Ubenimex (
INN
Inns are generally establishments or buildings where travelers can seek lodging, and usually, food and drink. Inns are typically located in the country or along a highway; before the advent of motorized transportation they also provided accommo ...
), also known more commonly as bestatin, is a competitive, reversible
protease inhibitor. It is an
inhibitor of
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),
leukotriene A4 hydrolase (a
zinc metalloprotease that displays both
epoxide hydrolase
Epoxide hydrolases (EH's), also known as epoxide hydratases, are enzymes that metabolize compounds that contain an epoxide residue; they convert this residue to two hydroxyl residues through an epoxide hydrolysis reaction to form diol products. ...
and
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 ...
activities),
alanyl aminopeptidase (aminopeptidase M/N),
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
membrane dipeptidase
Membrane dipeptidase (, ''renal dipeptidase'', ''dehydropeptidase I (DPH I)'', ''dipeptidase'', ''aminodipeptidase'', ''dipeptide hydrolase'', ''dipeptidyl hydrolase'', ''nonspecific dipeptidase'', ''glycosyl-phosphatidylinositol-anchored renal di ...
(leukotriene D
4 hydrolase). It is being studied for use in the treatment of
acute myelocytic leukemia
Acute myeloid leukemia (AML) is a cancer of the myeloid line of blood cells, characterized by the rapid growth of abnormal cells that build up in the bone marrow and blood and interfere with normal blood cell production. Symptoms may include ...
and
lymphedema
Lymphedema, also known as lymphoedema and lymphatic edema, is a condition of localized swelling caused by a compromised lymphatic system. The lymphatic system functions as a critical portion of the body's immune system and returns interstitial fl ...
.
It is derived from ''
Streptomyces olivoreticuli''.
Ubenimex has been found to inhibit the enzymatic degradation 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 ...
,
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 ...
,
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 enkephalin ...
s, and various other
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 and compounds.
See also
*
Amastatin
Amastatin, also known as 3-amino-2-hydroxy-5-methylhexanoyl-L-valyl-L-valyl-L-aspartic acid, is a naturally occurring, competitive and reversible aminopeptidase inhibitor that was isolated from ''Streptomyces sp. ME 98-M3''. It specifically inhib ...
*
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
External links
* The
MEROPS
MEROPS is an online database for peptidases (also known as proteases, proteinases and proteolytic enzymes) and their inhibitors. The classification scheme for peptidases was published by Rawlings & Barrett in 1993, and that for protein inhibitor ...
online database for peptidases and their inhibitors
Bestatin
Enkephalinase inhibitors
Protease inhibitors
Experimental cancer drugs
Secondary amino acids
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