Vacuolar-type H(+)-ATPase inhibitory activity of synthetic analogues of the concanamycins: is the hydrogen bond network involving the lactone carbonyl, the hemiacetal hydroxy group, and the C-19 hydroxy group essential for the biological activity of the concanamycins?
Synthetic analogue of the concanamycins, which lacks the hydrogen bond network existing in the concanamycin structure, retains vacuolar-type H(+)-ATPase (V-ATPase) inhibitory activity and induces apoptosis to cancer cells that overexpressing epidermal growth factor receptors (EGFR).
Yoshimoto
Yuya
Y
Department of Bioscience and Informatics, Faculty of Science and Technology, Keio University, 3-14-1 Hiyoshi, Kohoku-ku, Yokohama 223-8522, Japan.
Jyojima
Takaaki
T
Arita
Tsuyoshi
T
Ueda
Minoru
M
Imoto
Masaya
M
Matsumura
Shuichi
S
Toshima
Kazunobu
K
D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology; D004815:Epidermal Growth Factor / Q000494:pharmacology; D066246:ErbB Receptors / Q000502:physiology; D006801:Humans; D006860:Hydrogen Bonding; D006863:Hydrogen-Ion Concentration; D018942:Macrolides; D009363:Neoplasm Proteins; D013329:Structure-Activity Relationship; D025262:Vacuolar Proton-Translocating ATPases / Q000037:antagonists & inhibitors*
D000900:Anti-Bacterial Agents; D004791:Enzyme Inhibitors; D018942:Macrolides; D009363:Neoplasm Proteins; C076477:concanamycin F; D004815:Epidermal Growth Factor; D066246:ErbB Receptors; D025262:Vacuolar Proton-Translocating ATPases