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GPR35
G protein-coupled receptor 35 also known as GPR35 is a G protein-coupled receptor which in humans is encoded by the ''GPR35'' gene. Heightened expression of GPR35 is found in immune and gastrointestinal tissues, including the crypts of Lieberkühn. Ligands Endogenous ligands Although GPR35 is still considered an orphan receptor, there have been attempts to deorphanize it by identifying endogenous molecules that can activate the receptor. All of the currently proposed ligands are either unselective towards GPR35, or they lack high potency, a characteristic feature of natural ligands. The following list includes the most prominent examples: * kynurenic acidfree fulltext * LPA species [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Zaprinast
Zaprinast was an unsuccessful clinical drug candidate that was a precursor to the chemically related PDE5 inhibitors, such as sildenafil (Viagra), which successfully reached the market. It is a phosphodiesterase inhibitor, selective for the subtypes PDE5, PDE6, PDE9 and PDE11. IC50 values are 0.76, 0.15, 29.0, and 12.0 ''μ''M, respectively. Zaprinast inhibits the growth of asexual blood-stage malaria parasites ( ''P. falciparum'') ''in vitro'' with an ED50 value of 35 ''μ''M, and inhibits PfPDE1, a '' P. falciparum'' cGMP-specific phosphodiesterase, with an IC50 value of 3.8 ''μ''M. Zaprinast has also been shown to activate the orphan G-protein coupled receptor known as GPR35, both in rats and humans, and to inhibit the mitochondrial pyruvate Pyruvic acid (CH3COCOOH) is the simplest of the alpha-keto acids, with a carboxylic acid and a ketone functional group. Pyruvate, the conjugate base, CH3COCOO−, is an intermediate in several metabolic pathways throughout the cell ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Zaprinast
Zaprinast was an unsuccessful clinical drug candidate that was a precursor to the chemically related PDE5 inhibitors, such as sildenafil (Viagra), which successfully reached the market. It is a phosphodiesterase inhibitor, selective for the subtypes PDE5, PDE6, PDE9 and PDE11. IC50 values are 0.76, 0.15, 29.0, and 12.0 ''μ''M, respectively. Zaprinast inhibits the growth of asexual blood-stage malaria parasites ( ''P. falciparum'') ''in vitro'' with an ED50 value of 35 ''μ''M, and inhibits PfPDE1, a '' P. falciparum'' cGMP-specific phosphodiesterase, with an IC50 value of 3.8 ''μ''M. Zaprinast has also been shown to activate the orphan G-protein coupled receptor known as GPR35, both in rats and humans, and to inhibit the mitochondrial pyruvate Pyruvic acid (CH3COCOOH) is the simplest of the alpha-keto acids, with a carboxylic acid and a ketone functional group. Pyruvate, the conjugate base, CH3COCOO−, is an intermediate in several metabolic pathways throughout the cell ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Kynurenic Acid
Kynurenic acid (KYNA or KYN) is a product of the normal metabolism of amino acid -tryptophan. It has been shown that kynurenic acid possesses neuroactive activity. It acts as an antiexcitotoxic and anticonvulsant, most likely through acting as an antagonist at excitatory amino acid receptors. Because of this activity, it may influence important neurophysiological and neuropathological processes. As a result, kynurenic acid has been considered for use in therapy in certain neurobiological disorders. Conversely, increased levels of kynurenic acid have also been linked to certain pathological conditions. Kynurenic acid was discovered in 1853 by the German chemist Justus von Liebig in dog urine, which it was apparently named after.Liebig, J., Uber Kynurensäure, ''Justus Liebigs Ann. Chem.'', 86: 125-126, 1853. It is formed from -kynurenine in a reaction catalyzed by the enzyme kynurenine—oxoglutarate transaminase. Mechanism of action KYNA has been proposed to act on five targe ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pamoic Acid
Pamoic acid, also called embonic acid, is a 2-Naphthoic acid derivative. Salts and esters of pamoic acid are known as pamoates or embonates. It can be prepared by the reaction of 3-hydroxy-2-naphthoic acid with formaldehyde. In pharmacology, the salt form of pamoic acid (pamoate ion) can be used as a counterion of a drug compound to affect the dissolution rate of the drug. The presence of multiple oxygen atoms enables significant hydrogen bonding to occur. Hydrogen bonds facilitate the dissolution of compounds in water. Pharmaceutical drugs formulated this way include cycloguanil pamoate, hydroxyzine pamoate, imipramine pamoate, olanzapine pamoate hydrate, oxantel pamoate, pyrantel pamoate, and pyrvinium pamoate. Pamoic acid has agonist activity for the orphan G protein-coupled receptor GPR35 by which it activates ERK and beta-arrestin2, and causes antinociceptive Nociception (also nocioception, from Latin ''nocere'' 'to harm or hurt') is the Somatosensory system, sen ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
2q37 Monosomy
2q37 monosomy is a rare genetic disorder caused by a deletion of a segment at the end of chromosome 2. Signs and symptoms Almost all people with this syndrome have some degree of intellectual disability and facial dysmorphism (round face, deep-set eyes, thin upper lip). Behavioural problems are common. Brachymetaphalangism (metacarpal or metatarsal shortening) is reported in ~50% of cases overall, but is typically not evident below the age of 2 years. There is striking phenotypic variability, and the size and extent of the deleted region cannot be used as accurate predictors of prognosis. Some patients have additional problems such as congenital heart disease and seizures. Genetics The minimal deletion causing this syndrome has been defined as a 3 megabase region that contains the genes GPR35, GPC1 and STK25. Almost all deletions are found to be terminal deletions at the end of chromosome 2. There is a high frequency of ''de novo'' deletions, but multiple cases within a single ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lysophosphatidic Acid
