Preparation of purified GPCRs for structural studies.
Since the publication of the first X-ray structure of a GPCR (G-protein couple receptor) in 2000, the rate at which subsequent ones have appeared has steadily increased. This has required the development of new methodology to overcome the challenges presented by instability of isolated GPCRs, combined with a systematic optimization of existing approaches for protein expression, purification and crystallization. In addition, quality control measures that are predictive of successful outcomes have been identified. Repeated attempts at solving the structures of GPCRs have highlighted experimental approaches that are most likely to lead to success, and have allowed definition of a first-pass protocol for new receptors.
Heptares Therapeutics Ltd, Biopark, Broadwater Road, Welwyn Garden City, Hertfordshire AL7 3AX, UK.
Robert M
RM
Cooke
Markus
M
Koglin
James C
JC
Errey
Fiona H
FH
Marshall
D018360:Crystallography, X-Ray; D055808:Drug Discovery; D004591:Electrophoresis, Polyacrylamide Gel; D011487:Protein Conformation; D043562:Receptors, G-Protein-Coupled / Q000737:chemistry / Q000302:isolation & purification*
D043562:Receptors, G-Protein-Coupled