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ProteomicsRapid and direct control of target protein levels with VHL-recruiting dTAG molecules
Chemical biology strategies for directly perturbing protein homeostasis including the degradation tag (dTAG) system provide temporal advantages over genetic approaches and improved selectivity over small molecule inhibitors. We describe dTAGV-1, an exclusively selective VHL-recruiting dTAG molecule,...
ORGANISM(S): Homo sapiens (Human) 
2020-09-21 | PXD018937 | Pride
Proteomics Protac Dtag Degraders 
ProteomicsDiscovery of covalent CDK14 inhibitors with pan-TAIRE family specificity
Cyclin dependent kinase 14 (CDK14) and other TAIRE family kinases (CDKs 15-18) are proteins that lack functional annotation but are frequent off-targets of clinical kinase inhibitors. In this study we develop and characterize FMF-04-159-2, the first tool compound that specifically targets CDK14 cova...
ORGANISM(S): Homo sapiens (Human) 
2019-03-29 | PXD012692 | Pride
Covalent inhibitor Druggable genome Mitosis Taire kinase Cell-cycle Cdk14 
ProteomicsProteomic analysis of a molecular glue to redirect lysine acetyltransferase for selective induction of cell death
Lysine acetyltransferases (KATs) such as p300 and CBP regulate gene networks in healthy and malignant cells by scaffolding transcriptional machinery and by acetylating chromatin and transcription factors (TFs). In certain cancers including diffuse large B cell lymphomas, they contribute to tumor sup...
ORGANISM(S): Homo sapiens (Human) 
2026-07-21 | PXD059919 | Pride
Human Cancer Transcription Induced proximity Molecular glues 
GenomicsCDK7-dependent Transcriptional Addition in Basal-like Breast Cancer
Basal-like breast cancer (BBC) is a highly aggressive form of breast cancer that exhibits extremely high levels of genetic complexity and yet a relatively uniform transcriptional program. We postulate that BBC might be highly dependent on uninterrupted transcription of a key set of genes within this...
ORGANISM(S): Homo sapiens 
2015-01-23 | E-GEOD-65201 | biostudies-arrayexpress
ProteomicsMudPIT analysis of STRN4 interacting proteins from HEK TER cells expressing either SV40 ST or GFP
HEK TER cells expressing either SV40 ST or GFP (30 x 15-cm diameter plates) were harvested with lysis buffer (20 mM imidazole HCl, 2 mM EDTA, 2 mM EGTA, pH 7.0 with 10 ug/mL each of aprotinin, leupeptin, pepstatin, 1 mM benzamidine, and 1 mM PMSF). The clarified cell extract was incubated overnight ...
ORGANISM(S): Homo Sapiens (ncbitaxon:9606) 
2019-12-05 | MSV000084662 | MassIVE
ProteomicsEffect of Kinase Inhibitors on Intraerythrocytic Plasmodium falciparum Phosphoproteome
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
TranscriptomicsTargeting transcriptional dependencies in cancer using a covalent CDK7 inhibitor (expression)
Cyclin-dependent kinase 7 (CDK7) plays a critical role in the general regulation of RNA polymerase II-mediated transcription. However, the absence of selective CDK7 inhibitors has hindered the ability to investigate the consequences of acute and prolonged inhibition of CDK7 under normal and patholo...
ORGANISM(S): Homo sapiens 
2014-06-22 | E-GEOD-50624 | biostudies-arrayexpress
GenomicsTargeting Transcriptional Addictions in Small Cell Lung Cancer with a Covalent CDK7 Inhibitor (ChIP-seq)
Small cell lung cancer (SCLC) is an aggressive disease with high mortality. The identification of effective pharmacological strategies to target SCLC biology represents an urgent need. Using a high-throughput cellular screen of a diverse chemical library we observe that SCLC is sensitive to transcri...
ORGANISM(S): Homo sapiens 
2014-10-23 | E-GEOD-62412 | biostudies-arrayexpress
TranscriptomicsTargeting Transcriptional Addictions in Small Cell Lung Cancer with a Covalent CDK7 Inhibitor (Affymetrix)
Small cell lung cancer (SCLC) is an aggressive disease with high mortality. The identification of effective pharmacological strategies to target SCLC biology represents an urgent need. Using a high-throughput cellular screen of a diverse chemical library we observe that SCLC is sensitive to transcri...
ORGANISM(S): Homo sapiens 
2014-10-23 | E-GEOD-62609 | biostudies-arrayexpress
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