Premium
The A 3 adenosine receptor as multifaceted therapeutic target: pharmacology, medicinal chemistry, and in silico approaches
Author(s) -
Cheong Siew Lee,
Federico Stephanie,
Venkatesan Gopalakrishnan,
Mandel Alexander Laurence,
Shao YiMing,
Moro Stefano,
Spalluto Giampiero,
Pastorin Giorgia
Publication year - 2013
Publication title -
medicinal research reviews
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.868
H-Index - 130
eISSN - 1098-1128
pISSN - 0198-6325
DOI - 10.1002/med.20254
Subject(s) - adenosine receptor , pharmacology , in silico , allosteric regulation , molecular pharmacology , receptor , adenosine , cardioprotection , homology modeling , docking (animal) , drug discovery , computational biology , chemistry , druggability , g protein coupled receptor , medicine , biology , agonist , biochemistry , enzyme , gene , nursing , ischemia
Adenosine is an ubiquitous local modulator that regulates various physiological and pathological functions by stimulating four membrane receptors, namely A 1 , A 2A , A 2B , and A 3 . Among these G protein‐coupled receptors, the A 3 subtype is found mainly in the lung, liver, heart, eyes, and brain in our body. It has been associated with cerebroprotection and cardioprotection, as well as modulation of cellular growth upon its selective activation. On the other hand, its inhibition by selective antagonists has been reported to be potentially useful in the treatment of pathological conditions including glaucoma, inflammatory diseases, and cancer. In this review, we focused on the pharmacology and the therapeutic implications of the human (h)A 3 adenosine receptor (AR), together with an overview on the progress of hA 3 AR agonists, antagonists, allosteric modulators, and radioligands, as well as on the recent advances pertaining to the computational approaches (e.g., quantitative structure–activity relationships, homology modeling, molecular docking, and molecular dynamics simulations) applied to the modeling of hA 3 AR and drug design. © 2011 Wiley Periodicals, Inc. Med Res Rev