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Ecadotril
Ecadotril is a neutral endopeptidase inhibitor ((NEP) EC 3.4.24.11) and determined by the presence of peptidase family M13 as a neutral endopeptidase inhibited by phosphoramidon. Ecadotril is the (''S'')-enantiomer of racecadotril. NEP-like enzymes include the endothelin- converting enzymes. The peptidase M13 family believed to activate or inactivate oligopeptide (pro)-hormones such as opioid peptides, neprilysin is another member of this group, in the case of the metallopeptidases and aspartic, the nucleophiles clan or family for example MA, is an activated water molecule. The peptidase domain for members of this family also contains a bacterial member and resembles that of thermolysin the predicted active site residues for members of this family and thermolysin occur in the motif HEXXH. Thermolysin complexed with the inhibitor (''S'')-thiorphan are isomeric thiol-containing inhibitors of endopeptidase EC 24-11 (also called "enkephalinase"). See also * RB-101 * Candoxatril ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Neutral Endopeptidase
Neprilysin (), also known as membrane metallo-endopeptidase (MME), neutral endopeptidase (NEP), cluster of differentiation 10 (CD10), and common acute lymphoblastic leukemia antigen (CALLA) is an enzyme that in humans is encoded by the ''MME'' gene. Neprilysin is a zinc-dependent metalloprotease that cleaves peptides at the amino side of hydrophobic residues and inactivates several peptide hormones including glucagon, enkephalins, substance P, neurotensin, oxytocin, and bradykinin. It also degrades the amyloid beta peptide whose abnormal folding and aggregation in neural tissue has been implicated as a cause of Alzheimer's disease. Synthesized as a membrane-bound protein, the neprilysin ectodomain is released into the extracellular domain after it has been transported from the Golgi apparatus to the cell surface. Neprilysin is expressed in a wide variety of tissues and is particularly abundant in kidney. It is also a common acute lymphocytic leukemia antigen that is an impor ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Racecadotril
Racecadotril, also known as acetorphan, is an antidiarrheal medication which acts as a peripheral enkephalinase inhibitor. Unlike other opioid medications used to treat diarrhea, which reduce intestinal motility, racecadotril has an antisecretory effect — it reduces the secretion of water and electrolytes into the intestine. It is available in France (where it was first introduced in ~1990) and other European countries (including Germany, Italy, the United Kingdom, Spain, Portugal, Poland, Finland, Russia and the Czech Republic) as well as most of South America and some South East Asian countries (including China, India and Thailand), but not in the United States. It is sold under the tradename Hidrasec, among others. Thiorphan is the active metabolite of racecadotril, which exerts the bulk of its inhibitory actions on enkephalinases. Medical uses Racecadotril is used for the treatment of acute diarrhea in children and adults and has better tolerability than loperamide, as i ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Neprilysin
Neprilysin (), also known as membrane metallo-endopeptidase (MME), neutral endopeptidase (NEP), cluster of differentiation 10 (CD10), and common acute lymphoblastic leukemia antigen (CALLA) is an enzyme that in humans is encoded by the ''MME'' gene. Neprilysin is a zinc-dependent metalloprotease that cleaves peptides at the amino side of hydrophobic residues and inactivates several peptide hormones including glucagon, enkephalins, substance P, neurotensin, oxytocin, and bradykinin. It also degrades the amyloid beta peptide whose abnormal folding and aggregation in neural tissue has been implicated as a cause of Alzheimer's disease. Synthesized as a membrane-bound protein, the neprilysin ectodomain is released into the extracellular domain after it has been transported from the Golgi apparatus to the cell surface. Neprilysin is expressed in a wide variety of tissues and is particularly abundant in kidney. It is also a common acute lymphocytic leukemia antigen that is an important ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
RB-101
RB-101 is a drug that acts as an enkephalinase inhibitor, which is used in scientific research. RB-101 is a prodrug which acts by splitting at the disulfide bond once inside the brain, to form two selective enzyme inhibitors and blocking both types of the zinc-metallopeptidase enkephalinase enzymes. This inhibits the breakdown of the endogenous opioid peptides known as enkephalins. These two enzymes, aminopeptidase N (APN) and neutral endopeptidase 24.11 (NEP), are responsible for the breakdown of both kinds of enkephalin naturally found in the body, and so RB-101 causes a buildup of both Met-enkephalin and Leu-enkephalin. These peptides act primarily at the delta opioid receptor, although they also stimulate the mu opioid receptor to some extent through a delta-opioid receptor mediated interaction with another peptide cholecystokinin, and the enzyme-inhibiting effects of RB-101 thus produce indirect stimulation of both of these opioid receptor subtypes. This causes RB-101 to be ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Candoxatril
Candoxatril is the orally active prodrug of candoxatrilat (UK-73967). Human neutral endopeptidase Human neutral endopeptidase (neprilysin) as the neutral endopeptidase 24.11 complexed ( RB-101) with phosphoramidon degrades and inactivates a number of bioactive peptides. Two multiply connected folding domains of the neutral endopeptidase locus splicing of exons 1, 2a, or 2b to the common exon 3 composed of 24 exons of the human CALLA/NEP gene containing the active site, it is known as peptidase family M13 (neprilysin family, clan MA(E)) the gluzincins a faint but significant structural relationship of the metzincins to the thermolysin-like enzymes, Zincin is the simplest descriptor of biological space. The structure reveals two multiply connected folding domains which embrace a large central cavity containing the active site of the 5-indanyl ester prodrug candoxatril and differs from phosphoramidon Phosphoramidon is a chemical compound derived from cultures of '' Streptomyces ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Phosphoramidon
