Literature DB >> 11958991

Highly potent inhibitors of TNF-alpha production. Part 2: identification of drug candidates.

Toshiaki Matsui1, Takashi Kondo, Yoshitaka Nishita, Satoshi Itadani, Hiroshi Tsuruta, Setsuko Fujita, Nagashige Omawari, Masaru Sakai, Shuichi Nakazawa, Akihito Ogata, Hideaki Mori, Hiroyuki Ohno, Takaaki Obata, Hisao Nakai, Masaaki Toda.   

Abstract

Metabolic stabilization of the chemical lead 1, which is a structurally novel inhibitor of TNF-alpha production, was accomplished by introducing a (1S)-methyl group into the optically active backbone. As a result, 2, 3 and 4 were identified as drug candidates and evaluated pharmacologically. The analysis of an active conformer was also carried out.

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Year:  2002        PMID: 11958991     DOI: 10.1016/s0960-894x(02)00037-9

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  5 in total

1.  Exogenous ceramide-1-phosphate (C1P) and phospho-ceramide analogue-1 (PCERA-1) regulate key macrophage activities via distinct receptors.

Authors:  Sebastián Katz; Orna Ernst; Dorit Avni; Muhammad Athamna; Amir Philosoph; Lide Arana; Alberto Ouro; L Alexis Hoeferlin; Michael M Meijler; Charles E Chalfant; Antonio Gómez-Muñoz; Tsaffrir Zor
Journal:  Immunol Lett       Date:  2015-12-03       Impact factor: 3.685

2.  The ceramide-1-phosphate analogue PCERA-1 modulates tumour necrosis factor-alpha and interleukin-10 production in macrophages via the cAMP-PKA-CREB pathway in a GTP-dependent manner.

Authors:  Dorit Avni; Amir Philosoph; Michael M Meijler; Tsaffrir Zor
Journal:  Immunology       Date:  2009-11-16       Impact factor: 7.397

3.  A ceramide-1-phosphate analogue, PCERA-1, simultaneously suppresses tumour necrosis factor-alpha and induces interleukin-10 production in activated macrophages.

Authors:  Meir Goldsmith; Dorit Avni; Galit Levy-Rimler; Roi Mashiach; Orna Ernst; Maya Levi; Bill Webb; Michael M Meijler; Nathanael S Gray; Hugh Rosen; Tsaffrir Zor
Journal:  Immunology       Date:  2009-05       Impact factor: 7.397

Review 4.  The role of ceramide-1-phosphate in biological functions.

Authors:  L Alexis Hoeferlin; Dayanjan S Wijesinghe; Charles E Chalfant
Journal:  Handb Exp Pharmacol       Date:  2013

5.  Ceramide kinase regulates the production of tumor necrosis factor α (TNFα) via inhibition of TNFα-converting enzyme.

Authors:  Nadia F Lamour; Dayanjan S Wijesinghe; Jennifer A Mietla; Katherine E Ward; Robert V Stahelin; Charles E Chalfant
Journal:  J Biol Chem       Date:  2011-10-18       Impact factor: 5.157

  5 in total

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