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MGlu3 Receptor Antagonists
Metabotropic glutamate receptor 3 (mGluR3) is an inhibitory Gi/G0-coupled G-protein coupled receptor (GPCR) generally localized to presynaptic sites of neurons in classical circuits. However, in higher cortical circuits in primates, mGluR3 are localized post-synaptically, where they strengthen rather than weaken synaptic connectivity. In humans, mGluR3 is encoded by the ''GRM3'' gene. Deficits in mGluR3 signaling have been linked to impaired cognition in humans, and to increased risk of schizophrenia, consistent with their expanding role in cortical evolution. Structure In humans, mGluR3 is encoded by the GRM3 gene on chromosome 7. At least five protein-coding isoforms are predicted based on genomic information. The mGluR3 protein is a seven-pass transmembrane protein. Function L-glutamate is the major excitatory neurotransmitter in the central nervous system and activates both ionotropic and metabotropic glutamate receptors. Glutamatergic neurotransmission is involved i ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
GiG0 Alpha Subunits
Gi protein alpha subunit is a family of heterotrimeric G protein G alpha subunit, alpha subunits. This family is also commonly called the Gi/o (Gi /Go ) family or Gi/o/z/t family to include closely related family members. G alpha subunits may be referred to as Gi alpha, Gαi, or Giα. Family members There are four distinct subtypes of alpha subunits in the Gi/o/z/t alpha subunit family that define four families of heterotrimeric G proteins: * Gi proteins: Gi1α, Gi2α, and Gi3α * Go protein: Goα (in mouse there is alternative splicing to generate Go1α and Go2α) * Gz protein: Gzα * Transducins (Gt proteins): Gt1α, Gt2α, Gt3α Giα proteins Gi1α Gi1α is encoded by the gene GNAI1. Gi2α Gi2α is encoded by the gene GNAI2. Gi3α Gi3α is encoded by the gene GNAI3. Goα protein Go1α is encoded by the gene GNAO1. Gzα protein Gzα is encoded by the gene GNAZ. Transducin proteins Gt1α Transducin/Gt1α is encoded by the gene GNAT1. Gt2α ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Raptin
Raptin is a recently discovered human hormone produced by the hypothalamus during sleep. It is cleaved from reticulocalbin-2 (RCN2). Raptin binds to glutamate metabotropic receptor 3 (GRM3) in hypothalamus and stomach neurons that inhibit appetite and gastric emptying, respectively. A 2024 study reported that it signals satiety to the gut, curbing appetite. Poor/inadequate sleep reduces raptin levels, increasing appetite. Raptin levels measured lower in people with obesity. Raptin levels peak during nighttime sleeping and decline during the day. A 2022 study reported that a lack of sleep increased ghrelin production, increasing appetite, and limits leptin Leptin (from Ancient Greek, Greek λεπτός ''leptos'', "thin" or "light" or "small"), also known as obese protein, is a protein hormone predominantly made by adipocytes (cells of adipose tissue). Its primary role is likely to regulate long ..., which disrupts satiety signals. A genetic study of 2,000 obese individuals ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
PPM1A
Protein phosphatase 1A is an enzyme that in humans is encoded by the ''PPM1A'' gene. The protein encoded by this gene is a member of the PP2C family of Ser/Thr protein phosphatases. PP2C family members are known to be negative regulators of cell stress response pathways. This phosphatase dephosphorylates, and negatively regulates the activities of, MAP kinases and MAP kinase kinases. It has been shown to inhibit the activation of p38 and JNK kinase cascades induced by environmental stresses. This phosphatase can also dephosphorylate cyclin-dependent kinases, and thus may be involved in cell cycle control. Overexpression of this phosphatase is reported to activate the expression of the tumor suppressor gene TP53/p53, which leads to G2/M cell cycle arrest and apoptosis. Three alternatively spliced transcript variants encoding two distinct isoforms have been described. Interactions PPM1A has been shown to interact with Metabotropic glutamate receptor 3 Metabotropic glutamate ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
PICK1
Protein Interacting with C Kinase - 1 is a protein that in humans is encoded by the ''PICK1'' gene. Function The protein encoded by this gene contains a PDZ domain, through which it interacts with protein kinase C, alpha ( PRKCA). This protein may function as an adaptor that binds to and organizes the subcellular localization of a variety of membrane proteins. It has been shown to interact with multiple glutamate receptor subtypes, monoamine plasma membrane transporters, as well as non-voltage gated sodium channels, and may target PRKCA to these membrane proteins and thus regulate their distribution and function. This protein has also been found to act as an anchoring protein that specifically targets PRKCA to mitochondria in a ligand-specific manner. Three transcript variants encoding the same protein have been found for this gene. Interactions PICK1 has been shown to interact with: * ACCN2, * BNC1, * Dopamine transporter, * GRIA2, * GRIA3, * GRIA4, * GRIK1, * ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
GRIP1 (gene)
