Compounds

Bestatin (Ubenimex)

Bestatin (Ubenimex)_1

Producing organism:

Streptomyces oliboreticuli MD976-C7

Activity:

Inhibitor of aminopeptidase Bleucine aminopeptidasealanine aminopeptidasetripeptidyl and tetrapeptidyl aminopeptidaseImmunomodulator,Antitumor Agent

Clinical use:

Immunomodulator,Antineoplastic

Class no:

48 Reference(s)

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Title Author Journal Year Volume Page
Bestatin, an inhibitor of aminopeptidase B, produced by Actinomycetes. H. Umezawa; T. Aoyagi; H. Suda; M. Hamada; T. Takeuchi J. Antibiotics 1976 29 97-99
The structure of bestatin. H. Suda; T. Takita; T. Aoyagi; H. Umezawa J. Antibiotics 1976 29 100-101
X-ray structure determination of (2S,3R)-3-amino-2-hydroxy-4-phenylbutanoic acid, a new amino acid component of bestatin. H. Nakamura; H. Suda; T. Takita; T. Aoyagi; H. Umezawa J. Antibiotics 1976 29 102-103
The chemical synthesis of bestatin. H. Suda; T. Takita; T. Aoyagi; H. Umezawa J. Antibiotics 1976 29 600-601
Enhancement of delayed-type hypersensitivity by bestatin, an inhibitor of aminopeptidase B and leucine aminopeptidase. H. Umezawa; M. Ishizuka; T. Aoyagi; T. Takeuchi J. Antibiotics 1976 29 857-859
Inhibition of aminopeptidase B and leucine aminopeptidase by bestatin and its stereoisomer. H. Suda; T. Aoyagi; T. Takeuchi; H. Umezawa Archiv. Biochem. Biophys. 1976 177 196-200
Synthesis and structure-activity relationships of bestatin analogs, inhibitors of aminopeptidase B. R. Nishizawa; T. Saino; T. Takita; H. Suda; T. Aoyagi; H. Umezawa J. Med. Chem. 1977 20 510-515
Bestatin, a new specific inhibitor of aminopeptidases, enhances activation of small lymphocytes by concanavalin A. M. Saito; T. Aoyagi; H. Umezawa; Y. Nagai Biochem. Biophys. Res. Commun. 1977 76 526-533
Stimulatory effect of bestatin, a new specific inhibitor of aminopeptidases, on the blastogenesis of guinea pig lymphocytes. M. Saito; K. Takegoshi; T. Aoyagi; H. Umezawa; Y. Nagai Cellular Immunology 1978 40 247-264
Activation of DNA metabolism in T-cells by bestatin. W. E. G. Mueller; R. K. Zahn; J. Arendes; N. Munsch; H. Umezawa Biochem. Pharmacol. 1979 28 3131-3137
Effect of bestatin on mouse immune system and experimental murine tumors. M. Ishizuka; T. Masuda; N. Kanbayashi; S. Fukasawa; T. Takeuchi; T. Aoyagi; H. Umezawa J. Antibiotics 1980 33 642-652
Mitogenic effect of bestatin on lymphocytes. M. Ishizuka; J. Sato; Y. Sugiyama; T. Takeuchi; H. Umezawa J. Antibiotics 1980 33 653-662
Synthesis of bestatin and its analogues and their bioactivity. (Japanese) H. Umezawa; T. Takita Yuki Gosei Kagaku Kyokaishi 1980 38 1077-1083
A review of clinical studies of bestatin. S. Oka Recent Results in Cancer Research 1980 75 126-132
Screening of small molecular microbial products modulating immune responses and bestatin. H. Umezawa Recent Results in Cancer Research 1980 75 115-125
Fundamental studies on bestatin: A small molecular microbial product enhancing immune responses. H. Umezawa Recent Results in Cancer Research 1981 76 209-221
A review of clinical studies on bestatin, 1976-1978. S. Oka Recent Results in Cancer Research 1981 76 222-231
