Methyl 6-Cyanopyridine-3-carboxylate (cas: 89809-65-4) belongs to pyridine derivatives. The pyridine ring occurs in many important compounds, including agrochemicals, pharmaceuticals, and vitamins. Pyridine derivatives are also useful as small-molecule 婵?helix mimetics that inhibit protein-protein interactions, as well as functionally selective GABA ligands.Product Details of 89809-65-4
Improving the Selectivity of PACE4 Inhibitors through Modifications of the P1 Residue was written by Dianati, Vahid;Navals, Pauline;Couture, Frederic;Desjardins, Roxane;Dame, Anthony;Kwiatkowska, Anna;Day, Robert;Dory, Yves L.. And the article was included in Journal of Medicinal Chemistry in 2018.Product Details of 89809-65-4 This article mentions the following:
Paired basic amino acid cleaving enzyme 4 (PACE4), a serine endoprotease of the proprotein convertases family, has been recognized as a promising target for prostate cancer. We previously reported a selective and potent peptide-based inhibitor for PACE4, named the multi-Leu peptide (Ac-LLLLRVKR-NH2 sequence), which was then modified into a more potent and stable compound named C23 with the following structure: Ac-DLeu-LLLRVK-Amba (Amba: 4-amidinobenzylamide). Despite improvements in both in vitro and in vivo profiles of C23, its selectivity for PACE4 over furin was significantly reduced. We examined other Arg-mimetics instead of Amba to regain the lost selectivity. Our results indicated that the replacement of Amba with 5-(aminomethyl)picolinimidamide increased affinity for PACE4 and restored selectivity. Our results also provide a better insight on how structural differences between S1 pockets of PACE4 and furin could be employed in the rational design of selective inhibitors. In the experiment, the researchers used many compounds, for example, Methyl 6-Cyanopyridine-3-carboxylate (cas: 89809-65-4Product Details of 89809-65-4).
Methyl 6-Cyanopyridine-3-carboxylate (cas: 89809-65-4) belongs to pyridine derivatives. The pyridine ring occurs in many important compounds, including agrochemicals, pharmaceuticals, and vitamins. Pyridine derivatives are also useful as small-molecule 婵?helix mimetics that inhibit protein-protein interactions, as well as functionally selective GABA ligands.Product Details of 89809-65-4
Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem