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Membrane Steroid Receptor
Membrane steroid receptors (mSRs), also called extranuclear steroid receptors, are a class of cell surface receptors activated by endogenous steroids that mediate rapid, non-genomic signaling via modulation of intracellular signaling cascades. mSRs are another means besides classical nuclear steroid hormone receptors (SHRs) for steroids to mediate their biological effects. SHRs can produce slow genomic responses or rapid, non-genomic responses in the case of mSRs. List of membrane steroid receptors Known groups of mSRs, by ligand, include: * Membrane sex steroid receptors ** Membrane estrogen receptors (mERs) – GPER, ER-X, ERx, Gq-mER; Nav1.2; palmitoylated nuclear receptors ** Membrane progesterone receptors (mPRs) – PAQRs (mPRα, mPRβ, mPRγ, mPRδ, mPRϵ); PGRMC1, PGRMC2; ** Membrane androgen receptors (mARs) – GPRC6A, OXER1, ZIP9; TRPM8; Cav1.2 * Membrane corticosteroid receptors ** Membrane glucocorticoid receptors (mGRs) – caveolin-associated nuclear recep ...
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Cell Surface Receptor
Cell surface receptors (membrane receptors, transmembrane receptors) are receptors that are embedded in the plasma membrane of cells. They act in cell signaling by receiving (binding to) extracellular molecules. They are specialized integral membrane proteins that allow communication between the cell and the extracellular space. The extracellular molecules may be hormones, neurotransmitters, cytokines, growth factors, cell adhesion molecules, or nutrients; they react with the receptor to induce changes in the metabolism and activity of a cell. In the process of signal transduction, ligand binding affects a cascading chemical change through the cell membrane. Structure and mechanism Many membrane receptors are transmembrane proteins. There are various kinds, including glycoproteins and lipoproteins. Hundreds of different receptors are known and many more have yet to be studied. Transmembrane receptors are typically classified based on their tertiary (three-dimensional) stru ...
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MPRβ
Membrane progesterone receptor beta (mPRβ), or progestin and adipoQ receptor 8 (PAQR8), is a protein that in humans is encoded by the ''PAQR8'' gene. See also * Membrane progesterone receptor * Progestin and adipoQ receptor The progestin and adipoQ receptor (PAQR) family is a group of receptors related to but distinct from the G protein-coupled receptor family, which have the similar seven transmembrane structure, but the N-terminal is located on the inner side of the ... References Further reading * * * * * 7TM receptors {{gene-6-stub ...
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Caveolin
In molecular biology, caveolins are a family of integral membrane proteins that are the principal components of caveolae membranes and involved in receptor-independent endocytosis. Caveolins may act as scaffolding proteins within caveolar membranes by compartmentalizing and concentrating signaling molecules. They also induce positive (inward) membrane curvature by way of oligomerization, and hairpin insertion. Various classes of signaling molecules, including G-protein subunits, receptor and non-receptor tyrosine kinases, endothelial nitric oxide synthase (eNOS), and small GTPases, bind Cav-1 through its 'caveolin-scaffolding domain'. The caveolin gene family has three members in vertebrates: CAV1, CAV2, and CAV3, coding for the proteins caveolin-1, caveolin-2, and caveolin-3, respectively. All three members are membrane proteins with similar structure. Caveolin forms oligomers and associates with cholesterol and sphingolipids in certain areas of the cell membrane, leading to t ...
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Membrane Glucocorticoid Receptor
Membrane glucocorticoid receptors (mGRs) are a group of receptors which bind and are activated by glucocorticoids such as cortisol and corticosterone, as well as certain exogenous glucocorticoids such as dexamethasone. Unlike the classical nuclear glucocorticoid receptor (GR), which mediates its effects via genomic mechanisms, mGRs are cell surface receptors which rapidly alter cell signaling via modulation of intracellular signaling cascades. The identities of the mGRs have yet to be fully elucidated, but are thought to include membrane-associated classical GRs as well as yet-to-be-characterized G protein-coupled receptors (GPCRs). Rapid effects of dexamethasone were found not be reversed by the GR antagonist mifepristone, indicating additional receptors besides just the classical GR. mGRs have been implicated in the rapid effects of glucocorticoids in the early central stress response via modulating neuronal activity in the hypothalamus, hippocampus, amygdala, and prefrontal corte ...
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TRPM8
Transient receptor potential cation channel subfamily M (melastatin) member 8 (TRPM8), also known as the cold and menthol receptor 1 (CMR1), is a protein that in humans is encoded by the ''TRPM8'' gene. The TRPM8 channel is the primary molecular transducer of cold somatosensation in humans. In addition, mints can desensitize a region through the activation of TRPM8 receptors (the 'cold'/menthol receptor). Structure The TRPM8 channel is a homotetramer, composed of four identical subunits with a transmembrane domain with six helices (S1–6). The first four, S1–4, act as the voltage sensor and allow binding of menthol, icilin and similar channel agonists. S5 and S6 and a connecting loop, also part of the structure, make up the pore, a non-selective cation channel which consists of a highly conserved hydrophobic region. A range of diverse components are required for the high level of specificity in response to cold and menthol stimuli which eventually lead to ion flow through the ...