Properties and specificity of binding sites for the immunomodulator bestatin on the surface of mammalian cells. W. E. G. Mueller; D. Schuster; R. K. Zahn; A. Maidhof; G. Leyhausen; D. Falke; R. Koren; H. Umezawa Int. J. Immunopharmacol. 1982 4 393-400
Restoration of impaired immune functions of aged animals by chronic bestatin treatment. M. Bruley-Rosset; I. Florentin; N. Kiger; J. Schulz; G. Mathe Immunology 1979 38 75-83
Identification and properties of the cell membrane bound leucine aminopeptidase interacting with the potential immunostimulant and chemotherapeutic agent bestatin. G. Leyhausen; D. K. Schuster; P. Vaith; R. K. Zahn; H. Umezawa; D. Falke; W. E. G. Mueller Biochemical Pharmacology 1983 32 1051-1057
Immunochemical identification of the cell surface bound leucine aminopeptidase, the target enzyme for the immunostimulant bestatin. G. Leyhausen; M. Gramzow; R. K. Zahn; R. Steffen; H. Umezawa; W. E. G. Mueller J. Antibiotics 1983 36 728-734
Studies of the potential usefulness of bestatin in cancer treatment. H. Umezawa Cancer Treatment Symposia 1983 1 15-18
Effect of bestatin on syngeneic tumors in mice. F. Abe; K. Shibuya; M. Uchida; K. Takahashi; H. Horinishi; A. Matsuda; M. Ishizuka; T. Takeuchi; H. Umezawa Gann 1984 75 89-94
Antitumor effect of bestatin combined with bleomycin against hepatoma AH66 subcutaneously transplanted in rats. (Japanese) F. Abe; T. Yamashita; K. Takahashi; A. Matsuda; T. Ichikawa; H. Umezawa Jap. J. Antibiotics 1984 37 589-592
Biological effect of bestatin against rat ascites hepatomas and enhancement of interferon production. (Japanese) H. Sato Jap. J. Antibiotics 1984 9 405-987
Studies on low moelcular weight immunomodifiers, bestatin, etc. Discovery and actions. H. Umezawa Drugs Exptl. Clin. Res. 1984 10 519-531
Oscillation of enzyme networks in spleen triggered by an immunopotentiator, bestatin. T. Aoyagi; T. Wada; S. Ohuchi; F. Kojima; M. Nagai; F. Kawahara; H. Umezawa Biochemistry International 1984 9 405-411
Different enzymatic oscillations in vivo caused by the stereoisomers of an aminopeptidase inhibitor, bestatin. T. Aoyagi; T. Wada; K. Yamamoto; F. Kojima; M. Nagai; S. Harada; H. Umezawa J. Appl. Biochem. 1984 6 212-221
In vivo actions of bestatin-related compounds in relation to their actions in vitro. T. Aoyagi; T. Wada; S. Ohuchi; K. Kawamura; S. Fukatsu; H. Umezawa Biochemistry International 1985 9 643-650
Enhancement of antitumor effect of cytotoxic agents by bestatin. F. Abe; K. Shibuya; J. Ashizawa; K. Takahashi; H. Horinishi; A. Matsuda; M. Ishizuka; T. Takeuchi; H. Umezawa J. Antibiotics 1985 38 411-414
Mitogenic potentials of bestatin, amastatin, arphamenines A and B, FK-156 and FK-565 on spleen lymphocytes. N. Weissmann; G. Leyhausen; A. Maidhof; W. Tanaka; H. Umezawa; W. E. G. Mueller J. Antibiotics 1985 38 772-778
Potentiation of the bleomycin, arabinofuranosylcytosine and adriamycin-caused inhibition of DNA synthesis in lymphocytes by bestatin in vitro. G. Leyhausen; H. C. Schroeder; D. K. Schuster; A. Maidhof; H. Umezawa; W. E. G. Mueller Eur. J. Cancer Clin. Oncol. 1985 21 1325-1330
Bestatin, a microbial aminopeptidase inhibitor, inhibits DNA synthesis induced by insulin or epidermal growth factor in primary cultured rat hepatocytes. S. Takahashi; H. Kato; T. Seki; T. Noguchi; H. Naito; T. Aoyagi; H. Umezawa J. Antibiotics 1985 38 1767-1773
