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),
leukotriene A4 hydrolase (a
zinc metalloprotease that displays both
epoxide hydrolase and
aminopeptidase activities),
alanyl aminopeptidase (aminopeptidase M/N),
leucyl/cystinyl aminopeptidase (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.
It is derived from ''
Streptomyces olivoreticuli''.
Ubenimex has been found to inhibit the enzymatic degradation of
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 trave ...
,
enkephalins, 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.
...
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- ...
References
External links
* The
MEROPS online database for peptidases and their inhibitors
Bestatin
Enkephalinase inhibitors
Protease inhibitors
Experimental cancer drugs
Secondary amino acids
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