Researchers from China Pharmaceutical University reported the discovery and preclinical characterization of allosteric inhibitors of Src homology-2-containing protein tyrosine phosphatase 2 (SHP2) as ...

Allosteric activators or inhibitors induce small conformational changes that can either turn on or turn off an enzyme. X-ray crystallography and protein 'docking' experiments are creating new ...

Owing to complete inhibition of enzyme activity ... with Phe196 in UCR2 are key for PDE4D selectivity. Although such allosteric modulators only partially inhibit PDE4 activity, they are still ...

Our work encompasses a broad range of molecular mechanisms of action, spanning covalent inhibitors, allosteric inhibitors, enzyme activators, protein (or protein complex) stabilizers, and protein ...

ETX-636 is a novel orally bioavailable allosteric pan-mutant-selective PI3Kα inhibitor and degrader. This dual mechanism of action results in deep and durable pathway inhibition and induces ...

Enzyme activity is tightly regulated in living organisms to maintain homeostasis and respond to changing conditions. Enzymes can be regulated by various means, such as allosteric regulation (binding ...

Initiated combination portion of Phase 1 clinical trial of QTX3046, an oral KRASG12D-selective dual ON/OFF state allosteric inhibitor, with the EGFR inhibitor cetuximab – – Phase 1 clinical ...