Bestatin, an aminopeptidase inhibitor with a multipharmacologic function (Meeting abstract).

Important note: Information in this article was accurate in 1993. The state of the art may have changed since the publication date.

Bestatin, an aminopeptidase inhibitor with a multipharmacologic function (Meeting abstract).

Eighth Mediterranean Congress of Chemotherapy. May 24-9, 1992, Athens, Greece, p. 731, 1992. Unique Identifier : AIDSLINE ICDB/93688839
Mathe G; Chenu E; Bourut C; Orbach-Arbouys S; Institut du Cancer et d'Immunogenetique, Hopital Paul-Brousse,; Villejuif, France

Abstract: Bestatin, dipeptide N-([2S,3R]-3-amino-2-hydroxy-4-phenylbutanoyl)-L-leucine is a leucine aminopeptidase and B aminopeptidase inhibitor which exerts a direct stimulating effect on lymphocytes (and monocytes) via its fixation on cell surface leucine aminopeptidase, and an indirect one on monocytes (and lymphocytes) via B aminopeptidase inhibition of tuftsin catabolism. It is, thus, an immunomodifier as shown by Japanese groups and ourselves: (1) immunomodifier, especially stimulator, in normal young mice; (2) immunorestorative and spontaneous tumor preventive agent in aged mice; (3) immunorestorative in aged humans, in cancer patients and HIV-infected subjects. It stimulates granulocytopoiesis and thrombocytopoiesis in vitro, and can restore them in vivo in myelohypoplastic patients. The antiaminopeptidase action of bestatin also prevents enkephalin catabolism. This fact has led us, with encouraging preliminary results, to study its analgesic action and to investigate whether it can prevent relapses in drug addiction after detoxification.

Keywords: *Adjuvants, Immunologic Aminopeptidases/ANTAGONISTS & INHIB Animal Blood Platelets/CYTOLOGY Enkephalins Granulocytes/CYTOLOGY HIV Infections/PATHOLOGY Leucine/*ANALOGS & DERIVATIVES/PHARMACOLOGY/THERAPEUTIC USE Leucine Aminopeptidase/METABOLISM Lymphocytes/*CYTOLOGY/DRUG EFFECTS Mice Neoplasms/PATHOLOGY/*THERAPY Tuftsin/METABOLISM MONOGRAPH
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M9340828

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