8-1．簡単な解説
GABA（r-アミノ酪酸）代謝阻害剤（ギャバクリンと4,5-ジヒドリキシ安息香酸）を単離し、作用を明らかにした（原著論文1-4等）。プロスタグランジン合成酵素阻害剤（チエラビンＡとＣ等）を単離して作用機構を解明した（原著論文5-7等)。アセチル－CoAカルボキシラーゼ阻害剤として2-テトラデカニルグルタミン酸を単離して作用機構を研究した（原著論文8，10等）。グリセルアルデヒド3P-脱水素酵素阻害剤（コニンギン酸）を単離して性質と作用を特定した（原著論文9，11－13，15，17等）。その他にポリガラクチュロナーゼ阻害剤としてクロガリン（原著論文14等）、アセチル-CoAカルボキシラーゼ阻害剤として2-テトラデカニルグルタレート（原著論文18等）、プロテインプレニレーション阻害剤としてパチュリン(原著論文13等)、15-リポギシラネース阻害剤としてオロボール（原著論文19等）等を単離した。
8-2. 原著論文(19編)
- 1) Kobayashi K, Miyazawa S, Endo A. Isolation and inhibitory activity of gabaculine, a new potent inhibitor of γ-aminobutyrate aminotransferase produced by a Steptomyces. FEBS Lett 1977; 76: 207-210.
- 2) Endo A, Kitahara N. cis and trans-Aconitic acids as inhibitors of glutamate decarboxylase. Hoppe-Seyler’s Z Physiol Chem 1977; 358: 1365-1368.
- 3) Endo A, Kitahara N, Oka H, Miguchi-Fukazawa Y, Terahara A. Isoation of 4,5-dihydroxyisophthalic acid and related compounds. J Antibiot 1978; 34: 1351-1354.
- 4) Endo A, Kitahara N. Inhibition of brain decardoxylase by 4,5- dihydroxyisophthalic acid and related compounds. J Antibiot 1981; 34: 1351- 1354.
- 5) Kitahara N, Endo A. Xanthocillin X monomethyl ether, a potent inhibitor of prostaglandin biosynthesis produced by Thielavia terricola. J Antibiot 1981; 34:1556-1561.
- 6) Kitahara N, Endo A, Furuya K, Takahashi S. Thielavin A and B, new inhibitors of prostaglandin biosynthesis produced by Thielavia terricola. J Antibiot 1981; 34:1562-1568.
- 7) Sankawa U, Shibuya Y, Ebizuka Y, Noguchi H, Kinoshita Y, Iitaka Y, Endo A, Kitahara N. Depsids as potent inhibitors of prostaglandin biosynthesis: a new active site model for fatty acid cyclooxygenase. Prostaglandins 1982; 24: 21-34.
- 8) Endo A, Takeshima H, Kuwahara K. Acetyl-CoA carboxylase inhibitors from the fungus Congronella butreli. J Antibiot 1985; 38: 599-604.
- 9) Endo A, Hasumi K, Sakai K, Kanbe T. Specific inhibition of glyceraldehyde-3- phosphate dehydrogenase by koningic acid (heptelidic acid). J Antibiot 1985;38:920-925.
- 10) Takeshima H, Endo A, Wada K, Tanabe T. Inhibition of liver acetyl-coenzyme A carboxylase by 2-tetradecanylglutamate. J Antibiot 1986; 39: 275-280.
- 11) Sakai K, Hasumi K, Endo A. Inactivation of rabbit muscle glyceraldehyde-3- phosphate dehydrogenase by koningic acid. Biochim Biophys Acta 1988; 952: 297-303.
- 12) Sakai K, Hasumi K, Endo A. Two glyceradehyde-3-phosphate dehydrogenase isozymes from the konigic acid (heptelidic acid) producer Trichoderma koningii. Eur J Biochem 1990; 193: 195-202.
- 13) Sakai K, Hasumi K, Endo, A. Identification of koningic acid (heptelidic acid)-modified site in rabbit muscle glyceraldehyde-3-phosphate dehydrogenase. Biochim Biophys Acta 1991; 1077: 192-196.
- 14) Woo JT, Miura S, Murakawa S, Endo A. Chrogalin, a heat-stable glycoprotein that inhibits polygalacturonase: isolation, characterization and biological activity. J Ferment Bioeng 1991; 72: 7-10.
- 15) Kato M, Sakai K, Endo A. Konigic acid (heptelidic acid)-inhibition of glyceraldehyde-3-phosphate dehydrogenase from various sources. Biochim Biophys Acta 1992; 1120: 113-116.
- 16) Kataoka T, Magae J, Kasamo K, Yamanishi H, Endo A, Yamasaki M, Nagai K. Effects of prodigiosin 25-C on cultured cell lines: its similarity to mono- valent polyether ionophores and vacuolar type H+-ATPase inhibitors. J Antibiot 1992; 45: 1618-1625.
- 17) Watanabe H, Hasumi K, Fukushima Y, Sakai K, Endo A. Cloning of two isozymes of Trichoderma koningii glyceraldehyde-3-phoshate dehydrogenase with different sensitivity to koningic acid. Biochim Biophys Acta 1993; 1172: 43-48.
- 18) Miura S, Hasumi K, Endo A. Inhibition of protein prenylation by patulin. FEBS Lett 1993; 318: 88-90.
- 19) Kohyama T, Hasumi K, Endo A. Inhibition of 15-lipoxygenase by orobol. J Antibiot 1994; 47: 1069-1071.
