Abstract

NOVEL DEVELOPMENT AND ADVANCEMENT APPROACHES IN STRUCTURE-BASED DRUG DISCOVERY ON MEMBRANE INTEGRAL G-PROTEIN COUPLED CLASS- A RECEPTORS: A SYSTEMATIC REVIEW

Chintan Chandrakant Davande, Ankitesh Ramesh Gade, Saklen Dastagir Shaikh, Prasad Ramesh Gaikwad, Shoyal Ajan Shaikh and Vishal Vijay Naik*

ABSTRACT

G-protein coupled receptors are the larger and most important family of integral or transmembrane receptors which is involved in most of the physiological and environmental stimuli. Because of this characteristic the G-protein coupled receptors are the major target for the discovery of new drugs associated with various mammalian diseases. Current pharmaceutical market says over one third of marketed products having prime target is G-protein coupled receptors. Recent studies help to understand the structural biology of G-protein coupled receptors which includes three dimensional structure of GPCR, functions of GPCR, Ligand binding and pharmacological actions. This structural biology contributed in designing a new drug or therapeutic agent. This topic highlights latest or novel advance perspectives in GPCR structure with focus on Membrane receptor - Ligand interaction of class-A G-protein coupled receptors family as well as structural features for their activation, allosterism and biased signaling mechanism. Current methodologies for structure-based drug design in GPCR are also discussed.

Keywords: GPCRs, allosterism, biased ligand, rhodopsin, classification of GPCRs, MARTINI model, SBDD.