title: New tools for G-protein coupled receptor (GPCR) drug discovery: combination of baculoviral expression system and solid state NMR.
abstract: Biotechnology using molecular biology, biochemistry, biophysics, and computational approaches provides an alternative approach for classical pharmacological screening to look at ligand-receptor interactions and receptor specificity, which should support the design of selective drugs based on detailed structural principles. This review addresses specific approaches to study function, structure and relevance of a major pharmaceutical target, namely the G-Protein Coupled Receptors (GPCRs). The main aim of this review has been to exploit and combine GPCR over-expression in a baculoviral expression system with solid-state MAS NMR (ssNMR) approaches for the elucidation of electronic structures of the coordinating ligands/drugs and their modes of interactions with the GPCRs. This review summarizes the approaches, possible future experiments and developments using the above combination of tools for GPCR drug discovery.
authors.affiliation: Leiden Institute of Chemistry, Leiden University, Einsteinweg 55, P.O. Box 9502, 2300 RALeiden, The Netherlands. ratnala@stanford.edu
authors.forename: Venkata R P
authors.initials: VR
authors.lastname: Ratnala
mesh_terms: D016367:Baculoviridae / Q000378:metabolism; D015195:Drug Design; D006801:Humans; D019906:Nuclear Magnetic Resonance, Biomolecular / Q000379:methods*; D043562:Receptors, G-Protein-Coupled / Q000187:drug effects / Q000378:metabolism*
chemical_list: D043562:Receptors, G-Protein-Coupled