonstrated by the rat primary biliary cirrhosis (PBC) model.

Entities: Disease Gene Species

Year: 2019 PMID： 31312410 PMCID： PMC6627728 DOI： 10.1021/acsmedchemlett.9b00189

Source DB: PubMed Journal: ACS Med Chem Lett ISSN： 1948-5875 Impact factor: 4.345

39 in total

1. The effect of ursodeoxycholic acid therapy on liver fibrosis progression in primary biliary cirrhosis.

Authors: C Corpechot; F Carrat; A M Bonnand; R E Poupon; R Poupon
Journal: Hepatology Date: 2000-12 Impact factor: 17.425

2. Fenofibrate treatment in patients with primary biliary cirrhosis.

Authors: Hiromasa Ohira; Yukio Sato; Takato Ueno; Michio Sata
Journal: Am J Gastroenterol Date: 2002-08 Impact factor: 10.864

3. (3-substituted benzyl)thiazolidine-2,4-diones as structurally new antihyperglycemic agents.

Authors: M Nomura; S Kinoshita; H Satoh; T Maeda; K Murakami; M Tsunoda; H Miyachi; K Awano
Journal: Bioorg Med Chem Lett Date: 1999-02-22 Impact factor: 2.823

4. Long-term ursodeoxycholic acid delays histological progression in primary biliary cirrhosis.

Authors: P Angulo; K P Batts; T M Therneau; R A Jorgensen; E R Dickson; K D Lindor
Journal: Hepatology Date: 1999-03 Impact factor: 17.425

5. Molecular recognition of fatty acids by peroxisome proliferator-activated receptors.

Authors: H E Xu; M H Lambert; V G Montana; D J Parks; S G Blanchard; P J Brown; D D Sternbach; J M Lehmann; G B Wisely; T M Willson; S A Kliewer; M V Milburn
Journal: Mol Cell Date: 1999-03 Impact factor: 17.970

6. Structure of the PPARalpha and -gamma ligand binding domain in complex with AZ 242; ligand selectivity and agonist activation in the PPAR family.

Authors: P Cronet; J F Petersen; R Folmer; N Blomberg; K Sjöblom; U Karlsson; E L Lindstedt; K Bamberg
Journal: Structure Date: 2001-08 Impact factor: 5.006

7. Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.

Authors: Per Sauerberg; Ingrid Pettersson; Lone Jeppesen; Paul S Bury; John P Mogensen; Karsten Wassermann; Christian L Brand; Jeppe Sturis; Helle F Wöldike; Jan Fleckner; Anne-Sofie T Andersen; Steen B Mortensen; L Anders Svensson; Hanne B Rasmussen; Søren V Lehmann; Zdenek Polivka; Karel Sindelar; Vladimira Panajotova; Lars Ynddal; Erik M Wulff
Journal: J Med Chem Date: 2002-02-14 Impact factor: 7.446

Review 8. Primary biliary cirrhosis.

Authors: Jayant A Talwalkar; Keith D Lindor
Journal: Lancet Date: 2003-07-05 Impact factor: 79.321