Cell surface-bound leucine aminopeptidase: Target of the immunomodulator bestatin. W. E. G. Mueller; D. K. Schuster; G. Leyhausen; C. Sobel; H. Umezawa Cellular Biology of Ectoenzymes (Ed. G. W. Kreutzberg et al.)Springer-Verlag 1986 36 285-293
Bestatin suppresses the serum levels of several hydrolytic enzymes in a patient with progressive muscular dystrophy. T. Aoyagi; T. Wada; F. Kojima; M. Nagai; S. Harada; M. Kinoshita; N. Yamada; H. Umezawa J. Clin. Biochem. Nutr. 1986 1 65-72
Biosynthesis of an unusual amino acyl moiety contained in bestatin. A. Okuyama; H. Naganawa; S. Harada; T. Aoyagi; H. Umezawa Biochemistry International 1986 12 627-631
Bestatin: a low molecular immunomodifier. H. Umezawa; M. Ishizuka Natural Immunity, Cancer and Biological Response Modification (Eds. E. Lotzova; R. B. Herberman)Karger, Basel 1986 272-279
Bestatin, a low moelcular weight immunomodifier produced by microorganisms. H. Umezawa; M. Ishizuka; T. Takeuchi; F. Abe; K. Shibuya Developments in Industrial Microbiology (J. Industrial Microbiology Suppl. No. 1) (Ed. G. Pierce)Society for Industrial Microbiology 1987 27 31-36
Enhancement of interleukin 1 and interleukin 2 releases by ubenimex. K. Shibuya; E. Hayashi; F. Abe; K. Takahashi; H. Horinishi; M. Ishizuka; T. Takeuchi; H. Umezawa J. Antibiotics 1987 40 363-369
Antitumor cells found in tumor-bearing mice given ubenimex. M. Ishizuka; T. Masuda; S.Mizutani; T. Takeuchi; H. Umezawa J. Antibiotics 1987 40 697-701
Enhancement of colony formation of mouse bone marrow cells by ubenimex. K. Nemoto; F. Abe; K. Karakawa; H. Horinishi; H. Umezawa J. Antibiotics 1987 40 894-898
Synthesis of p-hydroxyubenimex. T. Saino; K. Seya; R. Nishizawa; T. Takita; T. Aoyagi; H. Umezawa J. Antibiotics 1987 40 1165-1169
Action of ubenimex on aminopeptidase activities in spleen cells and peritoneal macrophages from mice. H. Kuramochi; A. Motegi; M. Iwabuchi; K. Takahashi; H. Horinishi; H. Umezawa J. Antibiotics 1987 40 1605-1611
Effect of ubenimex on the production of murine interferon. A. Okura; M. Ishizuka; T. Takeuchi J. Antibiotics 1988 41 261-263
The effect of bestatin, a microbial aminopeptidase inhibitor, on epidermal growth factor-induced DNA synthesis and cell division in primary cultured hepatocytes of rats. S. Takahashi; Y. Ohishi; H. Kato; T. Noguchi; H. Naito; T. Aoyagi Experimental Cell Research 1989 183 399-412
Enhancement of host resistance to opportunistic infections by ubenimex (bestatin). M. Ishizuka; F. Abe; S. Abe; K. Uchida; T. Ikeda; N. Ito; K. Aoyagi; H. Yamaguchi; T. Takeuchi Microbial Infections. H. Friedman, et al. Eds., Plenum Press, New York 1992 319 193-200
Enhancement by ubenimex (bestatin) of host resistance to Candida albicans infection. K. Aoyagi; N. Itoh; F. Abe; S. Abe; K. Uchida; M. Ishizuka; T. Takeuchi; H. Yamaguchi J. Antibiotics 1992 45 1778-1784
Purification and characterization of a ubenimex (bestatin)-sensitive aminopeptidase β-like enzyme from K562 human chronic myeloid leukemia cells. M. Yamada; Y. Sukenaga; H. Fujii; F. Abe; T. Takeuchi FEBS Letters 1994 342 53-56