Sort   by:  
 Page size 
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
ProteomicsTherapeutic potential of allosteric HECT E3 ligase inhibition
Supplemental proteomics data Abstract: Inhibition of ubiquitin E3-ligases is therapeutically attractive; however, the absence of an active-site pocket impedes computational approaches to inhibitor identification. In a large unbiased physical screen, we discovered inhibitors that bind a cryptic cavi...
ORGANISM(S): Homo sapiens (Human) 
2025-05-26 | PXD051134 | Pride
Drug discovery E6ap Pulmonary arterial hypertension Small molecule Ubiquitin e3-ligase Vascular remodeling Hect Allosteric inhibition Smurf1 Glycine hinge 
ProteomicsCovalent allosteric inhibition of AARS1 lactyltransferase
Alanyl-tRNA synthetase 1 (AARS1) was recently identified as a lactyltransferase responsible for protein lactylation, a modification associated with epigenetic regulation and metabolic adaptation. AARS1 catalyzes lysine lactylation via an ATP- and lactate- dependent, but lactyl-CoA-independent mechan...
ORGANISM(S): Homo sapiens (Human) 
2026-07-29 | PXD076410 | Pride
Lactyltransferase Covalent ligand Aars1 
ProteomicsHDX-MS of CHIP wt and K30A mutant
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
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 
ProteomicsDistinct modulation of cellular immunopeptidome by the allosteric regulatory site of ER aminopeptidase 1
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
Hla Mhc class1 Inhibitor Erap1 Aminopetidase Immunopeptidomics Allosteric 
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
Genomics
The energetic and allosteric landscape for KRAS inhibition
PRJNA907205 | ENA
GenomicsAllosteric inhibition of proteolytic and ATPase activities of the proteasome by the BTK inhibitor CGI-1746
Allosteric inhibition of proteolytic and ATPase activities of the proteasome by the BTK inhibitor CGI-1746
PRJNA999365 | ENA
UnknownAllosteric Competition and Inhibition in AMPA Receptors.
Not available
S-EPMC10705377 | biostudies-literature
Sort   by:  
 Page size