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 accomm ...

), also known more commonly as bestatin, is a competitive, reversible protease inhibitor. It is an

inhibitor Inhibitor or inhibition may refer to: 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 neurotransmi ...

of arginyl aminopeptidase (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 N-terminus (beginning), of proteins or peptides. They are found in many organisms; in the cell, they are found in many organelles, in the cytosol (internal cellular f ...

activities), alanyl aminopeptidase (aminopeptidase M/N),

leucyl/cystinyl aminopeptidase Insulin regulated aminopeptidase (IRAP) is a protein that in humans is encoded by the leucyl and cystinyl aminopeptidase (''LNPEP'') gene. IRAP is a type II transmembrane protein which belongs to the oxytocinase subfamily of M1 aminopeptidases, a ...

(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 D₄ hydrolase). It is being studied for use in the treatment of acute myelocytic leukemia and

lymphedema Lymphedema, also known as lymphoedema and lymphatic edema, is a condition of localized edema, swelling caused by a compromised lymphatic system. The lymphatic system functions as a critical portion of the body's immune system and returns inters ...

. It is derived from '' Streptomyces olivoreticuli''. Ubenimex has been found to inhibit the enzymatic degradation of

oxytocin Oxytocin is a peptide hormone and neuropeptide normally produced in the hypothalamus and released by the posterior pituitary. Present in animals since early stages of evolution, in humans it plays roles in behavior that include Human bonding, ...

vasopressin Mammalian 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 ...

enkephalin An enkephalin is a pentapeptide involved in regulating nociception (pain sensation) in the body. The enkephalins are termed endogenous ligands, as they are internally derived (and therefore endogenous) and bind as ligands to the body's opioid ...

s, and various other

peptide Peptides are short chains of amino acids linked by peptide bonds. A polypeptide is a longer, continuous, unbranched peptide chain. Polypeptides that have a molecular mass of 10,000 Da or more are called proteins. Chains of fewer than twenty am ...

s and compounds.

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 inhibito ...

online database for peptidases and their inhibitors
Bestatin
Alpha-Amino acids Enkephalinase inhibitors Protease inhibitors Experimental cancer drugs Secondary amino acids Bacterial substances {{pharma-stub

See also

References

External links