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Drug-Receptor Interaction: Agonist01:25

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Agonists are drugs that interact with specific receptors in the body to produce a biological response. When an agonist binds to a receptor, it activates or enhances the receptor's function, leading to physiological effects. The interaction between agonist drugs and receptors is crucial for their therapeutic action in various medical treatments.
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Incretins include glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), which stimulate insulin secretion post-meals. In type 2 diabetes, GIP's efficacy is reduced, making GLP-1 a viable drug target. GIP originates from preproGIP.
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G Protein–Coupled Receptors (GPCRs) are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to various stimuli. GPCRs regulate critical physiological pathways and are excellent drug targets for treating diseases such as diabetes, cancer, obesity, depression, or Alzheimer's. Nearly 35% of approved drugs implement their therapeutic effects by selectively interacting with specific GPCRs.
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Quantifying Agonist Activity at G Protein-coupled Receptors
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GPR119 agonists 2009-2011.

Daniel J Buzard1, Juerg Lehmann, Sangdon Han

  • 1Department of Medicinal Chemistry, Arena Pharmaceuticals, 6166 Nancy Ridge Drive, San Diego, CA 92121, USA.

Pharmaceutical Patent Analyst
|November 19, 2013
PubMed
Summary
This summary is machine-generated.

New research explores G protein-coupled receptor 119 (GPR119) as a novel target for Type II diabetes treatment. Small-molecule agonists for GPR119 show promise for improved blood glucose control.

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Area of Science:

  • Pharmaceutical research and development
  • Endocrinology
  • Drug discovery

Background:

  • Type II diabetes mellitus incidence is rising globally, necessitating novel therapeutic strategies.
  • Glucagon-like peptide-1 receptor (GLP1R) agonists offer glucose-dependent insulin release but peptide mimetics are limited.
  • G protein-coupled receptor 119 (GPR119) presents a promising alternative target for diabetes treatment.

Purpose of the Study:

  • To review patent activity for GPR119 agonists between 2009 and 2011.
  • To assess the emerging landscape of small-molecule approaches targeting GPR119 for diabetes therapy.

Main Methods:

  • Comprehensive literature search of patent filings.
  • Analysis of patent applications related to GPR119 agonists.

Main Results:

  • Significant increase in patent applications for GPR119 agonists from 2009-2011.
  • GPR119 activation enhances incretin levels and insulin secretion in a glucose-dependent manner.

Conclusions:

  • GPR119 is a viable therapeutic target for Type II diabetes.
  • The surge in patent filings indicates strong pharmaceutical interest and R&D in GPR119 small-molecule agonists.