Literature DB >> 19349176

Aleglitazar, a new, potent, and balanced dual PPARalpha/gamma agonist for the treatment of type II diabetes.

Agnes Bénardeau1, Jörg Benz, Alfred Binggeli, Denise Blum, Markus Boehringer, Uwe Grether, Hans Hilpert, Bernd Kuhn, Hans Peter Märki, Markus Meyer, Kurt Püntener, Susanne Raab, Armin Ruf, Daniel Schlatter, Peter Mohr.   

Abstract

Design, synthesis, and SAR of novel alpha-alkoxy-beta-arylpropionic acids as potent and balanced PPARalphagamma coagonists are described. One representative thereof, Aleglitazar ((S)-2Aa), was chosen for clinical development. Its X-ray structure in complex with both receptors as well as its high efficacy in animal models of T2D and dyslipidemia are also presented.

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Year:  2009        PMID： 19349176     DOI： 10.1016/j.bmcl.2009.03.036

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


  16 in total

1.  The NEIGHBOR consortium primary open-angle glaucoma genome-wide association study: rationale, study design, and clinical variables.

Authors:  Janey L Wiggs; Michael A Hauser; Wael Abdrabou; Robert Rand Allingham; Donald L Budenz; Elizabeth Delbono; David S Friedman; Jae H Kang; Douglas Gaasterland; Terry Gaasterland; Richard K Lee; Paul R Lichter; Stephanie Loomis; Yutao Liu; Cathy McCarty; Felipe A Medeiros; Sayoko E Moroi; Lana M Olson; Anthony Realini; Julia E Richards; Frank W Rozsa; Joel S Schuman; Kuldev Singh; Joshua D Stein; Douglas Vollrath; Robert N Weinreb; Gadi Wollstein; Brian L Yaspan; Sachiko Yoneyama; Don Zack; Kang Zhang; Margaret Pericak-Vance; Louis R Pasquale; Jonathan L Haines
Journal:  J Glaucoma       Date:  2013-09       Impact factor: 2.503

2.  The dual PPARα/γ agonist aleglitazar increases the number and function of endothelial progenitor cells: implications for vascular function and atherogenesis.

Authors:  C M Werner; S H Schirmer; C Gensch; V Pavlickova; J Pöss; M B Wright; M Böhm; U Laufs
Journal:  Br J Pharmacol       Date:  2014-05       Impact factor: 8.739

3.  Effects of aleglitazar, a balanced dual peroxisome proliferator-activated receptor α/γ agonist on glycemic and lipid parameters in a primate model of the metabolic syndrome.

Authors:  Barbara C Hansen; Xenia T Tigno; Agnes Bénardeau; Markus Meyer; Elena Sebokova; Jacques Mizrahi
Journal:  Cardiovasc Diabetol       Date:  2011-01-20       Impact factor: 9.951

Review 4.  Modulating peroxisome proliferator-activated receptors for therapeutic benefit? Biology, clinical experience, and future prospects.

Authors:  Robert S Rosenson; R Scott Wright; Michael Farkouh; Jorge Plutzky
Journal:  Am Heart J       Date:  2012-10-16       Impact factor: 4.749

5.  Comparative molecular profiling of the PPARα/γ activator aleglitazar: PPAR selectivity, activity and interaction with cofactors.

Authors:  Michel Dietz; Peter Mohr; Bernd Kuhn; Hans Peter Maerki; Peter Hartman; Armin Ruf; Jörg Benz; Uwe Grether; Matthew B Wright
Journal:  ChemMedChem       Date:  2012-04-04       Impact factor: 3.466

6.  A newly identified CG301269 improves lipid and glucose metabolism without body weight gain through activation of peroxisome proliferator-activated receptor alpha and gamma.

Authors:  Hyun Woo Jeong; Joo-Won Lee; Woo Sik Kim; Sung Sik Choe; Kyung-Hee Kim; Ho Seon Park; Hyun Jung Shin; Gha Young Lee; Dongkyu Shin; Hanjae Lee; Jun Hee Lee; Eun Bok Choi; Hyeon Kyu Lee; Heekyoung Chung; Seung Bum Park; Kyong Soo Park; Hyo-Soo Kim; Seonggu Ro; Jae Bum Kim
Journal:  Diabetes       Date:  2011-02       Impact factor: 9.461

7.  Comparative transcriptional network modeling of three PPAR-α/γ co-agonists reveals distinct metabolic gene signatures in primary human hepatocytes.

Authors:  Renée Deehan; Pia Maerz-Weiss; Natalie L Catlett; Guido Steiner; Ben Wong; Matthew B Wright; Gil Blander; Keith O Elliston; William Ladd; Maria Bobadilla; Jacques Mizrahi; Carolina Haefliger; Alan Edgar
Journal:  PLoS One       Date:  2012-04-13       Impact factor: 3.240

8.  Molecular modelling study of the PPARγ receptor in relation to the mode of action/adverse outcome pathway framework for liver steatosis.

Authors:  Ivanka Tsakovska; Merilin Al Sharif; Petko Alov; Antonia Diukendjieva; Elena Fioravanzo; Mark T D Cronin; Ilza Pajeva
Journal:  Int J Mol Sci       Date:  2014-05-05       Impact factor: 5.923

Review 9.  A cardiologic approach to non-insulin antidiabetic pharmacotherapy in patients with heart disease.

Authors:  Enrique Z Fisman; Alexander Tenenbaum
Journal:  Cardiovasc Diabetol       Date:  2009-07-20       Impact factor: 9.951

10.  Cardiometabolic interventions - focus on transcriptional regulators.

Authors:  Joshua T Chai; Robin P Choudhury
Journal:  Eur J Cardiovasc Med       Date:  2013-08-13
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