Discovery and Characterization of a Novel Allosteric Small-Molecule Inhibitor of NADP<sup>+</sup>-Dependent Malic Enzyme 1
Tomohiro Yoshida, Tetsuhiro Kawabe, Lewis C. Cantley, Costas A. Lyssiotis
Abstract
, alongside known crystal structures of malic enzymes, indicated the determined crystal ME1-inhibitor complex is in the open form conformation. These results provide insights and a starting point for further discovery of drugs that inhibit ME1 activity in cancer cells.
Topics & Concepts
Allosteric regulationEnzymeChemistryMoleculeCharacterization (materials science)Small moleculeBiochemistryMalic enzymeStereochemistryMalic acidMaterials scienceNanotechnologyDehydrogenaseOrganic chemistryCitric acidCalcium signaling and nucleotide metabolismPancreatic function and diabetesAdenosine and Purinergic Signaling