Recent Advances on QSAR-Based Profiling of Agonist and Antagonist A(3) Adenosine Receptor Ligands

• Type: Article in International Scientific Journal
• Date: 2013

Authors

Changliang L Deng (Author) Other; Feng Luan (Author) Other; Maykel Cruz Monteagudo (Author) Other; Fernanda Borges (Author) FCUP; Natalia N D S Cordeiro (Author) FCUP

Journal

Title: Current Topics in Medicinal Chemistry

Vol. 13

Pages: 1048-1068

ISSN: 1568-0266

Publisher: Bentham Science

Indexing

ISI Web of Knowledge - 6 Citations

Scopus - 7 Citations

Scientific classification

FOS: Natural sciences > Chemical sciences

CORDIS: Physical sciences > Chemistry > Applied chemistry > Pharmaceutical chemistry

Other information

Authenticus ID: P-005-0X3

DOI: 10.2174/1568026611313090007

Abstract (EN): Adenosine receptors (ARs) are signaling molecules ubiquitously expressed in a wide variety of tissues in the human body. ARs mediate physiological functions by interacting with four subtypes of G-protein-coupled receptors, namely A(1), A(2A), A(2B) and A(3). The A(3) AR, probably the most studied subtype, is also ubiquitously expressed, with high levels in peripheral organs and low levels in the brain. This type of AR is involved in a variety of important pathophysiological processes, ranging from modulation of cerebral and cardiac ischemic damage to regulation of immunosuppression and inflammation. Consequently, the development of potent and selective A(3) AR ligands as promising therapeutic options for a variety of diseases has been a prime subject of medicinal chemistry research for more than two decades. Among the plethora of approaches applied quantitative structure activity relationships (QSAR) stands out for being largely employed due to their potential to increase the efficiency at initial stages of the drug discovery process. So, we provide a review of the main QSAR studies devoted to the design, discovery and development of agonist and antagonist A(3) adenosine receptor ligands. Common pitfalls of these QSAR applications and the current trends in this area are also analyzed.

Language: English

Type (Professor's evaluation): Scientific