Literature DB >> 20004097

Synthesis and biological activity of a potent and orally bioavailable SCD inhibitor (MF-438).

Serge Léger1, W Cameron Black, Denis Deschenes, Sarah Dolman, Jean-Pierre Falgueyret, Marc Gagnon, Sébastien Guiral, Zheng Huang, Jocelyne Guay, Yves Leblanc, Chun-Sing Li, Frédéric Massé, Renata Oballa, Lei Zhang.   

Abstract

A series of stearoyl-CoA desaturase 1 (SCD1) inhibitors were developed. Investigations of enzyme potency and metabolism led to the identification of the thiadiazole-pyridazine derivative MF-438 as a potent SCD1 inhibitor. MF-438 exhibits good pharmacokinetics and metabolic stability, thereby serving as a valuable tool for further understanding the role of SCD inhibition in biological and pharmacological models of diseases related to metabolic disorders. Copyright 2009 Elsevier Ltd. All rights reserved.

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Year:  2009        PMID： 20004097     DOI： 10.1016/j.bmcl.2009.11.111

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


  17 in total

1.  Plasma-based approach to measure target engagement for liver-targeting stearoyl-CoA desaturase 1 inhibitors.

Authors:  France Landry; Chi-Chung Chan; Zheng Huang; Gregoire Leclair; Chun Sing Li; Renata Oballa; Lei Zhang; Kevin Bateman
Journal:  J Lipid Res       Date:  2011-06-05       Impact factor: 5.922

2.  Stearoyl-CoA-desaturase 1 regulates lung cancer stemness via stabilization and nuclear localization of YAP/TAZ.

Authors:  A Noto; C De Vitis; M E Pisanu; G Roscilli; G Ricci; A Catizone; G Sorrentino; G Chianese; O Taglialatela-Scafati; D Trisciuoglio; D Del Bufalo; M Di Martile; A Di Napoli; L Ruco; S Costantini; Z Jakopin; A Budillon; G Melino; G Del Sal; G Ciliberto; R Mancini
Journal:  Oncogene       Date:  2017-04-03       Impact factor: 9.867

3.  Aberrant lipid metabolism in anaplastic thyroid carcinoma reveals stearoyl CoA desaturase 1 as a novel therapeutic target.

Authors:  Christina A von Roemeling; Laura A Marlow; Anthony B Pinkerton; Angela Crist; James Miller; Han W Tun; Robert C Smallridge; John A Copland
Journal:  J Clin Endocrinol Metab       Date:  2015-02-12       Impact factor: 5.958

4.  Inhibition of stearoyl-CoA desaturase 1 expression induces CHOP-dependent cell death in human cancer cells.

Authors:  Mélaine Minville-Walz; Anne-Sophie Pierre; Laurent Pichon; Sandrine Bellenger; Cécile Fèvre; Jérôme Bellenger; Christian Tessier; Michel Narce; Mickaël Rialland
Journal:  PLoS One       Date:  2010-12-16       Impact factor: 3.240

5.  Systemic down-regulation of delta-9 desaturase promotes muscle oxidative metabolism and accelerates muscle function recovery following nerve injury.

Authors:  Ghulam Hussain; Florent Schmitt; Alexandre Henriques; Thiebault Lequeu; Frederique Rene; Françoise Bindler; Sylvie Dirrig-Grosch; Hugues Oudart; Lavinia Palamiuc; Marie-Helene Metz-Boutigue; Luc Dupuis; Eric Marchioni; Jose-Luis Gonzalez De Aguilar; Jean-Philippe Loeffler
Journal:  PLoS One       Date:  2013-06-13       Impact factor: 3.240

6.  Roles of StearoylCoA Desaturase-1 in the Regulation of Cancer Cell Growth, Survival and Tumorigenesis.

Authors:  R Ariel Igal
Journal:  Cancers (Basel)       Date:  2011-05-20       Impact factor: 6.639

7.  Stearoyl-CoA desaturase-1 is a key factor for lung cancer-initiating cells.

Authors:  A Noto; S Raffa; C De Vitis; G Roscilli; D Malpicci; P Coluccia; A Di Napoli; A Ricci; M R Giovagnoli; L Aurisicchio; M R Torrisi; G Ciliberto; R Mancini
Journal:  Cell Death Dis       Date:  2013-12-05       Impact factor: 8.469

8.  Stearoyl-CoA desaturase inhibition blocks formation of hepatitis C virus-induced specialized membranes.

Authors:  Rodney K Lyn; Ragunath Singaravelu; Stacia Kargman; Shifawn O'Hara; Helen Chan; Renata Oballa; Zheng Huang; Daniel M Jones; Andrew Ridsdale; Rodney S Russell; Anthony W Partridge; John Paul Pezacki
Journal:  Sci Rep       Date:  2014-04-01       Impact factor: 4.379

9.  low neurotrophin receptor CD271 regulates phenotype switching in melanoma.

Authors:  Gaetana Restivo; Johanna Diener; Phil F Cheng; Gregor Kiowski; Mario Bonalli; Thomas Biedermann; Ernst Reichmann; Mitchell P Levesque; Reinhard Dummer; Lukas Sommer
Journal:  Nat Commun       Date:  2017-12-07       Impact factor: 14.919

10.  Membrane lipid saturation activates endoplasmic reticulum unfolded protein response transducers through their transmembrane domains.

Authors:  Romain Volmer; Kattria van der Ploeg; David Ron
Journal:  Proc Natl Acad Sci U S A       Date:  2013-03-04       Impact factor: 11.205
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