Antibodies to
G-Protein Coupled Receptors

G-protein coupled receptors (GPCRs) are cell surface receptors that transduce their ligand binding signal through ligand-induced association with a guanosine triphosphate-binding protein (G-protein). There are more GPCRs than any other receptors and they underly fundamental biological processes, such as vision, olfaction, pain, vascular tone, and cell migration. GPCRs are of outmost pharmacological importance and represent by far the largest class of targets for modern drugs. Ligands for GPCRs include small organic molecules, peptides and proteins. Chemokine receptors are a subclass of GPCRs that bind small chemotactic cytokines (chemokines) and are centrally involved in important pathologies such as cardiovascular disease, asthma, chronic inflammation, and AIDS.

Useful antibodies to GPCRs have been notoriously difficult to generate, because they cannot be obtained as purified antigens and recombinant high-level expression of GPCRs in host cells has been difficult. However, recent advances such as overexpression of GPCRs in optimized cell lines treated with sodium butyrate led to successful generation of a number of monoclonal antibodies that recognize GPCRs in their natural context and can block their function. Such antibodies are being used for proof-of-concept studies in animal models, and a subset of these has been advanced towards clinical evaluation in patients.

Antibody Solutions
Tel: 888-843-1069 Fax: 650-938-4390 E-mail: