Literature DB >> 18057753

Structural development of liver X receptor (LXR) antagonists derived from thalidomide-related glucosidase inhibitors.

Tomomi Noguchi-Yachide1, Hiroyuki Miyachi, Hiroshi Aoyama, Atsushi Aoyama, Makoto Makishima, Yuichi Hashimoto.   

Abstract

Following our previous discovery of LXR antagonistic activity of 2'-substituted phenylphthalimides derived from thalidomide-related glucosidase inhibitors, structure-activity studies and further structural development led to 5-chloro-N-2'-n-pentylphenyl-1,3-dithiophthalimide (5CPPSS-50), with IC50 values of about 10 and 13 microM for LXRalpha and LXRbeta, respectively.

Entities:  

Mesh：

Substances：

Year:  2007        PMID： 18057753     DOI： 10.1248/cpb.55.1750

Source DB:  PubMed          Journal:  Chem Pharm Bull (Tokyo)        ISSN： 0009-2363            Impact factor:   1.645


  4 in total

1.  Borylated 2,3,4,5-Tetrachlorophthalimide and Their 2,3,4,5-Tetrachlorobenzamide Analogues: Synthesis, Their Glycosidase Inhibition and Anticancer Properties in View to Boron Neutron Capture Therapy.

Authors:  David M Campkin; Yuna Shimadate; Barbara Bartholomew; Paul V Bernhardt; Robert J Nash; Jennette A Sakoff; Atsushi Kato; Michela I Simone
Journal:  Molecules       Date:  2022-05-26       Impact factor: 4.927

2.  Transcriptional regulation of human and rat hepatic lipid metabolism by the grapefruit flavonoid naringenin: role of PPARalpha, PPARgamma and LXRalpha.

Authors:  Jonathan Goldwasser; Pazit Y Cohen; Eric Yang; Patrick Balaguer; Martin L Yarmush; Yaakov Nahmias
Journal:  PLoS One       Date:  2010-08-25       Impact factor: 3.240

3.  Polarization of M2 macrophages requires Lamtor1 that integrates cytokine and amino-acid signals.

Authors:  Tetsuya Kimura; Shigeyuki Nada; Noriko Takegahara; Tatsusada Okuno; Satoshi Nojima; Sujin Kang; Daisuke Ito; Keiko Morimoto; Takashi Hosokawa; Yoshitomo Hayama; Yuichi Mitsui; Natsuki Sakurai; Hana Sarashina-Kida; Masayuki Nishide; Yohei Maeda; Hyota Takamatsu; Daisuke Okuzaki; Masaki Yamada; Masato Okada; Atsushi Kumanogoh
Journal:  Nat Commun       Date:  2016-10-12       Impact factor: 14.919

4.  Normalizing glycosphingolipids restores function in CD4+ T cells from lupus patients.

Authors:  Georgia McDonald; Shantal Deepak; Laura Miguel; Cleo J Hall; David A Isenberg; Anthony I Magee; Terry Butters; Elizabeth C Jury
Journal:  J Clin Invest       Date:  2014-01-27       Impact factor: 14.808
  4 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.