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Allosteric Modalities for Membrane-Bound Receptors: Insights from Drug Hunting for Brain Diseases

Journal of Medicinal Chemistry, ISSN: 1520-4804, Vol: 62, Issue: 13, Page: 5979-6002
2019
  • 14
    Citations
  • 0
    Usage
  • 56
    Captures
  • 0
    Mentions
  • 0
    Social Media
Metric Options:   Counts1 Year3 Year

Metrics Details

  • Citations
    14
    • Citation Indexes
      14
  • Captures
    56

Review Description

Medicinal chemists are accountable for embedding the appropriate drug target profile into the molecular architecture of a clinical candidate. An accurate characterization of the functional effects following binding of a drug to its biological target is a fundamental step in the discovery of new medicines, informing the translation of preclinical efficacy and safety observations into human trials. Membrane-bound proteins, particularly ion channels and G protein-coupled receptors (GPCRs), are biological targets prone to allosteric modulation. Investigations using allosteric drug candidates and chemical tools suggest that their functional effects may be tailored with a high degree of translational alignment, making them molecular tools to correct pathophysiological functional tone and enable personalized medicine when a causative target-to-disease link is known. We present select examples of functional molecular fine-tuning of allosterism and discuss consequences relevant to drug design.

Bibliographic Details

Coughlin, Quinn; Hopper, Allen T; Blanco, Maria-Jesus; Tirunagaru, Vijaya; Robichaud, Albert J; Doller, Dario

American Chemical Society (ACS)

Biochemistry, Genetics and Molecular Biology; Pharmacology, Toxicology and Pharmaceutics

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