Bestatin, an aminopeptidase inhibitor with a multi-pharmacological function. NLM AIDSLINE Important note: Information in this article was accurate in 1992. The state of the art may have changed since the publication date.

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Bestatin, an aminopeptidase inhibitor with a multi-pharmacological function.

Biomed Pharmacother. 1991;45(2-3):49-54. Unique Identifier : AIDSLINE MED/92003260
Mathe G; Institut du Cancer et d'Immunogenetique, Villejuif, France.

Abstract: Bestatin, the dipeptide N-((2S, 3R)-3-amino-2-hydroxy-4-phenyl butanyl) L-leucine is a leucine aminopeptidase and aminopeptidase-B inhibitor. It exerts a direct stimulating effect on lymphocytes (and monocytes) via its fixation on cell surface leucine-aminopeptidase, and an indirect effect on monocytes (and lymphocytes) via aminopeptidase B inhibition of tuftsin catabolism. Thus it is an immuno-modifier as shown by the Japanese and also our groups: a) immuno-modifier, especially stimulator, in normal young mice; b) immunorestorator and spontaneous tumor preventive agent in aged mice; c) immunorestorator in the elderly and in cancer patients and HIV infected subjects. It stimulates granulocytopoiesis and thrombocytopoiesis in vitro, and can restore them in vivo in myelo-hypoplastic man. The anti-aminopeptidase action of Bestatin also protects enkephalins against their catabolism, which encouraged us, with good preliminary results, to study its analgesic action and search for a preventive effect on desaddicted toxicomaniac relapses.
Keywords: Aminopeptidases/*ANTAGONISTS & INHIB Animal Antibiotics, Antineoplastic/*PHARMACOLOGY/THERAPEUTIC USE Human HIV Infections/DRUG THERAPY Leucine/*ANALOGS & DERIVATIVES/PHARMACOLOGY/THERAPEUTIC USE Mice Neoplasms/DRUG THERAPY Neoplasms, Experimental/DRUG THERAPY JOURNAL ARTICLE REVIEW REVIEW, TUTORIAL

KWDaminopeptidases/KWDantagonists&inhibanimalantibiotics,antineoplastic/KWDpharmacology/therapeuticusehumanhivinfections/drugtherapyleucine/KWDanalogs&derivatives/pharmacology/therapeuticusemiceneoplasms/drugtherapyneoplasms,experimental/drugtherapyjournalarticlereviewreview,tutorial
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Copyright © 1992 - National Library of Medicine. Reproduced under license with the National Library of Medicine, Bethesda, MD.

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