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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
The allosteric landscape of the Src kinase
Allosteric and Energetic Remodeling by Protein Domain Extensions
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
Global mapping of the energetic and allosteric landscapes of protein binding domains
Enzymes catalyze the reactions of life and are the targets of nearly all small molecule drugs. Most drugs inhibit enzymes by binding to conserved active sites, causing problems of specificity and toxicity. Targeting regulatory allosteric sites can increase specificity, overcome drug resistance and t...
ORGANISM(S): Homo sapiens Saccharomyces cerevisiae 
2024-04-27 | GSE247740 | GEO
Seven complete comparative maps of allosteric mutations in a protein family
ER aminopeptidase 1 (ERAP1) is an ER-resident aminopeptidase that excises N-terminal residues off peptides that then bind onto Major Histocompatibility Complex I molecules (MHC-I) and indirectly modulates adaptive immune responses. ERAP1 contains an allosteric regulatory site that accommodates the C...
ORGANISM(S): Homo sapiens (Human) 
2023-11-21 | PXD039584 | Pride
HDX-MS was used to establish that conformational-inhibition-signals extended from the TPR-domain to the U-box of CHIP. This underscores inter-domain allosteric regulation of CHIP by the core molecular chaperones. Defining the chaperone-associated TPR-domain of CHIP as a manager of inter-domain commu...
ORGANISM(S): Homo Sapiens (ncbitaxon:9606) 
2015-07-30 | MSV000079205 | MassIVE
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