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Drug-Target Interaction

Drug

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PubChem ID:4592
Structure:
Synonyms:
"insolution™ olomoucine"
101622-51-9
2-(2-Hydroxyethylamino)-6-benzylamino-9-isopropylpurine
2-(2-Hydroxyethylamino)-6-benzylamino-9-methylpurine
2-(Hydroxyethylamino)-6-benzylamino-9-methylpurine
2-[[6-(benzylamino)-9-methylpurin-2-yl]amino]ethanol
2-[[9-methyl-6-(phenylmethylamino)purin-2-yl]amino]ethanol
2-[[9-Methyl-6-[(phenylmethyl)amino]-9H-purin-2-yl]amino]-ethanol
2-{[6-(benzylamino)-9-methyl-9h-purin-2-yl]amino}ethanol
4erk
6-(Benzylamino)-2-(2-hydroxyethylamino)-9-methylpurine
6-Benzylamino-2-(2-hydroxyethylamino)-9-methylpurine
6-benzylamino-2-[2-hydroxyethylamino]-9-methylpurine
AC1L1IID
AC1Q4XZU
AIDS-007464
AIDS007464
AKOS005145988
AR-1D7506
BCBcMAP01_000205
Bio1_000336
Bio1_000825
Bio1_001314
Bio2_000335
Bio2_000815
BiomolKI2_000052
BiomolKI_000046
BMK1-E10
BRD-K82731415-001-03-9
BRD-K82731415-001-04-7
BSPBio_000990
C090046
CBiol_002050
CCG-100650
CHEBI:44661
CHEMBL280074
CPD-5442
DB02116
Ethanol, 2-[[9-methyl-6-[(phenylmethyl)amino]-9H-purin-2-yl]amino]-
EU-0100883
HMS1362B11
HMS1792B11
HMS1990B11
HMS3262B08
IDI1_002090
IN1179
IN1182
InSolution&trade
InSolution™ Olomoucine
KBio2_000330
KBio2_002898
KBio2_005466
KBio3_000659
KBio3_000660
KBioGR_000330
KBioSS_000330
Kinome_2870
Lopac-O-0886
Lopac0_000883
MolPort-003-849-700
NCGC00015763-01
NCGC00015763-02
NCGC00015763-03
NCGC00015763-04
NCGC00015763-05
NCGC00015763-06
NCGC00015763-07
NCGC00015763-08
NCGC00015763-09
NCGC00025096-01
NCGC00025096-02
NCGC00025096-03
NCGC00025096-04
NCGC00025096-05
NCGC00025096-06
NCGC00025096-07
NCI60_022916
NSC666096
O 0886
O0886_SIGMA
OLO
Olomoucine
SMP1_000281
ST50298830
ST5298830
Tocris-1284
UPCMLD-DP136
UPCMLD-DP136:001
UPCMLD-DP136:002
ZINC01641925

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:
----

References:

10871858
Cdk inhibitors, roscovitine and olomoucine, synergize with farnesyltransferase inhibitor (FTI) to induce efficient apoptosis of human cancer cell lines.. H Edamatsu; C L Gau; T Nemoto; L Guo; F Tamanoi (2000) Oncogene display abstract
Farnesyltransferase inhibitor (FTI) induces apoptosis of transformed cells. This involves changes in mitochondria, including decrease of mitochondrial membrane potential and the release of cytochrome c. The released cytochrome c then induces events leading to the activation of caspase-3. In this study, we report that purine derivative cyclin-dependent kinase (Cdk) inhibitors, roscovitine and olomoucine, dramatically enhance this FTI-induced apoptosis of human cancer cell lines. We noticed the synergy between Cdk inhibitors and FTI through our screen to identify compounds that enhance FTI-induced apoptosis of promyelocytic leukemic cell line HL-60. The Cdk inhibitors by themselves do not induce apoptosis at the concentrations used. Roscovitine synergizes with FTI to release cytochrome c from mitochondria. In addition, we detected synergistic effects of FTI and roscovitine to inhibit hyperphosphorylation of retinoblastoma protein. Enhancement of FTI-induced apoptosis by roscovitine is not unique to HL-60 cells, since similar synergy was observed with a leukemic cell line CEM and a prostate cancer cell line LNCaP. In LNCaP cells, in addition to roscovitine and olomoucine, phophatidylinositol 3-kinase (PI 3-kinase) inhibitor, LY294002, was effective in enhancing FTI-induced apoptosis. However, the effects of roscovitine appear to be distinct from those of LY294002, since roscovitine did not affect Akt activity while LY294002 significantly decreased the activity of Akt. Our finding of the synergy between FTI and Cdk inhibitor is significant for understanding the mechanism of action of FTI as well as for clinical use of FTI.