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Embryonic stem cells (ESCs) can be maintained in the naïve state through inhibition of Mek1/2 and Gsk3 (2i). A relevant effect of 2i is the inhibition of Cdk8/19, which are negative regulators of the Mediator complex, responsible for the activity of enhancers. Inhibition of Cdk8/19 (Cdk8/19i) stimul...
2021-02-10 | MTBLS301 | MetaboLights
Fibroblast growth factor receptors (FGFRs) can act as driving oncoproteins in certain cancers due to mutation, over-expression or activating gene fusions and are therefore attractive drug targets. Here we have characterized tumour cell responses to three new inhibitors of FGFR1-3, AZ12576089, AZ129...
ORGANISM(S): Homo sapiens 
Three flasks of asynchronous blood stage P. falciparum Dd2 culture were grown to ~15% parasitemia, 4% hematocrit using the Trager- Jensen method. Per biological replicate, parasites were treated with 5 x EC50 or EC90 of compound depending on the slope of the EC50 curve for 3 hours. Compounds are DC-...
ORGANISM(S): Homo Sapiens (ncbitaxon:9606) Plasmodium Falciparum Dd2 (ncbitaxon:57267) 
2023-04-03 | MSV000091619 | MassIVE
Kinase inhibitors (KIs) are important cancer drugs but often display polypharmacology that is molecularly not understood. This disconnect is particularly apparent in cancer entities such as sarcomas for which the oncogenic drivers are often not clear. To investigate more systematically how the cellu...
ORGANISM(S): Homo Sapiens (ncbitaxon:9606) 
2023-01-11 | MSV000091043 | MassIVE
The clinical efficacy of EGFR kinase inhibitors is limited by the development of drug resistance. The irreversible EGFR kinase inhibitor WZ4002 is effective against the most common mechanism of drug resistance mediated by the EGFR T790M mutation. Here we show that in multiple complementary models ha...
ORGANISM(S): Homo sapiens 
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