Ubenimex (
INN), also known more commonly as bestatin, is a competitive, reversible
protease inhibitor. It is an
inhibitor
Inhibitor or inhibition may refer to:
In biology
* Enzyme inhibitor, a substance that binds to an enzyme and decreases the enzyme's activity
* Reuptake inhibitor, a substance that increases neurotransmission by blocking the reuptake of a neurotra ...
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 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 sub ...
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 (leukotriene D
4 hydrolase). It is being studied for use in the treatment of
acute myelocytic leukemia and
lymphedema.
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. Oxytoc ...
,
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 ...
,
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 enkephal ...
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. ...
s and compounds.
See also
*
Amastatin
*
Pepstatin
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 inhibitors ...
online database for peptidases and their inhibitors
Bestatin
Enkephalinase inhibitors
Protease inhibitors
Experimental cancer drugs
Secondary amino acids
{{pharma-stub