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Drug-Target Interaction

Drug

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PubChem ID:6440856
Structure:
Synonyms:
(2R)-2-[(E)-2-phenylethenyl]-2,3-dihydropyran-6-one
(6r)-()-goniothalamin
(6R)-(+)-Goniothalamin
17303-67-2
2H-Pyran-2-one, 5,6-dihydro-6-(2-phenylethenyl)-, (S-(E))-
2H-Pyran-2-one, 5,6-dihydro-6-(2-phenylethenyl)-, (S-(E))- (9CI)
2h-pyran-2-one, 5,6-dihydro-6-styryl-, (5s)-()-
2H-Pyran-2-one, 5,6-dihydro-6-styryl-, (5S)-(+)-
AC1O5UBY
CCRIS 9005
CHEMBL464443
CID6440856
Goniothalamin
Goniothalamine
LS-127438
ZINC01686158

Target

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Uniprot ID:ICE_DROME
Synonyms:
Caspase
drICE
EC-Numbers:3.4.22.-
Organism:Drosophila melanogaster
Fruit fly
PDB IDs:-

Binding Affinities:

Ki: Kd:Ic 50:Ec50/Ic50:
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References:

10462048
Caspases-3 and -7 are activated in goniothalamin-induced apoptosis in human Jurkat T-cells.. S H Inayat-Hussain; A B Osman; L B Din; A M Ali; R T Snowden; M MacFarlane; K Cain (1999) FEBS letters display abstract
Goniothalamin, a plant styrylpyrone derivative isolated from Goniothalamus andersonii, induced apoptosis in Jurkat T-cells as assessed by the externalisation of phosphatidylserine. Immunoblotting showed processing of caspases-3 and -7 with the appearance of their catalytically active large subunits of 17 and 19 kDa, respectively. Activation of these caspases was further evidenced by detection of poly(ADP-ribose) polymerase cleavage (PARP). Pre-treatment with the caspase inhibitor benzyloxycarbonyl-Val-Ala-Asp fluoromethyl ketone (Z-VAD.FMK) blocked apoptosis and the resultant cleavage of these caspases and PARP. Our results demonstrate that activation of at least two effector caspases is a key feature of goniothalamin-induced apoptosis in Jurkat T-cells.