Ubenimex Explained

Ubenimex (INN), also known more commonly as bestatin, is a competitive, reversible protease inhibitor. It is an inhibitor of arginyl aminopeptidase (aminopeptidase B),[1] leukotriene A4 hydrolase (a zinc metalloprotease that displays both epoxide hydrolase and aminopeptidase activities),[2] alanyl aminopeptidase (aminopeptidase M/N),[3] leucyl/cystinyl aminopeptidase (oxytocinase/vasopressinase),[4] [5] and membrane dipeptidase (leukotriene D4 hydrolase). It is being studied for use in the treatment of acute myelocytic leukemia[6] and lymphedema.[7] It is derived from Streptomyces olivoreticuli.[8] Ubenimex has been found to inhibit the enzymatic degradation of oxytocin, vasopressin, enkephalins, and various other peptides and compounds.

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Notes and References

  1. 1976 . 29 . 97–99 . Bestatin, an inhibitor of aminopeptidase B, produced by actinomycetes.. Umezawa, H.. Aoyagi, T.. Suda, H.. Hamada, M.. Takeuchi, T.. The Journal of Antibiotics . 29 . 10.7164/antibiotics.29.97 . 931798 . free .
  2. 1994 . 48 . 131–137 . Modulation of pulmonary leukotriene formation and perfusion pressure by Bestatin, an inhibitor of leukotriene A4 hydrolase.. Muskardin, D.T.. Voelkel, N.F.. Fitzpatrick, F.A.. Biochemical Pharmacology . 48 . 10.1016/0006-2952(94)90232-1 . 8043014 .
  3. 1999 . 5 . 729–734 . Induction of apoptosis by Bestatin (ubenimex) in human leukemic cell lines . K Sekine . H Fujii . F Abe . Leukemia . 13 . 10.1038/sj.leu.2401388. 10374877 . free .
  4. Nakanishi Y, Nomura S, Okada M, Ito T, Katsumata Y, Kikkawa F, Hattori A, Tsujimoto M, Mizutani S . Immunoaffinity purification and characterization of native placental leucine aminopeptidase/oxytocinase from human placenta . Placenta . 21 . 7 . 628–34 . 2000 . 10985965 . 10.1053/plac.2000.0564 .
  5. Naruki M, Mizutani S, Goto K, Tsujimoto M, Nakazato H, Itakura A, Mizuno K, Kurauchi O, Kikkawa F, Tomoda Y . Oxytocin is hydrolyzed by an enzyme in human placenta that is identical to the oxytocinase of pregnancy serum . Peptides . 17 . 2 . 257–61 . 1996 . 8801531 . 10.1016/0196-9781(95)02124-8. 28486489 .
  6. 12938265 . 2003 . Hirayama . Y . Sakamaki . S . Takayanagi . N . Tsuji . Y . Sagawa . T . Chiba . H . Matsunaga . T . Niitsu . Y . Chemotherapy with ubenimex corresponding to patient age and organ disorder for 18 cases of acute myelogeneous leukemia in elderly patients--effects, complications and long-term survival . 30 . 8 . 1113–8 . Gan to Kagaku Ryoho. Cancer & Chemotherapy.
  7. 28490670 . 2017 . Tian . W . Rockson . S . Jiang . X . Kim . J . Begaye . A . Shuffle . EM . Tu . AB . Cribb . M . Nepiyushchikh . Z . Feroze . AH . Zamanian . RT . Dhillon . RT . Voelkel . NF . Peters-Golden . M . Kitajewski . J . Dixon . JB . Nicolls . MR . Leukotriene B4 antagonism ameliorates experimental lymphedema . 9 . 389 . eaal3920 . Science Translational Medicine . 10.1126/scitranslmed.aal3920. free .
  8. Bauvois. B. Dauzonne, D . Aminopeptidase-N/CD13 (EC 3.4.11.2) inhibitors: Chemistry, biological evaluations, and therapeutic prospects. Medicinal Research Reviews. 26. 1. 88–130. 10.1002/med.20044. 16216010. January 2006. 7168514.

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