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
MetabolomicsDevelopment of a first-in-class inhibitor of the mitochondrial glutamine transporter SLC1A5_var to target glutamine dependency in cancer

The mitochondrial glutamine transporter SLC1A5_var plays a central role in the metabolic reprogramming of cancer cells by facilitating glutamine import into mitochondria for energy production and redox homeostasis. Despite its critical function, the development of effective and selective inhibito...

2025-08-13 | MTBLS12852 | MetaboLights
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
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 
GenomicsAn allosteric pan-TEAD inhibitor blocks oncogenic YAP/TAZ signaling and overcomes KRAS G12C inhibitor resistance
An allosteric pan-TEAD inhibitor blocks oncogenic YAP/TAZ signaling and overcomes KRAS G12C inhibitor resistance
PRJNA952667 | ENA
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 
GenomicsThe tyrosine kinase inhibitor GNF-7 targets senescent cells through allosteric activation of GCN2
The tyrosine kinase inhibitor GNF-7 targets senescent cells through allosteric activation of GCN2
PRJNA1288031 | ENA
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 
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
GenomicsTranscriptomic changes in a KRASG12C mutant cell line (H358 cells) treated with the allosteric SHP2 inhibitor TNO155 for different times
Transcriptomic changes in a KRASG12C mutant cell line (H358 cells) treated with the allosteric SHP2 inhibitor TNO155 for different times
PRJNA1065823 | ENA
Sort   by:  
 Page size