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

• Tipo: Artigo em Revista Científica Internacional
• Data: 2013

Autores

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

Revista

Título: Current Topics in Medicinal Chemistry

Vol. 13

Páginas: 1048-1068

ISSN: 1568-0266

Editora: Bentham Science

Indexação

ISI Web of Knowledge - 6 Citações

Scopus - 7 Citações

Classificação Científica

FOS: Ciências exactas e naturais > Química

CORDIS: Ciências Físicas > Química > Química aplicada > Química farmacêutica

Outras Informações

ID Authenticus: 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.

Idioma: Inglês

Tipo (Avaliação Docente): Científica