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Structure-based and fragment-based GPCR drug discovery.

Stephen P Andrews1, Giles A Brown, John A Christopher

  • 1Heptares Therapeutics Ltd., BioPark, Welwyn Garden City, Hertfordshire, AL7 3AX (UK).

Chemmedchem
|December 20, 2013
PubMed
Summary
This summary is machine-generated.

Recent advances in stabilizing G protein-coupled receptors (GPCRs) enable structure- and fragment-based drug discovery. This review highlights new structural insights and their application in identifying potential drug candidates for this important target class.

Keywords:
G protein-coupled receptorsfragment-based drug discoverystructural biologystructure-based drug discovery

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Area of Science:

  • Biochemistry
  • Pharmacology
  • Structural Biology

Background:

  • G protein-coupled receptors (GPCRs) are crucial membrane proteins and historically significant drug targets.
  • Drug discovery for GPCRs has been limited by protein instability outside the cell membrane.
  • Recent breakthroughs in stabilizing GPCRs have revolutionized their structural biology.

Purpose of the Study:

  • To review the application of structure- and fragment-based drug discovery techniques to GPCRs.
  • To highlight advances in GPCR structural biology driven by improved receptor stabilization.
  • To discuss the use of these methods in identifying and progressing drug hits.

Main Methods:

  • Review of recent literature on GPCR stabilization techniques.
  • Analysis of structure-based drug discovery approaches applied to GPCRs.
  • Examination of fragment-based drug discovery methods validated for GPCRs.

Main Results:

  • Over the past six years, 21 new GPCR targets have been crystallized with ligands.
  • Increased availability of GPCR structural data facilitates structure-based drug discovery.
  • Fragment-based approaches have been successfully validated for GPCR hit identification.

Conclusions:

  • Advances in GPCR stabilization have unlocked powerful structure- and fragment-based drug discovery strategies.
  • These methods are increasingly utilized for hit identification and optimization in GPCR drug development.
  • The growing body of GPCR structural information promises accelerated therapeutic advancements.