Glutamate receptor-interacting protein 1 is a protein that in humans is encoded by the ''GRIP1'' gene. Interactions GRIP1 (gene) has been shown to interact with: * GRM3, * GRIA2, * GRIA3 Glutamate receptor 3 is a protein that in humans is encoded by the ''GRIA3'' gene. Function Glutamate receptors are the predominant excitatory neurotransmitter receptors in the mammalian brain and are activated in a variety of normal neurophys ..., * GRIA4, * GRIK2, and * GRIK3. References Further reading * * * * * * * * * * * * * * External links * * {{gene-12-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
LY 2389575
LY or ly may refer to: Government and politics * Libya (ISO 3166-1 country code LY) * Lý dynasty, a Vietnamese dynasty * Labour Youth of Ireland * Legislative Yuan, the unicameral legislature of the Republic of China (Taiwan) Science and technology * .ly, the Top-level domain for Libya * .ly, the default filetype extension of the GNU LilyPond sheet music format * Light-year, the ''distance'' that light travels in one year in a vacuum * Langley (unit), a unit of energy distribution over a given area Other uses * Lý (Vietnamese surname), a Vietnamese surname * Ly the Fairy, a character from ''Rayman 2: The Great Escape'' * '' -ly'', an adjectival and adverbial suffix in English * Hungarian ly, or ''elipszilon'', a digraph in the Hungarian alphabet * El Al (IATA airline designator LY) * LY Corporation , trading as LYC, is a Japanese internet company owned by A Holdings, a joint venture between SoftBank Group of Japan, and Naver Corporation of South Korea, founded in ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Metabotropic Glutamate Receptor 2
Metabotropic glutamate receptor 2 (mGluR2) is a protein that, in humans, is encoded by the ''GRM2'' gene. mGluR2 is a G protein-coupled receptor (GPCR) that couples with the Gi alpha subunit. The receptor functions as an autoreceptor for glutamate, that upon activation, inhibits the emptying of vesicular contents at the presynaptic terminal of glutamatergic neurons. Structure In humans, mGluR2 is encoded by the ''GRM2'' gene on chromosome 3. At least three protein-coding isoforms are predicted based on genomic information, as well as numerous non-coding isoforms. The mGluR2 protein is a seven-pass transmembrane protein. Function In humans, mGluR2 is only expressed in the brain, and not in any other tissue. In the brain, mGluR2 is expressed in neurons as well as astrocytes. Subcellularly, mGluR2 is predominantly positioned at the presynaptic terminal, although it is also expressed at the postsynaptic terminal. The metabotropic glutamate receptors are a family of G protein-co ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
IC50
Half maximal inhibitory concentration (IC50) is a measure of the potency of a substance in inhibiting a specific biological or biochemical function. IC50 is a quantitative measure that indicates how much of a particular inhibitory substance (e.g. drug) is needed to inhibit, ''in vitro'', a given biological process or biological component by 50%. The biological component could be an enzyme, cell, cell receptor or microbe. IC50 values are typically expressed as molar concentration. IC50 is commonly used as a measure of antagonist drug potency in pharmacological research. IC50 is comparable to other measures of potency, such as EC50 for excitatory drugs. EC50 represents the dose or plasma concentration required for obtaining 50% of a maximum effect ''in vivo''. IC50 can be determined with functional assays or with competition binding assays. Sometimes, IC50 values are converted to the pIC50 scale. :\ce = -\log_ \ce Due to the minus sign, higher values of pIC50 indicate ex ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Allosteric Modulator
In pharmacology and biochemistry, allosteric modulators are a group of substances that bind to a receptor to change that receptor's response to stimuli. Some of them, like benzodiazepines or alcohol, function as psychoactive drugs. The site that an allosteric modulator binds to (i.e., an ''allosteric site'') is not the same one to which an endogenous agonist of the receptor would bind (i.e., an ''orthosteric site''). Modulators and agonists can both be called receptor ligands. Allosteric modulators can be 1 of 3 types either: positive, negative or neutral. Positive types increase the response of the receptor by increasing the probability that an agonist will bind to a receptor (i.e. affinity), increasing its ability to activate the receptor (i.e. efficacy), or both. Negative types decrease the agonist affinity and/or efficacy. Neutral types don't affect agonist activity but can stop other modulators from binding to an allosteric site. Some modulators also work as allosteric agonist ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
ML337
ML337 is an experimental drug that acts as a negative allosteric modulator selective for the glutamate Glutamic acid (symbol Glu or E; known as glutamate in its anionic form) is an α-amino acid that is used by almost all living beings in the biosynthesis of proteins. It is a Essential amino acid, non-essential nutrient for humans, meaning that ... receptor mGluR3. It has only moderate potency with an IC50 of 450 nM, but is highly selective over the closely related subtype mGluR2 with no effect even at 30,000 nM, and so has been used to study the effects of mGluR3 in isolation, which had previously been difficult to separate from mGluR2 mediated effects. References Experimental drugs Alcohols Alkynes Benzamides Benzene derivatives Fluorobenzenes Methoxy compounds Piperidines {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
