Literature DB >> 17034149

Structural basis for the structure-activity relationships of peroxisome proliferator-activated receptor agonists.

Neeraj Mahindroo1, Yi-Hui Peng, Chia-Hui Lin, Uan-Kang Tan, Ekambaranellore Prakash, Tzu-Wen Lien, I-Lin Lu, Hong-Jen Lee, John Tsu-An Hsu, Xin Chen, Chun-Chen Liao, Ping-Chiang Lyu, Yu-Sheng Chao, Su-Ying Wu, Hsing-Pang Hsieh.   

Abstract

Type 2 diabetes has rapidly reached an epidemic proportion becoming a major threat to global public health. PPAR agonists have emerged as a leading class of oral antidiabetic drugs. We report a structure biology analysis of novel indole-based PPAR agonists to explain the structure-activity relationships and present a critical analysis of reasons for change in selectivity with change in the orientation of the same scaffolds. The results would be helpful in designing novel PPAR agonists.

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Year:  2006        PMID: 17034149     DOI: 10.1021/jm060663c

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  4 in total

1.  Dietary α-eleostearic acid ameliorates experimental inflammatory bowel disease in mice by activating peroxisome proliferator-activated receptor-γ.

Authors:  Stephanie N Lewis; Lera Brannan; Amir J Guri; Pinyi Lu; Raquel Hontecillas; Josep Bassaganya-Riera; David R Bevan
Journal:  PLoS One       Date:  2011-08-31       Impact factor: 3.240

2.  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

3.  Exploring Ligand Stability in Protein Crystal Structures Using Binding Pose Metadynamics.

Authors:  Lucia Fusani; David S Palmer; Don O Somers; Ian D Wall
Journal:  J Chem Inf Model       Date:  2020-01-22       Impact factor: 4.956

4.  Virtual Screening as a Technique for PPAR Modulator Discovery.

Authors:  Stephanie N Lewis; Josep Bassaganya-Riera; David R Bevan
Journal:  PPAR Res       Date:  2009-09-02       Impact factor: 4.964

  4 in total

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