Daurisoline derivatives inhibit the ability of calmodulin to stimulate cyclic nucleotide phosphodiesterase activity.
Daurisoline alkaloid derivatives were found to be potent calmodulin (CaM) antagonists. The ability of daurisoline derivatives to attenuate the stimulatory effect on calmodulin activated cyclic nucleotides phosphodiesterase (CaM-PDE) was studied. These compounds did not inhibit the basal activity of this enzyme. The hydrophobicity of these compounds was related to their inhibitory potency. It is suggested that such drugs bind directly to calmodulin in a Ca2(+)-dependent fashion, as indicated by their ability to change calmodulin fluorescence.
Hu
Z Y
ZY
Division of Biochemistry, China Pharmaceutical University, Jiangsu.
Xu
L M
LM
Sun
Y
Y
Chen
S L
SL
Cai
H M
HM
D000470:Alkaloids / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D000818:Animals; D044182:Benzylisoquinolines; D001665:Binding Sites; D002147:Calmodulin / Q000037:antagonists & inhibitors* / Q000378:metabolism* / Q000494:pharmacology; D066298:In Vitro Techniques; D015394:Molecular Structure; D013050:Spectrometry, Fluorescence
D000470:Alkaloids; D044182:Benzylisoquinolines; D002147:Calmodulin; C023968:daurisoline