Receptor-driven identification of novel human A₃ adenosine receptor antagonists as potential therapeutic agents

Methods Enzymol. 2010:485:225-44. doi: 10.1016/B978-0-12-381296-4.00013-0.

Abstract

The field of therapeutic application of the A₃ adenosine receptor (A₃AR) antagonists represents a rapidly growing and intense area of research in the adenosine field. Even if there are currently no A₃AR antagonists in clinical phases, in light of the plethora of biological effects attributed to A₃ARs, substantial efforts in medicinal chemistry have been directed toward developing antagonists for the A₃AR subtype. In this review, we summarize the more recent and promising evidences of the possible A₃AR application as drug candidates, and the role of the receptor-driven design in their in silico characterization.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenosine A3 Receptor Antagonists / chemistry*
  • Adenosine A3 Receptor Antagonists / pharmacology*
  • Drug Design*
  • Humans
  • Models, Molecular
  • Molecular Structure
  • Mutagenesis
  • Protein Binding
  • Receptor, Adenosine A3 / chemistry
  • Receptor, Adenosine A3 / genetics
  • Receptor, Adenosine A3 / metabolism*

Substances

  • Adenosine A3 Receptor Antagonists
  • Receptor, Adenosine A3