Results 111 to 120 of about 4,452,404 (339)
KRAS-specific inhibition using a DARPin binding to a site in the allosteric lobe
Nature Communications, 2019 Inhibiting the RAS oncogenic protein has largely been through targeting the switch regions that interact with signalling effector proteins. Here, we report designed ankyrin repeat proteins (DARPins) macromolecules that specifically inhibit the KRAS ...
N. Béry +15 more
semanticscholar +1 more source
Advanced Science, EarlyView.Genome‐scale metabolic modeling is preceded to the engineered E. coli cell factory for the de novo biosynthesis of biopesticide chrysanthemic acid. The debranching strategy redirects metabolic flux, enhancing precursor and target compound production.
Jiangpeng Yu +6 more
wiley +1 more source
Science Advances, 2019 We decipher how an allosteric inhibitor activates the ClpP protease machinery by binding to the catalytic site. Coordinated conformational transitions in oligomeric enzymatic complexes modulate function in response to substrates and play a crucial role ...
semanticscholar +1 more source
Advanced Science, EarlyView.Phospholipid transfer protein(PLTP) plays a critical role in forming a complex with kinase A (AURKA) and P65. This interaction facilitates phosphorylation of P65 at Ser536, leading to the activation of the NF‐κB signaling pathway. Ultimately, this leads to the upregulation of downstream cytokines, including IL‐6, IL‐8, and CSF‐1, which promotes M2 ...
Xinyue Liang +14 more
wiley +1 more source
Chemical, target, and bioactive properties of allosteric modulation.
PLoS Computational Biology, 2014 Allosteric modulators are ligands for proteins that exert their effects via a different binding site than the natural (orthosteric) ligand site and hence form a conceptually distinct class of ligands for a target of interest.
Gerard J P van Westen +2 more
doaj +1 more source
Allosteric Site on SHIP2 Identified Through Fluorescent Ligand Screening and Crystallography: A Potential New Target for Intervention [PDF]
, 2021 Hayley Whitfield +8 more
openalex +1 more source
Magnetically‐Induced Suppression of Oxidative Stress Prevents Venous Thrombosis
Advanced Science, EarlyView.Venous thromboembolism (VTE) remains a leading cause of cardiovascular mortality. This study demonstrates that static magnetic fields (SMF) offer a novel non‐pharmacological intervention against VTE by mitigating endothelial oxidative stress. Mechanistically, SMF elevates intracellular Ca2+, boosts ATP production, and suppresses NOX4‐mediated ROS ...
Nana Zhang +12 more
wiley +1 more source
A New Paradigm for KIM-PTP Drug Discovery: Identification of Allosteric Sites with Potential for Selective Inhibition Using Virtual Screening and LEI Analysis [PDF]
, 2021 James Truslow Adams +2 more
openalex +1 more source
Novel Allosteric Sites on Ras for Lead Generation
PLoS ONE, 2011 Aberrant Ras activity is a hallmark of diverse cancers and developmental diseases. Unfortunately, conventional efforts to develop effective small molecule Ras inhibitors have met with limited success. We have developed a novel multi-level computational approach to discover potential inhibitors of previously uncharacterized allosteric sites.
Grant, Barry J +6 more
openaire +6 more sources