Discovery of a “Gatekeeper” Antagonist that Blocks Entry Pathway to Retinoid X Receptors (RXRs) without Allosteric Ligand Inhibition in Permissive RXR Heterodimers-Reference-Cited by-同舟云学术

Discovery of a “Gatekeeper” Antagonist that Blocks Entry Pathway to Retinoid X Receptors (RXRs) without Allosteric Ligand Inhibition in Permissive RXR Heterodimers

Published:2020-12-24 Issue:1 Volume:64 Page:430-439
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Watanabe Masaki¹,Fujihara Michiko¹²,Motoyama Tomoharu³,Kawasaki Mayu³,Yamada Shoya¹⁴,Takamura Yuta¹,Ito Sohei³^ORCID,Makishima Makoto⁵^ORCID,Nakano Shogo³^ORCID,Kakuta Hiroki¹^ORCID

Affiliation:

1. Division of Pharmaceutical Sciences, Okayama University Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, 1-1-1, Tsushima-naka, Kita-ku, Okayama 700-8530, Japan

2. AIBIOS Company. Ltd., Tri-Seven Roppongi 8F 7-7-7 Roppongi, Minato-ku, Tokyo 106-0032, Japan

3. Graduate School of Integrated Pharmaceutical and Nutritional Sciences, University of Shizuoka, 52-1 Yada, Suruga-ku, Shizuoka 422-8526, Japan

4. Research Fellowship Division, Japan Society for the Promotion of Science, Sumitomo-Ichibancho FS Bldg., 8 Ichibancho, Chiyoda-ku, Tokyo 102-8472, Japan

5. Division of Biochemistry, Department of Biomedical Sciences, Nihon University School of Medicine, 30-1 Oyaguchi-kamicho, Itabashi-ku, Tokyo 173-8610, Japan

Funder

Tokyo Biochemical Research Foundation

Japan Society for the Promotion of Science

Kobayashi Foundation

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.0c01354

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1. The nuclear receptor superfamily: The second decade