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Drug-Target Interaction

Drug

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PubChem ID:1645
Structure:
Synonyms:
253014_ALDRICH
253014_SIGMA
3-AB
3-AB cpd
3-ABA
3-amino benzamide
3-Amino-benzamide
3-Aminobenzamide
3-Aminobenzimide
3544-24-9
3AB
4-14-00-01094 (Beilstein Handbook Reference)
A 0788
A0630
A0788_SIGMA
AC-10266
AC1L1BX0
AC1Q4ZAY
AC1Q4ZAZ
AG-F-22659
AIDS-059768
AIDS059768
AKOS000118163
Ambap3139
ARONIS015032
BB_SC-7456
BCBcMAP01_000186
Benzamide, 3-amino-
Benzamide, 3-amino- (9CI)
Benzamide, m-amino-
Bio1_000466
Bio1_000955
Bio1_001444
Bio2_000152
Bio2_000632
Biochem Biophys Res Commun 225: 826
BRN 2802373
BSPBio_001432
BSPBio_002603
C025160
C7H8N2O
CCG-39623
CCRIS 3925
CHEMBL81977
cMAP_000029
DivK1c_000717
EINECS 222-586-9
EU-0100043
HMS1361H14
HMS1791H14
HMS1989H14
HMS3260I07
HMS502D19
HSCI1_000265
HSDB 7581
I01-3900
IDI1_000717
IDI1_033902
INO-1001-Supplied by Selleck Chemicals
INO1001, INO-1001
KBio1_000717
KBio2_000152
KBio2_001972
KBio2_002355
KBio2_002720
KBio2_004540
KBio2_004923
KBio2_005288
KBio2_007108
KBio2_007491
KBio3_000303
KBio3_000304
KBio3_001823
KBio3_002834
KBioGR_000152
KBioGR_001512
KBioGR_002355
KBioSS_000152
KBioSS_001972
KBioSS_002358
Lopac-A-0788
Lopac0_000043
LS-25343
m-amino benzamide
m-Aminobenzamide
meta-aminobenzamide
MLS002153497
MolPort-000-150-925
NCGC00015034-01
NCGC00015034-02
NCGC00015034-03
NCGC00015034-04
NCGC00015034-05
NCGC00015034-06
NCGC00015034-07
NCGC00015034-08
NCGC00024792-01
NCGC00024792-02
NCGC00024792-03
NCGC00024792-04
NCGC00024792-05
NCGC00024792-06
NINDS_000717
NSC 36962
NSC36962
Oprea1_589004
PARP Inhibitor I, 3-ABA
S1132_Selleck
SMP2_000089
SMR000375902
SPBio_001514
Spectrum2_001577
Spectrum3_000972
Spectrum4_001096
Spectrum5_001459
Spectrum_001492
STK730785
Tocris-0788
UPCMLD-DP128
UPCMLD-DP128:001
ZINC00157165

Target

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Uniprot ID:POKL_HUMAN
Synonyms:
Putative HERV-K_Xq28 provirus ancestral Pol protein
EC-Numbers:2.7.7.49
Organism:Homo sapiens
Human
PDB IDs:-

Binding Affinities:

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

References:

15370971
Pharmacological inhibition of DNA repair enzymes differentially modulates telomerase activity and apoptosis in two human leukaemia cell lines.. D Dubner; M del Rosario Pérez; S Michelin; M Bourguignon; P Moreau; E D Carosella; P Gisone (2004) International journal of radiation biology display abstract
PURPOSE: To investigate the effect of wortmannin and 3-aminobenzamide (3-AB) on telomerase activity and apoptosis in two human leukaemia cells. MATERIALS AND METHODS: MOLT-4 (p53-wild type) and KG1a (p53-null) cells were irradiated with gamma-rays (3 Gy at 1.57 Gy min(-1)) and the effects of wortmannin and 3-AB were evaluated. Telomerase activity was measured by polymerase chain reaction and the expression of human telomerase reverse transcriptase, human telomerase RNA and telomerase-associated protein 1 was assessed by reverse transcriptase-polymerase chain reaction. Apoptosis was evaluated by fluorescence microscopy and flow cytometry. RESULTS: A radiation-induced up-regulation of telomerase activity was observed from 4 h post-irradiation in both cell lines. This up-regulation was abrogated by wortmannin and 3-AB. Telomerase activity was maximal 24 h post-irradiation, coinciding with an accumulation of human telomerase reverse transcriptase mRNA. Apoptosis and G2/M arrest were evident from 4 h post-irradiation in MOLT-4 cells. KG1a cells exhibited a G2/M block at 24 h post-irradiation and apoptosis increased between 24 and 48 h post-irradiation. 3-AB abolished G2/M blockage and enhanced radiation-induced apoptosis in both cell lines, while wortmannin increased apoptosis only in MOLT-4 cells. CONCLUSIONS: 3-AB inhibits the radiation-associated telomerase activity increase and enhances apoptosis in MOLT-4 and KG1a cells. Wortmannin, which also inhibits the radiation-associated telomerase activity increase in both cell lines, does not modify radiation-induced apoptosis in KG1a cells. DNA repair enzymes might be selective targets for enhancing radiosensitivity in certain tumour cells.