Lysophosphatidic acid (LPA) is a phospholipid derivative that can act as a signaling molecule. Function LPA acts as a potent mitogen due to its activation of three high-affinity G-protein-coupled receptors called LPAR1, LPAR2, and LPAR3 (also known as EDG2, EDG4, and EDG7). Additional, newly identified LPA receptors include LPAR4 (P2RY9, GPR23), LPAR5 (GPR92) and LPAR6 (P2RY5, GPR87). Clinical significance Because of its ability to stimulate cell proliferation, aberrant LPA-signaling has been linked to cancer in numerous ways. Dysregulation of autotaxin or the LPA receptors can lead to hyperproliferation, which may contribute to oncogenesis and metastasis. LPA may be the cause of pruritus (itching) in individuals with cholestatic (impaired bile flow) diseases. GTPase activation Downstream of LPA receptor activation, the small GTPase Rho can be activated, subsequently activating Rho kinase. This can lead to the formation of stress fibers and cell migration through the inhibiti ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lodoxamide
Lodoxamide is an antiallergic pharmaceutical drug. It is marketed under the tradename Alomide in the UK. Like cromoglicic acid it acts as a mast cell stabilizer. In 2014 lodoxamide and bufrolin were found to be potent agonists at the G protein-coupled receptor 35, an orphan receptor believed to play a role in inflammatory processes, pain and the development of stomach cancer. See also *Nedocromil *Zaprinast * Amlexanox *Pemirolast *Pamoic acid *Kynurenic acid Kynurenic acid (KYNA or KYN) is a product of the normal metabolism of amino acid -tryptophan. It has been shown that kynurenic acid possesses neuroactive activity. It acts as an antiexcitotoxic and anticonvulsant, most likely through acting as an ... * CXCL17 References Nitriles Chloroarenes Carboxamides Dicarboxylic acids Mast cell stabilizers {{respiratory-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
2q37 Deletion Syndrome
2q37 deletion syndrome is a disorder caused by the deletion of a small piece of chromosome 2 in which one or more of 3 sub-bands, 2q37.1, 2q37.2, and 2q37.3, of the last band of one of the chromosome 2’s long arms are deleted. The first report of this disorder was in 1989. Symptoms and signs The earliest signs and symptoms occur in newborns and consist of hypotonia, but show up in youth as developmental delays, low muscle tone, learning disabilities, being overweight, autism-like symptoms, seizures, eczema, asthma, chest and ear infections, and abnormalities in face, hands, and feet such as brachydactyly. Autism-like symptoms consist of odd obsessions, repetitive behavior, poor use of eye contact, impaired speech, poor understanding of others’ emotions, idiosyncratic use of words or phrases. People with this disorder also tend to have a characteristic appearance, including prominent forehead, thin, highly arched eyebrows, depressed nasal bridge, full cheeks, deficient nasal al ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Brachydactyly Mental Retardation Syndrome
Brachydactyly (Greek βραχύς = "short" plus δάκτυλος = "finger"), is a medical term which literally means "short finger". The shortness is relative to the length of other long bones and other parts of the body. Brachydactyly is an inherited, dominant trait. It most often occurs as an isolated dysmelia, but can also occur with other anomalies as part of many congenital syndromes. Brachydactyly may also be a signal that one is at risk for congenital heart disease due to the association between congenital heart disease and carpenter's syndrome and the link between carpenter's syndrome and brachydactyly Nomograms for normal values of finger length as a ratio to other body measurements have been published. In clinical genetics, the most commonly used index of digit length is the dimensionless ratio of the length of the third (middle) finger to the hand length. Both are expressed in the same units (centimeters, for example) and are measured in an open hand from the finger ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Rodent
Rodents (from Latin , 'to gnaw') are mammals of the order Rodentia (), which are characterized by a single pair of continuously growing incisors in each of the upper and lower jaws. About 40% of all mammal species are rodents. They are native to all major land masses except for New Zealand, Antarctica, and several oceanic islands, though they have subsequently been introduced to most of these land masses by human activity. Rodents are extremely diverse in their ecology and lifestyles and can be found in almost every terrestrial habitat, including human-made environments. Species can be arboreal, fossorial (burrowing), saltatorial/richochetal (leaping on their hind legs), or semiaquatic. However, all rodents share several morphological features, including having only a single upper and lower pair of ever-growing incisors. Well-known rodents include mice, rats, squirrels, prairie dogs, porcupines, beavers, guinea pigs, and hamsters. Rabbits, hares, and pikas, whose i ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Receptor Antagonist
A receptor antagonist is a type of receptor ligand or drug that blocks or dampens a biological response by binding to and blocking a receptor rather than activating it like an agonist. Antagonist drugs interfere in the natural operation of receptor proteins.Pharmacology Guide: In vitro pharmacology: concentration-response curves " '' GlaxoWellcome.'' Retrieved on December 6, 2007. They are sometimes called blockers; examples include alpha blockers, |
Pharmaceutical Drugs
A medication (also called medicament, medicine, pharmaceutical drug, medicinal drug or simply drug) is a drug used to diagnose, cure, treat, or prevent disease. Drug therapy (pharmacotherapy) is an important part of the medical field and relies on the science of pharmacology for continual advancement and on pharmacy for appropriate management. Drugs are classified in multiple ways. One of the key divisions is by level of control, which distinguishes prescription drugs (those that a pharmacist dispenses only on the order of a physician, physician assistant, or qualified nurse) from over-the-counter drugs (those that consumers can order for themselves). Another key distinction is between traditional small molecule drugs, usually derived from chemical synthesis, and biopharmaceuticals, which include recombinant proteins, vaccines, blood products used therapeutically (such as IVIG), gene therapy, monoclonal antibodies and cell therapy (for instance, stem cell therapies). Other ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