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ZIP9
Zinc transporter ZIP9, also known as Zrt- and Irt-like protein 9 (ZIP9) and solute carrier family 39 member 9, is a protein that in humans is encoded by the ''SLC39A9'' gene. This protein is the 9th member out of 14 ZIP family proteins, which is a membrane androgen receptor (mAR) coupled to G proteins, and also classified as a zinc transporter protein. ZIP family proteins transport zinc metal from the extracellular environment into cells through cell membrane. Classification and nomenclature Mammalian cells have two major groups of zinc transporter proteins; the ones that export zinc from the cytoplasm to the extracellular space ( efflux), which are called ZnT (SLC30 family) , and ZIP (SLC39 family) proteins whose functions are in the opposite direction (influx). ZIP family proteins are named as Zrt- and Irt-like proteins because of their similarities to Zrt and Irt proteins which are respectively zinc and iron -regulated transporter proteins in yeast and Arabidopsis that ...
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OXER1
Oxoeicosanoid receptor 1 (OXER1) also known as G-protein coupled receptor 170 (GPR170) is a protein that in humans is encoded by the OXER1 gene located on human chromosome 2p21; it is the principal receptor for the 5-Hydroxyicosatetraenoic acid family of carboxy fatty acid metabolites derived from arachidonic acid. The receptor has also been termed hGPCR48, HGPCR48, and R527 but OXER1 is now its preferred designation. OXER1 is a G protein-coupled receptor (GPCR) that is structurally related to the hydroxy-carboxylic acid (HCA) family of G protein-coupled receptors whose three members are HCA1 (GPR81), HCA2 (Niacin receptor 1), and HCA3 ( Niacin receptor 2); OXER1 has 30.3%, 30.7%, and 30.7% amino acid sequence identity with these GPCRs, respectively. It is also related (30.4% amino acid sequence identity) to the recently defined receptor, GPR31, for the hydroxyl-carboxy fatty acid 12-HETE. Species and tissue distribution Orthologs of OXER1 are found in various mammalian sp ...
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GPRC6A
G protein-coupled receptor family C group 6 member A (GPRC6A) is a protein that in humans is encoded by the ''GPRC6A'' gene. This protein functions as a receptor of L-α-amino acids, cations (e.g., calcium), osteocalcin, and steroids. It is a membrane androgen receptor. Clinical significance GPRC6A has also been linked to prostate cancer progression, and it has been shown to mediate rapid, non-genomic prostate cancer cell responses to testosterone. See also * ZIP9 Zinc transporter ZIP9, also known as Zrt- and Irt-like protein 9 (ZIP9) and solute carrier family 39 member 9, is a protein that in humans is encoded by the ''SLC39A9'' gene. This protein is the 9th member out of 14 ZIP family proteins, which is ... References Further reading * * * * * External links * * G protein-coupled receptors {{transmembranereceptor-stub ...
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Membrane Androgen Receptor
Membrane androgen receptors (mARs) are a group of G protein-coupled receptors (GPCRs) which bind and are activated by testosterone and/or other androgens. Unlike the androgen receptor (AR), a nuclear receptor which mediates its effects via genomic mechanisms, mARs are cell surface receptors which rapidly alter cell signaling via modulation of intracellular signaling cascades. Known or proposed mARs include ZIP9 and GPRC6A. GPRC6A has been found to be involved in testicular function and prostate cancer. mARs have also been found to be expressed in breast cancer cells. Activation of mARs by testosterone has been found to increase skeletal muscle strength, indicating potential anabolic effects. mARs have also been implicated in the antigonadotropic effects of androgens. 3α-Androstanediol, an active metabolite of dihydrotestosterone (DHT) and a weak androgen as well as a neurosteroid via acting as a positive allosteric modulator of the GABAA receptor, rapidly influences sexual r ...
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PGRMC2
Progesterone receptor membrane component 2 (abbreviated PGRMC2) is a protein which is encoded by the ''PGRMC2'' gene. It has been detected in the placenta, liver, and spermatozoa, among other areas. See also * PGRMC * PGRMC1 * Membrane progesterone receptor Membrane progesterone receptors (mPRs) are a group of cell surface receptors and membrane steroid receptors belonging to the progestin and adipoQ receptor (PAQR) family which bind the endogenous progestogen and neurosteroid progesterone, as well as ... References Receptors {{protein-stub ...
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PGRMC1
Progesterone receptor membrane component 1 (abbreviated PGRMC1) is a protein which co-purifies with progesterone binding proteins in the liver and ovary. In humans, the PGRMC1 protein is encoded by the ''PGRMC1'' gene. The sole biochemical function of PGRMC1 is heme-binding. PGRMC1 shares key structural motifs with cytochrome b5. PGRMC1 binds and activates P450 proteins, which are important in drug, hormone and lipid metabolism. PGRMC1 also binds to PAIR-BP1 (plasminogen activator inhibitor RNA-binding protein-1). However, its expression outside of the reproductive tract and in males suggests multiple functions for the protein. These may include binding to Insig (insulin-induced gene), which regulates cholesterol synthesis. Expression PGRMC1 is highly expressed in the liver and kidney in humans with lower expression in the brain, lung, heart, skeletal muscle and pancreas. In rodents, PGRMC1 is found in the liver, lung, kidney and brain. PGRMC1 is over-expressed in breast ...
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