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TRPV4
Transient receptor potential cation channel subfamily V member 4 is an ion channel protein that in humans is encoded by the ''TRPV4'' gene. The ''TRPV4'' gene encodes TRPV4, initially named "vanilloid-receptor related osmotically activated channel" (VR-OAC) and "OSM9-like transient receptor potential channel, member 4 (OTRPC4)", a member of the vanilloid subfamily in the transient receptor potential (TRP) superfamily of ion channels. The encoded protein is a Ca2+-permeable, nonselective cation channel that has been found involved in multiple physiologic functions, dysfunctions and also disease. It functions in the regulation of systemic osmotic pressure by the brain, in vascular function, in liver, intestinal, renal and bladder function, in skin barrier function and response of the skin to ultraviolet-B radiation, in growth and structural integrity of the skeleton, in function of joints, in airway- and lung function, in retinal and inner ear function, and in pain. The channel is ac ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Congenital Distal Spinal Muscular Atrophy
Congenital distal spinal muscular atrophy is a Heredity, hereditary condition characterized by muscle wasting (atrophy), particularly of Anatomical terms of location#Proximal and distal, distal muscles in legs and hands, and by early-onset contractures (permanent shortening of a muscle or joint) of the hip, knee, and ankle. Affected individuals often have shorter lower limbs relative to the trunk and upper limbs. The condition is a result of a loss of Anterior horn of spinal cord, anterior horn cells localized to lumbar and Neck, cervical regions of the spinal cord early in infancy, which in turn is caused by a mutation of the ''TRPV4'' gene. The disorder is inherited in an autosomal dominant manner. Arm muscle and function, as well as cardiac and respiratory functions are typically well preserved. Signs and symptoms The presentation is as follows: * Neurogenic muscle weakness * Atrophy (of lower and upper limbs) * Club foot * Arthrogryposis * Scoliosis * Platyspondyly * Pes ca ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
HC-067047
HC-067047 is a drug which acts as a potent and selective antagonist for the TRPV4 receptor. It has been used to investigate the role of TRPV4 receptors in a number of areas, such as regulation of blood pressure, bladder function and some forms of pain, as well as neurological functions. See also * JWH-147 * RN-9893 * SET2 * ZINC17988990 ZINC17988990 is a drug which acts as a potent and selective inhibitor for the TRPV5 calcium channel, with an IC50 of 177 nM and high selectivity for TRPV5 over TRPV6 and the other subtypes of TRPV. It is the first selective inhibitor to be deve ... References Pyrroles {{pharm-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Transient Receptor Potential
Transient receptor potential channels (TRP channels) are a group of ion channels located mostly on the plasma membrane of numerous animal cell types. Most of these are grouped into two broad groups: Group 1 includes TRPC ( "C" for canonical), TRPV ("V" for vanilloid), TRPVL ("VL" for vanilloid-like), TRPM ("M" for melastatin), TRPS ("S" for soromelastatin), TRPN ("N" for no mechanoreceptor potential C), and TRPA ("A" for ankyrin). Group 2 consists of TRPP ("P" for polycystic) and TRPML ("ML" for mucolipin). Other less-well categorized TRP channels exist, including yeast channels and a number of Group 1 and Group 2 channels present in non-animals. Many of these channels mediate a variety of sensations such as pain, temperature, different kinds of tastes, pressure, and vision. In the body, some TRP channels are thought to behave like microscopic thermometers and used in animals to sense hot or cold. Some TRP channels are activated by molecules found in spices like garlic (allicin) ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
TRPV
TRPV is a family of transient receptor potential cation channels (TRP channels) in animals. All TRPVs are highly calcium selective. TRP channels are a large group of ion channels consisting of six protein families, located mostly on the plasma membrane of numerous human and animal cell types, and in some fungi. TRP channels were initially discovered in the ''trp'' mutant strain of the fruit fly ''Drosophila'' that displayed transient elevation of potential in response to light stimuli, and were therefore named "transient receptor potential" channels. The name now refers only to a family of proteins with similar structure and function, not to the mechanism of their activation. Later, TRP channels were found in vertebrates where they are ubiquitously expressed in many cell types and tissues. There are about 28 TRP channels that share some structural similarity to each other. These are grouped into two broad groups: group 1 includes TRPC ( "C" for canonical), TRPV ("V" for vanill ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
GSK1016790A
GSK1016790A (aka GSK101) is a drug developed by GlaxoSmithKline which acts as a potent and selective agonist for the TRPV4 receptor. It has been used to study the role of TRPV4 receptors in the function of smooth muscle tissue, particularly that lining blood vessels, lymphatic system, and the bladder The urinary bladder, or simply bladder, is a hollow organ in humans and other vertebrates that stores urine from the kidneys before disposal by urination. In humans the bladder is a distensible organ that sits on the pelvic floor. Urine enters .... References Piperazines {{pharm-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Specialized Proresolving Mediators
