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Related Concept Videos

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Pharmacogenomics: Identification of New Drug Targets

Advances in genomics have profoundly influenced drug discovery by increasing both the speed and accuracy of pharmaceutical development. Pharmacogenomics, which examines how genetic variation influences drug response, facilitates the identification of novel therapeutic targets and enables patient stratification for personalized treatment. These strategies contribute to improved drug efficacy, minimized adverse effects, and more efficient clinical trial design.Mapping genetic differences...

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A Flow Cytometry-based Assay to Identify Compounds That Disrupt Binding of Fluorescently-labeled CXC Chemokine Ligand 12 to CXC Chemokine Receptor 4
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CCR5 pharmacology methodologies and associated applications.

Roy Mansfield1, Sarah Able, Paul Griffin

  • 1Pfizer GRD-Sandwich Laboratories, Sandwich, Kent, United Kingdom.

Methods in Enzymology
|May 19, 2009
PubMed
Summary

The chemokine receptor CCR5 is crucial for HIV-1 entry. Blocking CCR5 with drugs like maraviroc offers a new treatment strategy for HIV infection and potentially inflammatory diseases.

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Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors
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Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors
16:16

Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors

Published on: September 13, 2013

Area of Science:

  • Immunology
  • Virology
  • Pharmacology

Background:

  • CCR5 is a G protein-coupled receptor involved in immune responses.
  • Its primary role in research is as a coreceptor for HIV-1 entry into host cells.
  • Genetic studies show CCR5 deficiency confers resistance to HIV-1 infection.

Purpose of the Study:

  • To describe methods for characterizing CCR5 pharmacology.
  • To detail the application of this data in drug discovery for HIV-1.
  • To highlight maraviroc as a CCR5 antagonist for HIV treatment.

Main Methods:

  • Pharmacological characterization of CCR5.
  • Functional assays to assess CCR5 antagonist activity.
  • Application of drug discovery principles to identify CCR5 blockers.

Main Results:

  • Identification of potent functional antagonists for CCR5.
  • Maraviroc demonstrated significant anti-HIV-1 activity.
  • CCR5 antagonists offer a novel therapeutic approach for HIV infection.

Conclusions:

  • CCR5 antagonists represent a new class of anti-HIV drugs.
  • Maraviroc is a key example of successful CCR5-targeted therapy.
  • CCR5-based strategies may also benefit inflammatory conditions.