Home
Drugs
Targets
Pathways
Ontologies
Cyp450s
Adv.search
Help/FAQ

Drug-Target Interaction

Drug

show drug details
PubChem ID:6437373
Structure:
Synonyms:
(4R,5R)-1,4,5,6-Tetrahydro-5-hydroxy-4-((E)-(3S)-3-hydroxy-1-octenyl)-1-phenylcyclopenta(b)pyrrole-2-valeric acid
6,9-deepoxy-6,9-(phenylimino)-delta (6,8)pgI1
6,9-desepoxy-6,9-(phenylimino)-delta-(6,8)prostaglandin I1
79672-88-1
C26H35NO4
Cyclopenta(b)pyrrole-2-pentanoic acid,
Cyclopenta(b)pyrrole-2-pentanoic acid, 1,4,5,6-tetrahydro-5-hydroxy-4-((1E,3S)-3-hydroxy-1-octenyl)-1-phenyl-, (4R,5R)-
Cyclopenta(b)pyrrole-2-pentanoic acid, 1,4,5,6-tetrahydro-5-hydroxy-4-(3-hydroxy-1-octenyl)-1-phenyl-, (4R-(4alpha(1E,3S*),5beta))-
D05498
LS-177493
Piriprost
Piriprost (USAN/INN)
Piriprost [USAN:INN]
Piriprostium [Latin]
U 60,257
U 60257
U 60257B
U-60,257
U-60257

Target

show target details
Uniprot ID:LOX5_HUMAN
Synonyms:
5-lipoxygenase
5-LO
Arachidonate 5-lipoxygenase
EC-Numbers:1.13.11.34
Organism:Homo sapiens
Human
PDB IDs:2ABV
Structure:
2ABV

Binding Affinities:

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

References:

2117290
Effects of the 5-lipoxygenase inhibitors AA-863 and U-60,257 on human glioma cell lines.. I Gáti; M Bergström; K Csóka; C Muhr; J Carlsson (1990) Prostaglandins, leukotrienes, and essential fatty acids display abstract
The effects of two specific 5-lipoxygenase inhibitors AA-863 and U-60,257 (piriprost) on the growth of two human glioma cell lines, U-343 MGa and U-251 MG were investigated. Both monolayer cultured cells and spheroids were studied. The results of the monolayer studies showed potent and dose dependent inhibitory effects on the proliferation of glioma cells (IC50/one week treatment/of AA-863: 9.0 microM, IC50 of U-60,257: 40.0 microM). The experiments made on the tumor spheroids suggested an inhibitory effect on proliferation and volume growth already at lower doses (AA-863: 0.4-2.0 microM, U-60,257: 1.0-5.0 microM), a dose range where effects were not found in monolayers. At higher doses (AA-863: 10.0-30.0 microM, U-60,257: 30.0-90.0 microM) the experiments with spheroids failed to demonstrate a further inhibitory effect on spheroid volume, probably attributed to phenomena such as swelling of cells, dissociation of spheroid structure and development of necrosis. The clearly dose dependent inhibitory effect on the proliferation of human glioma cells in monolayer culture and the inhibitory effects on spheroid growth with these specific inhibitors indicate a role for lipoxygenase products in the growth of gliomas.