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Related Concept Videos

GPCR Desensitization01:12

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G protein-coupled receptor (GPCR) signaling plays a crucial role in cell functioning. GPCR desensitization is an equally essential process. It allows cells to respond to changing environments and regain sensitivity to new stimuli while preventing unnecessary stimulation when no longer needed. Prolonged exposure to stimuli leads to GPCR desensitization. It involves blocking the receptors from binding and activating additional G proteins. This inhibits activation of downstream effectors, thereby...
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Drug discovery is a multifaceted process involving extensive screening, testing, and optimization of lead compounds to identify potential new drugs for therapeutic use. It combines several approaches, including screening large numbers of natural products, chemical modification of known active molecules, identification of new drug targets, and rational design based on biological mechanisms and drug-receptor structure. These approaches are carried out in both academic research laboratories and...
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Many fundamental cell functions such as muscle contraction and nerve transmission rely on the electrical signals produced by the movement of positively and negatively charged ions across the cell membrane. One competent method to record current flowing across the whole cell or single ion channel is the patch-clamp technique.
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Updated: Sep 20, 2025

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Accelerating GPCR Drug Discovery With Conformation-Stabilizing VHHs.

Toon Laeremans1, Zara A Sands1, Pieter Claes1

  • 1Confo Therapeutics NV, Zwijnaarde, Belgium.

Frontiers in Molecular Biosciences
|June 9, 2022
PubMed
Summary

Camelid-derived single variable domains (ConfoBodies) stabilize G protein-coupled receptors (GPCRs) for drug discovery. These tools enhance screening and structure-based design, accelerating the development of novel GPCR-targeted therapeutics.

Keywords:
ConfoBodyGPCRSBDDVHHactive statebiosensorconformationconformer

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Area of Science:

  • Biochemistry and structural biology
  • Pharmacology and drug discovery
  • Molecular and cellular biology

Background:

  • G protein-coupled receptors (GPCRs) are crucial drug targets, with 40% of marketed drugs modulating them.
  • Significant potential exists for targeting the 60% of non-olfactory GPCRs lacking clinical candidates.
  • Conventional high-throughput screening (HTS) for GPCRs faces challenges due to low success rates and difficulties in structure determination.

Purpose of the Study:

  • To review the application of camelid-derived immunoglobulin single variable domains (VHHs), termed ConfoBodies, for stabilizing GPCRs.
  • To highlight how ConfoBodies accelerate drug discovery by enabling better understanding of GPCR pharmacology and structure.
  • To demonstrate the impact of ConfoBodies on translational research through active state screening and structure-informed drug design.

Main Methods:

  • Utilizing VHHs (ConfoBodies) to stabilize specific GPCR conformations and GPCR:signal transducer complexes.
  • Employing stabilized GPCRs for enhanced in vitro screening assays.
  • Applying structural biology techniques to ConfoBody-stabilized GPCRs for structure-based drug design.

Main Results:

  • ConfoBodies effectively stabilize disease-relevant GPCR states and complexes.
  • These stabilized targets facilitate improved screening and deconvolution of complex GPCR pharmacology.
  • Structure-informed design using ConfoBody-stabilized GPCRs enables identification of novel chemical matter with improved potency and selectivity.

Conclusions:

  • ConfoBodies are powerful tools for overcoming challenges in GPCR drug discovery.
  • They significantly enhance the efficiency of screening campaigns and structure-based rational design.
  • ConfoBodies hold substantial promise for accelerating the development of novel therapeutics targeting GPCRs.