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GPCR annotated library 640

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G protein-coupled receptors (GPCRs), also known as seven-(pass)-transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptor, and G protein-linked receptors (GPLR), constitute a large protein family of receptors that detect molecules outside the cell and activate internal signal transduction pathways and, ultimately, cellular responses.
Coupling with G proteins, they are called seven-transmembrane receptors because they pass through the cell membrane seven times

• G protein-coupled receptors (GPCR) are transmembrane proteins
• Physiologically the GPCR function can be modulated by small molecules via
– Direct receptor binders
– Allosteric binders that cause conformational changes within a receptor
• GPCRs are important drug targets and it is believed that 30-50% of marketed drugs target GPCRs for the
broadest spectrum of clinical areas, such as
– CNS disorders, e.g. antidepressants, anxiety, cognitive impairments
– Inflammatory diseases, e.g. rheumatoid arthritis, pain, edema
– Cardiovascular system, e.g. hypertension, atherosclerosis, arterial stiffness
– Metabolic diseases, e.g. diabetes, obesity, appetite
A unique collection of small molecule compounds with annotated activities for GPCR protein targets
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