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Drug-Target Interaction

Drug

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PubChem ID:58035
Structure:
Synonyms:
(Z)-N-[2-(2,5-Dihydroxyphenyl)ethenyl]-formamide (cis Erbstatin)
100827-28-9
AC1L1O6Q
ERBSTATIN
Erbstatin, synthetic non-solvated
MLS000756834
N-[2-(2,5-dihydroxyphenyl)ethenyl]formamide
NCI60_004786
NCI60_017556
NSC610187
SMR000529090

Target

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Uniprot ID:Q62710_RAT
Synonyms:
Nitric oxide synthase
EC-Numbers:-
Organism:Rat
Rattus norvegicus
PDB IDs:-

Binding Affinities:

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

References:

7544862
Possible involvement of tyrosine kinase in the LPS-promoted initiation of L-arginine-induced relaxation of rat aorta mediated by induction of no synthase.. H Moritoki; T Hisayama; S Takeuchi; W Kondoh; Y Takeji (1995) Life sciences display abstract
Tyrosine kinase inhibitors herbimycin A, genistein and erbstatin analog prevented endotoxin (LPS)-promoted initiation of L-arginine (Arg)-induced relaxations and cGMP formation in rat thoracic aorta, which appear to be mediated by nitric oxide synthase expressed by LPS in the vascular smooth muscle. Similarly, interleukin-1 beta (IL-1 beta) triggered initiation of Arg-induced relaxation of the arteries. In addition, in the aortic smooth muscle cells cultured in the presence of Arg, LPS- or IL-1 beta-triggered accumulation of nitrite was suppressed by the tyrosine kinase inhibitors. These results suggest that tyrosine kinase is involved in the LPS- and IL-1 beta-promoted induction of nitric oxide synthase in the vascular smooth muscle, which in turn mediates production of NO from added Arg, thus stimulating formation of cGMP and causing relaxation. Alternatively, it is possible that LPS acts indirectly through cytokines such as IL-1 beta.