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Challenges in developing P2 purinoceptor-based therapeutics

M Williams1

  • 1Neuroscience Discovery, Abbott Laboratories, Abbott Park, IL 60064, USA.

Ciba Foundation Symposium
|January 1, 1996
PubMed
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P2 purinoceptors, including adenosine triphosphate (ATP) and uridine triphosphate (UTP), regulate tissue function and show therapeutic potential. Identifying selective receptor subtype interactions is key for drug discovery.

Area of Science:

  • Pharmacology
  • Molecular Biology
  • Biochemistry

Background:

  • P2 purinoceptor superfamily plays a diverse role in tissue function regulation.
  • Specific P2 receptor subtypes likely have distinct functions based on tissue distribution and disease context.

Purpose of the Study:

  • To explore the therapeutic potential of P2 purinoceptors and related nucleotides.
  • To identify novel pharmacophores for selective P2 receptor subtype interactions.

Main Methods:

  • Molecular cloning, expression, and functional characterization of P2 purinoceptors.
  • Evaluation of adenosine triphosphate (ATP) as an anticancer agent and anesthetic adjunct.
  • Study of uridine triphosphate (UTP) for cystic fibrosis treatment.
  • Assessment of ARL67085 as a P2T receptor antagonist for antithrombotic therapy.

Related Experiment Videos

  • Utilizing high-throughput screening with chemical and natural product libraries.

    • Main Results:

    • Adenosine triphosphate (ATP) is under investigation for anticancer and anesthetic applications.
    • Uridine triphosphate (UTP) is being studied as a potential treatment for cystic fibrosis.
    • ARL67085 demonstrates potent and selective P2T receptor antagonism, suggesting antithrombotic potential.

    Conclusions:

    • Targeting P2 purinoceptors offers significant therapeutic opportunities.
    • Discovery of novel pharmacophores with selective subtype interactions is crucial for advancing P2 purinoceptor-based therapies.
    • High-throughput screening is essential for identifying new drug leads in this area.