Specialized pro-resolving mediators (SPM, also termed specialized proresolving mediators) are a large and growing class of cell signaling molecules formed in cells by the metabolism of polyunsaturated fatty acids (PUFA) by one or a combination of lipoxygenase, cyclooxygenase, and cytochrome P450 monooxygenase enzymes. Pre-clinical studies, primarily in animal models and human tissues, implicate SPM in orchestrating the resolution of inflammation. Prominent members include the resolvins and Protectin D1, protectins. SPM join the long list of other physiological agents which tend to limit inflammation (see ) including glucocorticoids, interleukin 10 (an anti-inflammatory cytokine), interleukin 1 receptor antagonist (an inhibitor of the action of pro-inflammatory cytokine, interleukin 1), annexin A1 (an inhibitor of formation of pro-inflammatory metabolites of polyunsaturated fatty acids), and the gaseous resolvins, carbon monoxide (see ), nitric oxide (see ), and hydrogen sulfide (se ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
MAP7
Ensconsin is a protein that in humans is encoded by the ''MAP7'' gene. Function The product of this gene is a microtubule-associated protein that is predominantly expressed in cells of epithelial origin. Microtubule-associated proteins are thought to be involved in microtubule dynamics, which is essential for cell polarization and differentiation. This protein has been shown to be able to stabilize microtubules, and may serve to modulate microtubule functions. Studies of the related mouse protein also suggested an essential role in microtubule function required for spermatogenesis. Interactions MAP7 has been shown to interact with TRPV4 Transient receptor potential cation channel subfamily V member 4 is an ion channel protein that in humans is encoded by the ''TRPV4'' gene. The ''TRPV4'' gene encodes TRPV4, initially named "vanilloid-receptor related osmotically activated channe .... References Further reading * * * * * * * * * * {{gene-6-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ruthenium Red
The inorganic dye ammoniated ruthenium oxychloride, also known as ruthenium red, is used in histology to stain aldehyde fixed mucopolysaccharides. Ruthenium red (RR) has also been used as a pharmacological tool to study specific cellular mechanisms. Selectivity is a significant issue in such studies as RR is known to interact with many proteins. These include mammalian ion channels (CatSper1, TASK, RyR1, RyR2, RyR3, TRPM6, TRPM8, TRPV1, TRPV2, TRPV3, TRPV4, TRPV5, TRPV6, TRPA1, mCa1, mCa2, CALHM1) TRPP3, a plant ion channel, Ca2+-ATPase, mitochondrial Ca2+ uniporter, tubulin, myosin light-chain phosphatase, and Ca2+ binding proteins such as calmodulin. Ruthenium red displays nanomolar potency against several of its binding partners (e.g. TRPV4, ryanodine receptors,...). For example, it is a potent inhibitor of intracellular calcium release by ryanodine receptors (Kd ~20 nM). As a TRPA1 blocker, it assists in reducing the airway inflammation caused by pepper spray. RR has been ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
RN-9893
RN-9893 is a drug which acts as a potent and selective blocker of the TRPV4 ion channel. It has been used to investigate the role of TRPV4 channels in the function of heart valves. See also * HC-067047 * SET2 SET2 is a drug which acts as a selective antagonist for the TRPV2 receptor. It is moderately potent with an IC50 of 460nM, but is highly selective for TRPV2 over the other subtypes of TRPV, and is the first such compound to be developed. A role ... References Piperazines Nitro compounds Sulfonamides Amides Isopropyl compounds Trifluoromethyl compounds {{pharm-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
CMKLR1
Chemokine like receptor 1 also known as ChemR23 (Chemerin Receptor 23) is a protein that in humans is encoded by the ''CMKLR1'' gene. Chemokine receptor-like 1 is a G protein-coupled receptor for the chemoattractant adipokine chemerin and the omega-3 fatty acid eicosapentaenoic acid-derived specialized pro-resolving molecule, resolvin E1 (see Specialized proresolving mediators#EPA-derived resolvins (i.e. RvE)). The murine receptor that shares almost 80% homology with the human receptor, is called Dez. Tissue distribution CMKLR1 shows wide RNA expression profile but is notably high in plasmacytoid dendritic cells, macrophages, cardiomyocytes, adipocytes and endothelial cells. Function Activating CMKLR1 by an agonist mobilizes intracellular calcium and causes the activation of several other signaling cascades like the ERK1 and NF-κB. Initial studies of CMKLR1 suggested that it might have a role in the inflammatory pathways. Its cognate ligand, chemerin was found in joint a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Down-regulate
In the biology, biological context of organisms' regulation of gene expression, production of gene products, downregulation is the process by which a cell (biology), cell decreases the quantity of a cellular component, such as RNA or protein, in response to an external stimulus. The complementary process that involves increases of such components is called upregulation. An example of downregulation is the cellular decrease in the expression of a specific Receptor (biochemistry), receptor in response to its increased activation by a molecule, such as a hormone or neurotransmitter, which reduces the cell's sensitivity to the molecule. This is an example of a locally acting (negative feedback) mechanism. An example of upregulation is the response of liver cells exposed to such xenobiotic molecules as Polychlorinated dibenzodioxins, dioxin. In this situation, the cells increase their production of cytochrome P450, cytochrome P450 enzymes, which in turn increases degradation of these d ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
