Ko143

E852343

Ko143 is a potent and selective small-molecule inhibitor of the breast cancer resistance protein (BCRP/ABCG2) efflux transporter used in research to study and overcome multidrug resistance.

All labels observed (1)

Label Occurrences
Ko143 canonical 1

How this entity was disambiguated

Statements (46)

Predicate Object
instanceOf ABCG2 inhibitor ⓘ
BCRP inhibitor ⓘ
chemosensitizer ⓘ
research chemical ⓘ
small-molecule inhibitor ⓘ
affects drug efflux mediated by BCRP ⓘ
associatedWith multidrug resistance in oncology research ⓘ
discoveredAs derivative of fungal toxin fumitremorgin C ⓘ
effect increases intracellular accumulation of BCRP substrates ⓘ
reverses BCRP-mediated drug resistance ⓘ
fieldOfUse drug transport and disposition research ⓘ
oncology research ⓘ
pharmacology research ⓘ
hasAdvantage reduced neurotoxicity compared with fumitremorgin C in preclinical studies ⓘ
hasProperty high potency against BCRP ⓘ
high selectivity for BCRP over other ABC transporters ⓘ
non-competitive BCRP inhibition (commonly reported) ⓘ
hasSynonym Ko 143 ⓘ
Ko-143 ⓘ
mechanismOfAction inhibition of BCRP/ABCG2 efflux transporter activity ⓘ
roleInResearch positive control in BCRP inhibition assays ⓘ
reference inhibitor in transporter selectivity panels ⓘ
tool compound to validate BCRP involvement in drug transport ⓘ
selectivityProfile more selective for BCRP than for MRP1 ⓘ
more selective for BCRP than for P-glycoprotein ⓘ
speciesStudiedIn human-derived cell lines ⓘ
mouse models ⓘ
rat models ⓘ
targets ABCG2 ⓘ
linked to: ABCG2 gene

BCRP ⓘ
breast cancer resistance protein ⓘ
linked to: BCRP
transportersComparedWith MRP1 (ABCC1) ⓘ
P-glycoprotein (ABCB1) ⓘ
linked to: P-glycoprotein
usedFor in vitro transporter inhibition assays ⓘ
in vivo transporter inhibition studies ⓘ
overcoming multidrug resistance in cancer models ⓘ
study of multidrug resistance mechanisms ⓘ
usedIn animal models of drug resistance ⓘ
cancer cell line studies ⓘ
transfected cell systems expressing ABCG2 ⓘ
usedTo assess drug–drug interaction risk via BCRP inhibition ⓘ
characterize pharmacokinetics of BCRP substrates ⓘ
usedWith BCRP substrate chemotherapeutic agents ⓘ
SN-38 ⓘ
mitoxantrone ⓘ
topotecan ⓘ

How these facts were elicited

Referenced by (1)

Full triples — surface form annotated when it differs from this entity's canonical label.

BCRP → inhibitedBy → Ko143 ⓘ