CINXE.COM

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receptors (7-TM receptors)</strong>, are integral membrane proteins that contain seven membrane-spanning helices. As the name suggests they are coupled to <a href='/pharmacology/heterotrimeric-g-protein-gtpases'>heterotrimeric G proteins</a> on the intracellular side of the membrane. Upon ligand binding, the GPCR undergoes a conformational change which is transmitted to the G protein causing activation. Further signal transduction depends on the type of G protein.</p> <div class="pharm_sub_cats"><h3>Products for GPCRs / 7-TM Receptors</h3><ul class="tile_column_1"><li><a href="/pharmacology/5-ht-receptors" title="Browse products for 5-HT Receptors">5-HT Receptors</a></li><li><a href="/pharmacology/acetylcholine-muscarinic-receptors" title="Browse products for Acetylcholine Muscarinic Receptors">Acetylcholine Muscarinic Receptors</a></li><li><a href="/pharmacology/adenosine-receptors" title="Browse products for Adenosine Receptors">Adenosine Receptors</a></li><li><a href="/pharmacology/adrenergic-receptors" title="Browse products for Adrenergic Receptors">Adrenergic Receptors</a></li><li><a href="/pharmacology/calcium-sensing-receptor" title="Browse products for Calcium-Sensing Receptor">Calcium-Sensing Receptor</a></li><li><a href="/pharmacology/cannabinoid-receptors" title="Browse products for Cannabinoid Receptors">Cannabinoid Receptors</a></li><li><a href="/pharmacology/chemokine-receptors" title="Browse products for Chemokine Receptors">Chemokine Receptors</a></li><li><a href="/pharmacology/dopamine-receptors" title="Browse products for Dopamine Receptors">Dopamine Receptors</a></li><li><a href="/pharmacology/estrogen-gper-receptors" title="Browse products for Estrogen (GPER) Receptors">Estrogen (GPER) Receptors</a></li><li><a href="/pharmacology/free-fatty-acid-receptors" title="Browse products for Free Fatty Acid Receptors">Free Fatty Acid Receptors</a></li><li><a href="/pharmacology/gabab-receptors" title="Browse products for GABAB Receptors">GABA<sub>B</sub> Receptors</a></li><li><a href="/pharmacology/glutamate-metabotropic-receptors" title="Browse products for Glutamate (Metabotropic) Receptors">Glutamate (Metabotropic) Receptors</a></li><li><a href="/pharmacology/gpba-receptors" title="Browse products for GPBA Receptors">GPBA Receptors</a></li><li><a href="/pharmacology/gpr119" title="Browse products for GPR119">GPR119</a></li><li><a href="/pharmacology/gpr35" title="Browse products for GPR35">GPR35</a></li></ul><ul class="tile_column_2"><li><a href="/pharmacology/gpr55" title="Browse products for GPR55">GPR55</a></li><li><a href="/pharmacology/histamine-receptors" title="Browse products for Histamine Receptors">Histamine Receptors</a></li><li><a href="/pharmacology/hydroxycarboxylic-acid-receptors" title="Browse products for Hydroxycarboxylic Acid Receptors">Hydroxycarboxylic Acid Receptors</a></li><li><a href="/pharmacology/leukotriene-and-related-receptors" title="Browse products for Leukotriene and Related Receptors">Leukotriene and Related Receptors</a></li><li><a href="/pharmacology/lysophosphatidic-acid-receptors" title="Browse products for Lysophosphatidic Acid Receptors">Lysophosphatidic Acid Receptors</a></li><li><a href="/pharmacology/melatonin-receptors" title="Browse products for Melatonin Receptors">Melatonin Receptors</a></li><li><a href="/pharmacology/opioid-receptors" title="Browse products for Opioid Receptors">Opioid Receptors</a></li><li><a href="/pharmacology/orphan-7-tm-receptors" title="Browse products for Orphan 7-TM Receptors">Orphan 7-TM Receptors</a></li><li><a href="/pharmacology/peptide-receptors" title="Browse products for Peptide Receptors">Peptide Receptors</a></li><li><a href="/pharmacology/platelet-activating-factor-paf-receptors" title="Browse products for Platelet-Activating Factor (PAF) Receptors">Platelet-Activating Factor (PAF) Receptors</a></li><li><a href="/pharmacology/prostanoid-receptors" title="Browse products for Prostanoid Receptors">Prostanoid Receptors</a></li><li><a href="/pharmacology/purinergic-p2y-receptors" title="Browse products for Purinergic (P2Y) Receptors">Purinergic (P2Y) Receptors</a></li><li><a href="/pharmacology/smoothened-receptors" title="Browse products for Smoothened Receptors">Smoothened Receptors</a></li><li><a href="/pharmacology/sphingosine-1-phosphate-receptors" title="Browse products for Sphingosine-1-Phosphate Receptors">Sphingosine-1-Phosphate Receptors</a></li><li><a href="/pharmacology/trace-amine-1-receptor" title="Browse products for Trace Amine 1 Receptor">Trace Amine 1 Receptor</a></li></ul></div> <div class="pharm_rel_cats"><h3>Related Targets</h3><ul class="tile_column_1"><li><a href="/product-type/fluorescent-receptor-probes" title="Browse products for Fluorescent Receptor Probes">Fluorescent Receptor Probes</a></li></ul><ul class="tile_column_2"></ul></div> <div class="pharm_long_desc"><h3>Classification</h3> <p>GPCRs or 7-TM receptors are activated by a wide variety of ligands including light, olfactory stimulants, peptides, hormones and neurotransmitters. They are grouped into 6 classes based on sequence homology and functional similarity:</p> <ul> <li>Class A (or 1) (Rhodopsin-like)</li> <li>Class B (or 2) (Secretin receptor family)</li> <li>Class C (or 3) (Metabotropic glutamate/pheromone)</li> <li>Class D (or 4) (Fungal mating pheromone receptors)</li> <li>Class E (or 5) (Cyclic AMP receptors)</li> <li>Class F (or 6) (Frizzled/Smoothened)</li> </ul> <h3>Physiology and Disease</h3> <p>The human genome encodes roughly 350 GPCRs / 7-TM receptors, of which approximately 150 of these have an unknown function. They comprise the largest family of receptors in the human genome and because of their large number, widespread distribution and important roles in cell physiology and biochemistry, they play an important role in medicine.