So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Vasta, James D.; Andersen, Kristen A.; Deck, Kathryn M.; Nizzi, Christopher P.; Eisenstein, Richard S.; Raines, Ronald T. researched the compound: Ethyl oxazole-5-carboxylate( cas:118994-89-1 ).Electric Literature of C6H7NO3.They published the article 《Selective Inhibition of Collagen Prolyl 4-Hydroxylase in Human Cells》 about this compound( cas:118994-89-1 ) in ACS Chemical Biology. Keywords: collagen prolyl hydroxylase inhibitor fibrosis metastasis antimetastatic antifibrotic. We’ll tell you more about this compound (cas:118994-89-1).
Collagen is the most abundant protein in animals. Its overproduction is associated with fibrosis and cancer metastasis. The stability of collagen relies on posttranslational modifications, the most prevalent being the hydroxylation of collagen strands by collagen prolyl 4-hydroxylases (CP4Hs). Catalysis by CP4Hs enlists an iron cofactor to convert proline residues to 4-hydroxyproline residues, which are essential for the conformational stability of mature collagen. Et 3,4-dihydroxybenzoate (EDHB) is commonly used as a “”P4H”” inhibitor in cells, but suffers from low potency, poor selectivity, and off-target effects that cause iron deficiency. Dicarboxylates of 2,2′-bipyridine are among the most potent known CP4H inhibitors but suffer from a high affinity for free iron. A screen of biheteroaryl compounds revealed that replacing one pyridyl group with a thiazole moiety retains potency and enhances selectivity. A diester of 2-(5-carboxythiazol-2-yl)pyridine-5-carboxylic acid is bioavailable to human cells and inhibits collagen biosynthesis at concentrations that neither cause general toxicity nor disrupt iron homeostasis. These data anoint a potent and selective probe for CP4H and a potential lead for the development of a new class of antifibrotic and antimetastatic agents.
If you want to learn more about this compound(Ethyl oxazole-5-carboxylate)Electric Literature of C6H7NO3, you may wish to communicate with the author of the article,or consult the relevant literature related to this compound(118994-89-1).