Structure-Activity Relationship within a Series of Degradation Products of Tautomycin

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概要

• 論文の詳細を見る

• Tautomycin, a protein serine/threonine phosphatase inhibitor, was chemically degraded, and five derivatives were investigated for their biological activities. None of them exerted any inhibitory effects on the activity of protein phosphatase types 1 and 2A. However, one derivative, named TM2a, induced a significant morphological change (bleb-formation) of human myeloid leukemia K562 cells. TM2b, the trimethyl ester of TM2, did not induce bleb-formation. Thus, the maleic anhydride structure played an important role in the biological activity. The biological properties of TM2a toward K562 cells resembled those of a phorbol ester, rather than of tautomycin. The phorbol ester-induced bleb formation was abrogated by a non-specific inhibitor of protein kinases, staurosporine, and by an inhibitor of protein kinase C (PKC), H-7, but TM2a-induced bleb formation was abrogated only by staurosporine. Enhanced phosphorylation of the two proteins was observed after their exposure to TM2a. This Suggest that the effect was not due to any inhibition of protein phosphatase 1 or 2A, but rather to the activation of an unidentified kinase, possibly of the PKC family, or to inhibition of a protein phosphatase other than type 1 or 2A.

• 社団法人日本農芸化学会の論文
• 1996-01-23

著者

• Magae Junji

  Radiation Safety Research Center, Central Institute of Electric Power Industry

• KATAOKA Takao

  Department of Bioengineering, Tokyo Institute of Technology

• MAGAE Junji

  Department of Bioengineering, Tokyo Institute of Technology

• NAGAI Kazuo

  Department of Bioengineering, Tokyo Institute of Technology

• Magae J

  Tokyo Inst. Technol. Yokohama Jpn

• Magae Junji

  京都府立医科大学 麻酔学

• Magae Junji

  Dep. Of Biotechnology Inst. Of Res. And Innovation

• Magae Junji

  Radiation Safety Research Center Central Institute Of Electric Power Industry

• Magae J

  Inst. Res. And Innovation Kashiwa Jpn

• Kataoka T

  Tokyo Inst. Technol. Yokohama Jpn

• Kataoka Takao

  東京工業大学

• Isono K

  Inst. Physical And Chemical Res. Saitama Jpn

• Uramoto M

  Riken (the Institute Of Physical And Chemical Research)

• Uramoto M

  Tamagawa Univ. Tokyo Jpn

• Uramoto M

  Department Of Applied Biological Chemistry Tamagawa University

• Osada H

  Antibiotics Laboratory Advanced Science Institute Riken

• Kudo T

  Inst. Physical And Chemical Res. (riken) Saitama Jpn

• Ueki Masashi

  Riken Institute

• OSADA Hiroyuki

  The Institute of Physical and Chemical Research (RIKEN)

• ISONO Kiyoshi

  The Institute of Physical and Chemical Research, RIKEN

• UBUKATA Makoto

  Biotechnology Research Center, Toyama Prefectural University

• NISHIYAMA Uichi

  Department of Bioengineering, Tokyo Institute of Technology

• ERDODI Ferenc

  Department of Medical Chemistry, Medical University of Debercen

• HARTSHORNE David

  Department of Animal Sciences, University of Arizona, Tucson

• ISONO Kiyoshi

  Department of Marine Science and Technology, Tokai University

• URAMOTO Masakazu

  The Institute of Physical and Chemical Research

• Nagai K

  Yamanouchi Pharmaceutical Co. Ltd. Tokyo Jpn

• Nagai Kazuo

  Department Of Applied Biological Chemistry Chubu University

• Nagai K

  Chubu Univ. Aichi Jpn

• Isono K

  The Institute Of Physical And Chemical Research Riken

• Isono Kiyoshi

  The Institute Of Physical And Chemical Research(riken)

• Isono Kiyoshi

  The Institute Of Physical And Chemical Research (riken):(present Address) Department Of Marine Scien

• Kataoka Takao

  Department Of Bioengineering Tokyo Institute Of Technology

• Erdodi Ferenc

  Department Of Medical Chemistry Medical University Of Debercen

• Ubukata Makoto

  Biotechnology Research Center Toyama Prefecture University

• Isono K

  Tokai Univ. Shimizu Jpn

• Hartshorne David

  Department Of Animal Sciences University Of Arizona Tucson

• Nishiyama Uichi

  Department Of Bioengineering Tokyo Institute Of Technology

• Ubukata Makoto

  Biotechnology Research Center Toyama Prefectural University

• Kataoka Takao

  Department Of Applied Biology Kyoto Institute Of Technology

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