TY - JOUR
T1 - Isolation of a novel substrate-competitive tyrosine kinase inhibitor, desmal, from the plant Desmos chinensis
AU - Kakeya, Hideaki
AU - Imoto, Masaya
AU - Tabata, Yuji
AU - Iwami, Junko
AU - Matsumoto, Haruhiko
AU - Nakamura, Kazuo
AU - Koyano, Takashi
AU - Tadano, Kin ichi
AU - Umezawa, Kazuo
PY - 1993/4/5
Y1 - 1993/4/5
N2 - In the course of a screening program for tyrosine kinase inhibitors, the chloroform extract of a tropical plant, Desmos chinensis, strongly inhibited the enzyme activity. The active substance was purified by silica gel, gel filtration, and finally crystallized. The structure was elucidated by mass spectrometry and X-ray crystallography to be 8-formyl-2,5,7-trihydroxy-6-methylflavanone, and we named it desmal. Desmal competed with peptide substrate and non-competed with ATP. It inhibited tyrosine kinase in situ in epidermal growth factor (EGF) receptor-overexpressing NIH3T3 (ER 12) cells. It also inhibited EGF-induced inositol phosphate formation and morphological changes.
AB - In the course of a screening program for tyrosine kinase inhibitors, the chloroform extract of a tropical plant, Desmos chinensis, strongly inhibited the enzyme activity. The active substance was purified by silica gel, gel filtration, and finally crystallized. The structure was elucidated by mass spectrometry and X-ray crystallography to be 8-formyl-2,5,7-trihydroxy-6-methylflavanone, and we named it desmal. Desmal competed with peptide substrate and non-competed with ATP. It inhibited tyrosine kinase in situ in epidermal growth factor (EGF) receptor-overexpressing NIH3T3 (ER 12) cells. It also inhibited EGF-induced inositol phosphate formation and morphological changes.
KW - Desmos chinensis, Desmal
KW - Epidermal growth factor
KW - Tyrosine kinase
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U2 - 10.1016/0014-5793(93)80085-9
DO - 10.1016/0014-5793(93)80085-9
M3 - Article
C2 - 8458434
AN - SCOPUS:0027412301
VL - 320
SP - 169
EP - 172
JO - FEBS Letters
JF - FEBS Letters
SN - 0014-5793
IS - 2
ER -