Until recently, the only high-resolution GPCR crystal structures were of bovine rhodopsin. Structural analysis of GPCRs for hormones and neurotransmitters has been hindered by their low natural abundance, their inherent structural flexibility, and the instability of these proteins in detergent solutions. Biochemical and biophysical studies provide evidence that the flexible and dynamic character of GPCRs is in part responsible for the failure to generate diffraction quality crystals. The Kobilka Lab used two approaches to overcome this structural flexibility and obtained crystal structures of the human β2 adrenergic receptor (β2AR), a receptor for adrenaline and noradrenaline that plays important roles in cardiovascular and pulmonary physiology. The successful crystallization of the β2AR paves with way for obtaining structures of other GPCRs.
ConfometRx has obtained the exclusive licensing rights for GPCR-T4Lysozyme fusion technology from Stanford University, and will provide this technology and its expertise in GPCR expression, structural engineering, biochemistry and crystallography on a contract/collaborative basis to partners in the biotechnology and pharmaceutical industries.
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