In vitrometabolism of an estrogen-related receptor γ modulator, GSK5182, by human liver microsomes and recombinant cytochrome P450s

Author:

Joo Jeongmin1,Wu Zhexue1,Lee Boram1,Shon Jong Cheol1,Lee Taeho1,Lee In-Kyu2,Sim Taebo3,Kim Kyung-Hee4,Kim Nam Doo4,Kim Seong Heon4,Liu Kwang-Hyeon1

Affiliation:

1. College of Pharmacy and Research Institute of Pharmaceutical Sciences; Kyungpook National University; Daegu 702-701 Korea

2. Department of Internal Medicine; Kyungpook National University Hospital, Kyungpook National University School of Medicine; Daegu 700-721 Korea

3. Chemical Kinomics Research Center; Korea Institute of Science and Technology; Seoul 136-791 Korea

4. New Drug Development Center; Daegu-Gyeongbuk Medical Innovation Foundation; Daegu 701-310 Korea

Funder

National Research Foundation of Korea

Ministry of Health & Welfare, Korea

Publisher

Wiley

Subject

Pharmacology (medical),Pharmaceutical Science,Pharmacology,General Medicine

Reference28 articles.

1. Structure-guided synthesis of tamoxifen analogs with improved selectivity for the orphan ERRgamma;Chao;Bioorg Med Chem Lett,2006

2. Human ERRgamma, a third member of the estrogen receptor-related receptor (ERR) subfamily of orphan nuclear receptors: tissue-specific isoforms are expressed during development and in the adult;Heard;Mol Endocrinol,2000

3. Hormone-independent transcriptional activation and coactivator binding by novel orphan nuclear receptor ERR3;Hong;J Biol Chem,1999

4. Orphan nuclear receptor estrogen-related receptor gamma (ERRgamma) is key regulator of hepatic gluconeogenesis;Kim;J Biol Chem,2012

5. Inverse agonist of nuclear receptor ERRgamma mediates antidiabetic effect through inhibition of hepatic gluconeogenesis;Kim;Diabetes,2013

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