Phosphoramidon is a chemical compound derived from cultures of '' Streptomyces tanashiensis''. It is an inhibitor of the enzyme thermolysin, of the membrane metallo-endopeptidase,Phosphoramidon at and of the endothelin converting enzyme. Chemically, phosphoramidon differs from its closely related peptidase inhibitor talopeptin by a single stereocenter. Because of its enzyme inhibitory properties, phosphoramidon is widely used as a biochemical tool. References ...[...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Enantiomer
In chemistry, an enantiomer ( /ɪˈnænti.əmər, ɛ-, -oʊ-/ ''ih-NAN-tee-ə-mər''; from Ancient Greek ἐνάντιος ''(enántios)'' 'opposite', and μέρος ''(méros)'' 'part') – also called optical isomer, antipode, or optical antipode – is one of two stereoisomers that are non-superposable onto their own mirror image. Enantiomers are much like one's right and left hands, when looking at the same face, they cannot be superposed onto each other. No amount of reorientation will allow the four unique groups on the chiral carbon (see Chirality (chemistry)) to line up exactly. The number of stereoisomers a molecule has can be determined by the number of chiral carbons it has. Stereoisomers include both enantiomers and diastereomers. Diastereomers, like enantiomers, share the same molecular formula and are non-superposable onto each other however, they are not mirror images of each other. A molecule with chirality rotates plane-polarized light. A mixture of equals a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Endothelin
Endothelins are peptides with receptor (biochemistry), receptors and effects in many body organs. Endothelin constricts blood vessels and raises blood pressure. The endothelins are normally kept in balance by other mechanisms, but when gene expression, overexpressed, they contribute to high blood pressure (hypertension), heart disease, and potentially other diseases. Endothelins are 21-amino acid vasoconstriction, vasoconstricting peptides produced primarily in the endothelium having a key role in smooth muscle, vascular homeostasis. Endothelins are implicated in vascular diseases of several organ systems, including the heart, lungs, kidneys, and brain. As of 2018, endothelins remain under extensive basic research, basic and clinical research to define their roles in several organ systems. Etymology Endothelins derived the name from their isolation in cultured endothelial cells. Isoforms There are three isoforms of the peptide (identified as ET-1, -2, -3), each encoded by ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Endothelin Converting Enzyme 1
converting enzyme 1, also known as ECE1, is an enzyme which in humans is encoded by the ''ECE1'' gene. Function Endothelin-converting enzyme-1 is involved in the proteolytic processing of endothelin-1 (EDN1), -2 ( EDN2), and -3 (EDN3 Endothelin-3 is a protein that in humans is encoded by the ''EDN3'' gene. The protein encoded by this gene is a member of the endothelin family. Endothelins are endothelium-derived vasoactive peptides involved in a variety of biological functions ...) to biologically active peptides. References Further reading * * * * * * * * * * * * * * * * * * * * * {{gene-1-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Thermolysin
Thermolysin (, ''Bacillus thermoproteolyticus neutral proteinase'', ''thermoase'', ''thermoase Y10'', ''TLN'') is a thermostable neutral metalloproteinase enzyme produced by the Gram-positive bacteria ''Bacillus thermoproteolyticus''. It requires one zinc ion for enzyme activity and four calcium ions for structural stability. Thermolysin specifically catalyzes the hydrolysis of peptide bonds containing hydrophobic amino acids. However thermolysin is also widely used for peptide bond formation through the reverse reaction of hydrolysis. Thermolysin is the most stable member of a family of metalloproteinases produced by various ''Bacillus'' species. These enzymes are also termed 'neutral' proteinases or thermolysin -like proteinases (TLPs). Synthesis Like all bacterial extracellular proteases thermolysin is first synthesised by the bacterium as a pre-proenzyme. Thermolysin is synthesized as a pre-proenzyme consisting of a signal peptide 28 amino acids long, a pro-peptide 204 ami ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Thiorphan
Thiorphan is the active metabolite of the antidiarrheal racecadotril (acetorphan). It prevents the degradation of endogenous enkephalin An enkephalin is a pentapeptide involved in regulating nociception in the body. The enkephalins are termed endogenous ligands, as they are internally derived and bind to the body's opioid receptors. Discovered in 1975, two forms of enkephali ...s by acting as an enkephalinase inhibitor. References Enkephalinase inhibitors Antidiarrhoeals Amino acid derivatives Thiols Carboxamides Propionamides {{gastrointestinal-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Enkephalinase
Enkephalinases are enzymes that degrade endogenous enkephalin opioid peptides. They include: * Aminopeptidase N (APN) * Neutral endopeptidase (NEP) * Dipeptidyl peptidase 3 (DPP3) * Carboxypeptidase A6 (CPA6) * Leucyl/cystinyl aminopeptidase (LNPEP) * Angiotensin-converting enzyme (ACE) See also * Enkephalinase inhibitor * Oxytocinase Oxytocinase is a type of enzyme that metabolizes the endogenous neuropeptide, oxytocin. The most well-characterized oxytocinase is leucyl/cystinyl aminopeptidase, which is also an enkephalinase. Other oxytocinases are also known. During pregnancy, o ... References Hydrolases Human proteins Nociception {{Enzyme-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