</p> <p>Diseases involving mutations of GPCRs / 7-TM receptors are relatively rare, however disorders that involve antibodies directed against GPCRs are more common. Typically disease can be caused by:</p> <ul> <li>Non-functional receptors (GHRH and familial growth hormone deficiency)</li> <li>Constitutive activation (Rhodopsin and retinitis pigmentosa)</li> <li>Changes in ligand binding specificity (Thyroid-stimulating hormone receptor and hyperthyroidism of pregnancy)</li> <li>Improper receptor processing (vasopressin receptor and diabetes insipidus)</li> <li>Antibodies directed against the receptors (Thyroid stimulation hormone receptor and Graves disease)</li> <li>Constitutively active or inactive G proteins</li> </ul> <p>GPCRS / 7-TM receptors are the target of around half of all modern medicinal drugs. Their expression on the cell surface makes them readily accessible to hydrophilic drugs and their non-uniform expression provides selectivity in activating or blocking physiological events. Agonists and antagonists of GPCRs / 7-TM receptors are used in the treatment of disease in every organ system.</p></div> </div> <div id="sidebar" class="col-xs-12 col-sm-4 col-md-3 col-lg-3 col-xl-3"> <div class="resources_sidebar_container"> <div class="fp_four_box"> <div class="fp_box_wrapper"><h3>Featured New Products</h3> <div class="fp_featured_product"><a href="/products/vu-0542270_8151">8151 | VU 0542270</a><br /> Selective inhibitor of K<sub>ir</sub>6.1 K<sub>ATP</sub> channels</div> <div class="fp_featured_product"><a href="/products/rna-imaging-probe-1c_8813">8813 | RNA Imaging Probe 1c</a><br /> Fluorogenic RNA imaging probe</div> <div class="fp_featured_product"><a href="/products/lsn-3318839_7959">7959 | LSN 3318839</a><br /> Glucagon-like peptide-1 receptor <br />(GLP1-R) positive allosteric modulator</div> <div class="fp_featured_product"><a href="/products/chir-99021-in-solution_8170">8170 | CHIR 99021 in solution</a><br /> Sterile-filtered 10 mM solution of CHIR 99021 pre-dissolved in DMSO</div> <div class="fp_featured_product"><a href="/products/bi-3231_8039">8039 | BI 3231</a><br /> Potent and selective hydroxysteroid 17尾 dehydrogenase 13 (HSD17B13) inhibitor</div> </div> </div> </div> <div class="distributor_region"></div> <div class="widget"> <div class="widget_title">Literature in this Area</div> <div class="widget_content carousel slide" id="ds_literature_scroller" data-ride="carousel" data-interval="8000">  <div class="carousel-inner"><div class="item active"><div class="highlight">Allosteric GPCR Pharmacology Poster</div><h5>Written by Arthur Christopoulos, David Thal, Denise Wootten and Patrick M. Sexton</h5> <a href="/literature/life-science-posters/allosteric-gpcr-pharmacology"><img loading="lazy" src="https://resources.tocris.com/images/literature/posters/regular/636206.jpg" alt="Allosteric GPCR Pharmacology Poster"></a><p class="small">Our Allosteric GPCR Pharmacology Poster discusses key facets of GPCR allostery and highlights therapeutic applications of allosteric modulators.</p><a class="btn btn-quinary" href="/literature/literature-request/636206" rel="nofollow" title="Request copy of the Allosteric GPCR Pharmacology Poster">Request copy</a><a class="btn btn-quinary pdf-download" href="https://resources.tocris.com/pdfs/literature/posters/allosteric-gpcr-pharmacology-poster-2019.pdf" download="https://resources.tocris.com/pdfs/literature/posters/allosteric-gpcr-pharmacology-poster-2019.pdf" rel="nofollow" target="_blank" title="Download PDF of the Allosteric GPCR Pharmacology Poster" data-title="Allosteric GPCR Pharmacology Poster">Download PDF<div class="lit_pdf"></div></a></div><div class="item"><div class="highlight">GPCR Efficacy and Biased Agonism Life Science Poster</div><h5>Written by Patrick M. Sexton, Arthur Christopoulos and Denise Wootten</h5> <a href="/literature/life-science-posters/gpcr-efficacy-and-biased-agonism"><img loading="lazy" src="https://resources.tocris.com/images/literature/posters/regular/629782.jpg" alt="GPCR Efficacy and Biased Agonism Poster"></a><p class="small">Our GPCR Efficacy and Biased Agonism discusses cutting edge GPCR signaling pharmacology and highlights therapeutic applications of biased agonism</p><a class="btn btn-quinary" href="/literature/literature-request/629782" rel="nofollow" title="Request copy of the GPCR Efficacy and Biased Agonism Poster">Request copy</a><a class="btn btn-quinary pdf-download" href="https://resources.tocris.com/pdfs/literature/posters/gpcr-efficacy-biased-agonism-poster-v1-2019.pdf" download="https://resources.tocris.com/pdfs/literature/posters/gpcr-efficacy-biased-agonism-poster-v1-2019.pdf" rel="nofollow" target="_blank" title="Download PDF of the GPCR Efficacy and Biased Agonism Poster" data-title="GPCR Efficacy 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