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MetabolomicsLimited nutrient availability in the tumor microenvironment renders pancreatic tumors sensitive to allosteric IDH1 inhibitors

Nutrient-deprived conditions in the tumor microenvironment (TME) restrain cancer cell viability due to increased free radicals and reduced energy production. In pancreatic cancer cells, a cytosolic metabolic enzyme, wild-type isocitrate dehydrogenase 1 (wtIDH1), enables the adaptation to these co...

2022-04-29 | MTBLS4722 | MetaboLights
ProteomicsATP-competitive and allosteric inhibitors induce differential conformational changes at the autoinhibitory interface of Akt
We use HDX-MS to interrogate the AKT1 DrLink conformational changes upon binding AKT1 active site inhibitors A-443654, Capivasertib, and Uprosertib, Akt1 allosteric inhibitor MK-2206, and ADP.
ORGANISM(S): Homo sapiens (Human) 
2024-08-23 | PXD039028 | Pride
Akt1 drlink Atp competitive inhibitors Allosteric inhibitors Akt1 Protein kinase b Hdx-ms 
ProteomicsSmall Molecule Allosteric inhibitors of GPX4
Encouraged by the dependence of drug-resistant, metastatic cancers on GPX4, we examined biophysical mechanisms of GPX4 inhibition, which revealed an unexpected allosteric binding site. We found that this site was involved in native modulation of GPX4 activity. Binding of inhibitors to this allosteri...
ORGANISM(S): Homo Sapiens (ncbitaxon:9606) 
2022-10-12 | MSV000090526 | MassIVE
ProteomicsSelective inhibitors of JAK1 targeting a subtype-restricted allosteric cysteine
The JAK family of non-receptor tyrosine kinases includes four subtypes (JAK1, JAK2, JAK3, and TYK2) and is responsible for signal transduction downstream of diverse cytokine receptors. JAK inhibitors have emerged as important therapies for immuno(onc)ological disorders, but their use is limited by u...
ORGANISM(S): Homo sapiens (Human) Mus musculus (Mouse) 
2023-07-20 | PXD031384 | Pride
Abpp Pbmc Cysteine Allosteric Splenocyte Kinase Jak1 inhibitor 
ProteomicsSelective inhibitors of SARM1 targeting an allosteric cysteine in the autoregulatory ARM domain
The NAD hydrolase (NADase) SARM1 acts as a central executioner of programmed axon death and is a possible therapeutic target for neurodegenerative disorders. While orthosteric inhibitors of SARM1 have been described, this multi-domain enzyme is also subject to intricate forms of autoregulation, sugg...
ORGANISM(S): Homo sapiens (Human) 
2022-08-22 | PXD035400 | Pride
Covalent Chemical proteomics Allosteric inhibition Axonopathy Neurodegeneration 
GenomicsNovel IDH1 Mutant Inhibitors for Treatment of Acute Myeloid Leukemia (ERRBS)
Neomorphic mutations in isocitrate dehydrogenase 1 (IDH1) are driver mutations in acute myeloid leukemia (AML) and other cancers. We report the development of new allosteric inhibitors of mutant IDH1. Crystallographic and biochemical results demonstrated that compounds of this chemical series bind t...
ORGANISM(S): Homo sapiens 
2015-09-21 | E-GEOD-72247 | biostudies-arrayexpress
GenomicsAllosteric HSP70 inhibitors perturb mitochondrial proteostasis and overcome proteasome inhibitor resistance in multiple myeloma
Allosteric HSP70 inhibitors perturb mitochondrial proteostasis and overcome proteasome inhibitor resistance in multiple myeloma
PRJNA625299 | ENA
TranscriptomicsNovel IDH1 Mutant Inhibitors for Treatment of Acute Myeloid Leukemia (expression)
Neomorphic mutations in isocitrate dehydrogenase 1 (IDH1) are driver mutations in acute myeloid leukemia (AML) and other cancers. We report the development of new allosteric inhibitors of mutant IDH1. Crystallographic and biochemical results demonstrated that compounds of this chemical series bind t...
ORGANISM(S): Homo sapiens 
2015-09-21 | E-GEOD-72152 | biostudies-arrayexpress
TranscriptomicsmTOR inhibitors synergistically induce regression, reversal of gene expression and autophagy in hepatocellular carcinoma
The mTOR-allosteric inhibitor, RAD001, in combination with a PI3K/mTOR ATP-site competitive inhibitor, BEZ235, causes gene reprogramming, autophagy and tumor regression, in a mouse model approximating human HCC with poor prognosis, leading to an investigator Phase 1B-2 clinical trial. Comparative st...
ORGANISM(S): Mus musculus 
2012-07-11 | E-GEOD-37129 | biostudies-arrayexpress
GenomicsRNA-seq of prostate cancer cell lines with acquired resistance to AKT inhibitors GDC-0068 (ATP competitive) or MK206 (allosteric)
RNA-seq of prostate cancer cell lines with acquired resistance to AKT inhibitors GDC-0068 (ATP competitive) or MK206 (allosteric)
PRJNA578702 | ENA
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