Synthesis and Tumor-promoting Activities of 12-Epi-phorbol-12,13-dibutyrate

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概要

• 論文の詳細を見る

• 12-Epi-phorbol-12,13-dibutyrate (1), the C12-epimer of the most frequently used phorbol ester probe, phorbol-12,13-dibutyrate (PDBu), has been synthesized from phorbol in 9 steps in order to investigate the structural requirements for tumor-promoting activity. Compound 1 showed about 100-fold weaker in vitro biological activities related to in vivo tumor promotion, Epstein-Barr virus early antigen (EBV-EA)-inducing ability, superoxide (O_2^-) generation-inducing ability, and binding to the protein kinase C (PKC) regulatory domain surrogate peptides. The results indicated that the β-stereochemistry at position 12 of the phorbol skeleton is important for optimal activity. Binding selectivity to each PKC C1 domain of 1 was almost equal to that of PDBu.

• 社団法人日本農芸化学会の論文
• 2000-11-23

著者

• OHIGASHI Hajime

  Division of Food Science and Biotechnology, Graduate School of Agriculture, Kyoto University

• Ohigashi H

  Department Of Surgery Osaka Medical Center For Cancer And Cardiovascular Diseases

• Ohigashi Hiroaki

  Department Of Surgery The Center For Adult Diseases

• 入江 一浩

  京都大学農学部

• Tanaka Minoru

  Division of Biological Sciences, Graduate School of Science, Hokkaido University

• 入江 一浩

  京都大学 食品工学

• 入江 一浩

  京都大学 農

• 入江 一浩

  京都大学大学院農学研究科食品生物科学

• Nakamura Yoshimasa

  Division Of Applied Life Sciences Graduate School Of Agriculture Kyoto University

• Nakamura Y

  Division Of Applied Life Sciences Graduate School Of Agriculture Kyoto University

• Ohigashi H

  Graduate School Of Agriculture Kyoto University

• Ohigashi H

  Division Of Applied Life Sciences Graduate School Of Agriculture Kyoto University

• Wender P

  Department Of Chemistry Stanford University

• Nakagawa Y

  Graduate School Of Agriculture Kyoto University

• Nakagawa Yu

  Graduate School Of Agriculture Kyoto University

• Wender Paul

  Department Of Chemistry Stanford University

• Nakagawa Yasue

  Department Of Food Faculty Of Home Economics Jissen Women's University

• Ohigashi Hajime

  Division Of Applied Life Sciences Graduate School Of Agriculture Kyoto University

• IRIE KAZUHIRO

  Division of Food Science and Biotechnology, Graduate School of Agriculture, Kyoto University

• NAKAHARA Akifumi

  Division of Applied Life Sciences, Graduate School of Agriculture, Kyoto University

• IKAWA Yasuyuki

  Division of Applied Life Sciences, Graduate School of Agriculture, Kyoto University

• NAKAGAWA Yu

  Division of Applied Life Sciences, Graduate School of Agriculture, Kyoto University

• A.WENDER Paul

  Department of Chemistry, Stanford University

• Nakahara A

  Graduate School Of Agriculture Kyoto University

• Ikawa Yasuyuki

  Division Of Applied Life Sciences Graduate School Of Agriculture Kyoto University

• A.wender Paul

  Department Of Chemistry Stanford University

• Irie Kazuhiro

  Division Of Food Science And Biotechnology Graduate School Of Agriculture Kyoto University

• 入江 一浩

  Division Of Food Science And Biotechnology Graduate School Of Agriculture Kyoto University

• Nakagawa Yu

  Division Of Food Science And Biotechnology Graduate School Of Agriculture Kyoto University

• Tanaka Minoru

  Division Of Applied Life Sciences Graduate School Of Agriculture Kyoto University

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