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GPCRs: Exploring New Paradigms

Date Added: February 08, 2012 03:12:05 AM
Author: Stephen Jones
Category: Health

As one of the largest and most diverse protein families in nature, the G-protein coupled receptor (GPCR) superfamily play important roles in a variety of biological and pathological processes such as development and proliferation, neuromodulation, angiogenesis, metabolic disorders, inflammation, and viral infection. Not surprisingly, it is one of the most targeted protein families in pharmaceutical research today (Schlyer 2006). All members of this superfamily share a similar seven transmembrane domain, but are grouped on the basis of shared sequence motifs into the following broad classes: Class A Rhodopsin-like Class B Secretin-like Class C Metabotropic glutamate/pheromone Class D Fungal pheromone Class E cAMP receptors Frizzled/Smoothened Vomeronasal receptors Putative/unclassified The pharmaceutical industry has focused on development of modulators to this protein family, but GPCRs also represent an attractive target as biomarkers. Recent studies have implicated endothelin receptors, chemokine receptors and lysophosphatidic acid receptors in tumorgenesis and metastasis, and a recent in silico analysis found a number of GPCRs that were up-regulated in various cancers which suggests not only targets of therapeutic value, but of diagnostic and prognostic value as well. A summary of these up-regulated receptors is below. Lung cancer Edg2, P2Y purinoceptor 6, PAR-2, PAR-3, GPR68 Breast cancer CCR1, CXCR-4, PAR-2 Prostate cancer Beta 2 adrenergic receptor, CXCR-3, CXCR-4, GPR68 Melanoma Edg6, PAR-2, mGluR1 Gastric cancer CXCR-4, P2Y purinoceptor 5 Lymphoma Beta 2 adrenergic receptor, Edg1, CCR7 While research continues, it is evident that GPCRs are critical in countless biological functions--and disfunctions. While the emphasis is on their role in drug development, it is becoming increasingly clear that G-protein coupled receptors will play a critical role as indicators of disease with diagnostic and prognostic potential. IMGENEX carries over 900 IHC, WB, and flow validated GPCR antibodies. View our complete antibody list grouped by class and family. Also see our complete list of Tissue Microarray slides--perfect for GPCR localization studies. IMGENEX India Pvt Ltd. the only biotech company in Orissa and one of its kinds in Eastern India. IMGENEX India started in Oct as an outsourcing branch of IMGENEX Corporation, San Diego, USA. Find out more information about Drug Discovery.
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