Fragment-based Discovery of Allosteric Modulators on Metabotropic Glutamate Receptor 5

• In: Poster Presentation
• At: Stockholm (Sweden) (2017)
• Type: Poster
• Poster code: P-A-007-Monday
• By: BIAN, Yuemin (University of Pittsburgh, School of Pharmacy, Pittsburgh, United States)
• Co-author(s): Yuemin Bian: School of Pharmacy, University of Pittsburgh, Pittsburgh, United States;Drug Discovery Institute, University of Pittsburgh, Pittsburgh, United States;NIH National Center of Excellence for Computational Drug Abuse Research, National Institution of Health, Pittsburgh, United States
  Zhiwei Feng: School of Pharmacy, University of Pittsburgh, Pittsburgh, United States;Drug Discovery Institute, University of Pittsburgh, Pittsburgh, United States;NIH National Center of Excellence for Computational Drug Abuse Research, National Institution of Health, Pittsburgh, United States
  Peng Yang: School of Pharmacy, University of Pittsburgh, Pittsburgh, United States;Drug Discovery Institute, University of Pittsburgh, Pittsburgh, United States;NIH National Center of Excellence for Computational Drug Abuse Research, National Institution of Health, Pittsburgh, United States
  Xiang-Qun Xie: School of Pharmacy, University of Pittsburgh, Pittsburgh, United States;NIH National Center of Excellence for Computational Drug Abuse Research, National Institution of Health, Pittsburgh, United States;Drug Discovery Institute, University of Pittsburgh, Pittsburgh, United States;Department of Computational Biology and Structural Biology, University of Pittsburgh, Pittsburgh, United States
  
• Abstract:

  Backgrounds

  Allosteric modulators exhibit significant advantages against the corresponding orthosteric ligands, including better physicochemical properties, improved selectivity, and reduced risk of over-sensitization towards their receptors. mGlu₅, a member of class C GPCRs, has been considered a promising therapeutic target for treating many CNS..

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