A Combined Bioinformatics and Chemoinformatics Approach for Developing Asymmetric Bivalent AMPA Receptor Positive Allosteric Modulators as Neuroprotective Agents

Haijun Chen, Cheng Z. Wang, Chunyong Ding, Christopher Wild, Bryan Copits, Geoffrey T. Swanson, Kenneth M. Johnson, Jia Zhou

Research output: Contribution to journalArticlepeer-review

24 Scopus citations

Abstract

PAMs new in town! An effective, combined bioinformatics and chemoinformatics approach was applied to the design of novel asymmetric bivalent α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor positive allosteric modulators (PAMs) with marked potency invitro and efficacy invivo for preventing neuroapoptosis. The novel chemotype could provide pharmacological probes and potential therapeutic agents for glutamatergic hypofunction and its related neurological and psychiatric disorders.

Original languageEnglish (US)
Pages (from-to)226-230
Number of pages5
JournalChemMedChem
Volume8
Issue number2
DOIs
StatePublished - Feb 2013

Keywords

  • Bioinformatics
  • Biological space
  • Chemical space
  • Chemoinformatics
  • Drug design
  • Neuroprotective agents

ASJC Scopus subject areas

  • Drug Discovery
  • General Pharmacology, Toxicology and Pharmaceutics
  • Molecular Medicine
  • Biochemistry
  • Pharmacology
  • Organic Chemistry

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