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Drug-Target Interaction

Drug

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PubChem ID:4713
Structure:
Synonyms:
"2′-amino-3′-methoxyflavone"
167869-21-8
2′-Amino-3′-methoxyflavone
2'-AMINO-3'-METHOXYFLAVONE
2-(2'-amino-3'-methoxyphenyl)oxanaphthalen-4-one
2-(2-Amino-3-methoxyphenyl)-4H-1-benzopyran-4-one
2-(2-Amino-3-methoxyphenyl)-chromen-4-one
2-(2-amino-3-methoxyphenyl)chromen-4-one
4H-1-Benzopyran-4-one, 2-(2-amino-3-methoxyphenyl)-
4H-1-Benzopyran-4-one, 2-(2-amino-3-methoxyphenyl)- & Z-100
AC1L1ISD
AC1Q6AK0
AIDS-220091
AIDS220091
AR-1C6511
BCBcMAP01_000049
Bio1_000475
Bio1_000964
Bio1_001453
Bio2_000338
Bio2_000818
BiomolKI2_000011
BiomolKI_000001
BIP0711
BMK1-B1
BRD-K62810658-001-05-6
BSPBio_000996
C093973
CCG-100605
CHEBI:150222
CHEMBL35482
EC-000.2425
EU-0101028
HMS1362B17
HMS1792B17
HMS1990B17
HMS3229M08
HMS3263M17
IDI1_002093
IN1172
KBio2_000336
KBio2_002904
KBio2_005472
KBio3_000671
KBio3_000672
KBioGR_000336
KBioSS_000336
Lopac-P-215
Lopac0_001028
LS-182409
MolPort-000-005-902
NCGC00015790-01
NCGC00015790-02
NCGC00015790-03
NCGC00015790-04
NCGC00015790-05
NCGC00015790-06
NCGC00015790-07
NCGC00015790-08
NCGC00025045-01
NCGC00025045-02
NCGC00025045-03
NCGC00025045-04
NCGC00025045-05
NCGC00179347-01
nchembio.282-comp4
NCI60_028554
NSC679828
P-215
P215_SIGMA
PD 098059
PD 98,059
PD 98059
PD 98059 & Z-100
PD 98059, PD98059
PD-098059
PD-98059
PD098059
PD09859
PD98059
PD98059-Supplied by Selleck Chemicals
S1177_Selleck
SMP2_000052
Tocris-1213
ZINC01420826

Target

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Uniprot ID:TERT_HUMAN
Synonyms:
HEST2
Telomerase catalytic subunit
Telomerase reverse transcriptase
Telomerase-associated protein 2
TP2
EC-Numbers:2.7.7.49
Organism:Homo sapiens
Human
PDB IDs:2BCK
Structure:
2BCK

Binding Affinities:

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

References:

14706142
To inhibit ERK for enhancing chemotherapy sensitivity of drug-resistance cell lines of leukemia and ovarian carcinoma. Deng-Ju Li; Yao-Zhen Zhang; Wei Huang; Fan-Kai Meng (2003) Zhongguo shi yan xue ye xue za zhi / Zhongguo bing li sheng li xue hui display abstract
The aim was to study the roles of extracellular regulated protein kinases (ERK) and telomerase activity in drug resistance of human leukemia and ovarian carcinoma cells. Flow cytometry was used to analyze apoptosis rate. Telomere repeat amplification protocol (TRAP) and bioluminescence analysis method were used for detection of telomerase activity. The phosphorylated ERK(1/2) protein expression was observed by Western blot method. The results showed that the specific inhibitor PD98059 of ERK kinase 1 (MEK(1)) enhanced the sensitivity of HL-60/E6 leukemia cell lines to harringtonine (HRT) or COC1/DDP ovarian carcinoma cell lines to cis-dichlorodiamine platinum (DDP). Both PD98059 and chemotherapy drugs HRT and DDP reduced the phosphorylated ERK(1) and ERK(2) protein expression level, and down-regulated the telomerase activity. The sole action of each was inferior to the combination action of PD98059 and HRT or DDP. In conclusion, ERK and telomerase serve a function to some extent in drug resistance of leukemia and ovarian carcinoma cells. The inhibition of ERK signal transduction pathways led to reduction of phosphorylated ERK(1) and ERK(2) protein expression level, and successionally down-regulated the telomerase activity. The final result was to enhance the sensitivity of HL-60/E6 to HRT or COC1/DDP to DDP.