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Amastatin, also known as 3-amino-2-hydroxy-5-methylhexanoyl-L-valyl-L-valyl-L-aspartic acid, is a
naturally occurring A natural product is a natural compound or substance produced by a living organism—that is, found in nature. In the broadest sense, natural products include any substance produced by life. Natural products can also be prepared by chemical sy ...
, competitive and reversible
aminopeptidase Aminopeptidases are enzymes that catalyze the cleavage of amino acids from the amino terminus ( N-terminus) of proteins or peptides (exopeptidases). They are widely distributed throughout the animal and plant kingdoms and are found in many subcel ...
inhibitor that was isolated from ''
Streptomyces ''Streptomyces'' is the largest genus of Actinomycetota and the type genus of the family Streptomycetaceae. Over 500 species of ''Streptomyces'' bacteria have been described. As with the other Actinomycetota, streptomycetes are gram-positive, ...
sp. ME 98-M3''. It specifically inhibits
leucyl aminopeptidase Leucyl aminopeptidases (, ''leucine aminopeptidase'', ''LAPs'', ''leucyl peptidase'', ''peptidase S'', ''cytosol aminopeptidase'', ''cathepsin III'', ''L-leucine aminopeptidase'', ''leucinaminopeptidase'', ''leucinamide aminopeptidase'', ''FTBL pr ...
, alanyl aminopeptidase (aminopeptidase M/N), bacterial leucyl aminopeptidase (''Aeromonas proteolytica'' aminopeptidase),
leucyl/cystinyl aminopeptidase Leucyl/cystinyl aminopeptidase, also known as cystinyl aminopeptidase (CAP), insulin-regulated aminopeptidase (IRAP), human placental leucine aminopeptidase (PLAP), oxytocinase, and vasopressinase, is an enzyme of the aminopeptidase group that in ...
(oxytocinase/vasopressinase), and, to a lesser extent, glutamyl aminopeptidase (aminopeptidase A), as well as other aminopeptidases. It does not inhibit
arginyl aminopeptidase Aminopeptidase B (, ''arylamidase II'', ''arginine aminopeptidase'', ''arginyl aminopeptidase'', ''Cl—activated arginine aminopeptidase'', ''cytosol aminopeptidase IV'', ''L-arginine aminopeptidase'') is an enzyme. This enzyme catalyses the fo ...
(aminopeptidase B). Amastatin has been found to potentiate the
central nervous system The central nervous system (CNS) is the part of the nervous system consisting primarily of the brain and spinal cord. The CNS is so named because the brain integrates the received information and coordinates and influences the activity of all par ...
effects of
oxytocin Oxytocin (Oxt or OT) is a peptide hormone and neuropeptide normally produced in the hypothalamus and released by the posterior pituitary. It plays a role in social bonding, reproduction, childbirth, and the period after childbirth. Oxytocin ...
and
vasopressin Human vasopressin, also called antidiuretic hormone (ADH), arginine vasopressin (AVP) or argipressin, is a hormone synthesized from the AVP gene as a peptide prohormone in neurons in the hypothalamus, and is converted to AVP. It then travel ...
''in vivo''. It also inhibits the degradation of
met-enkephalin Met-enkephalin, also known as metenkefalin (INN), sometimes referred to as opioid growth factor (OGF), is a naturally occurring A natural product is a natural compound or substance produced by a living organism—that is, found in nature. In ...
,
dynorphin A Dynorphin A is a dynorphin, an endogenous opioid peptide with the amino acid sequence: Tyr-Gly-Gly-Phe-Leu-Arg-Arg-Ile-Arg-Pro-Lys-Leu-Lys. Dynorphin A1–8 is a truncated form of dynorphin A with the amino acid sequence: Tyr-Gly-Gly-Phe-Leu-Ar ...
, and other
endogenous Endogenous substances and processes are those that originate from within a living system such as an organism, tissue, or cell. In contrast, exogenous substances and processes are those that originate from outside of an organism. For example, es ...
peptide Peptides (, ) are short chains of amino acids linked by peptide bonds. Long chains of amino acids are called proteins. Chains of fewer than twenty amino acids are called oligopeptides, and include dipeptides, tripeptides, and tetrapeptides. A ...
s.


See also

*
Bestatin Ubenimex (INN), also known more commonly as bestatin, is a competitive, reversible protease inhibitor. It is an inhibitor of arginyl aminopeptidase (aminopeptidase B), leukotriene A4 hydrolase (a zinc metalloprotease that displays both epoxide ...
*
Pepstatin Pepstatin is a potent inhibitor of aspartyl proteases. It is a hexa-peptide containing the unusual amino acid statine (Sta, (3S,4S)-4-amino-3-hydroxy-6-methylheptanoic acid), having the sequence Isovaleryl-Val-Val-Sta-Ala-Sta (Iva-Val-Val-Sta-Al ...


References

Enkephalinase inhibitors Peptides Protease inhibitors {{drug-stub