Fragment screening of N-acetylmannosamine kinase reveals noncarbohydrate inhibitors was written by Aretz, Jonas;Wratil, Paul Robin;Wamhoff, Eike-Christian;Nguyen, Hoang Giang;Reutter, Werner;Rademacher, Christoph. And the article was included in Canadian Journal of Chemistry in 2016.Application of 122637-39-2 This article mentions the following:
Many biol. processes from infection to tumor immune evasion are controlled by cell surface sialylation. To gather further insight into these processes, methods to alter cell surface sialylation are required. One way to achieve this is inhibiting the key enzyme of sialic acid de novo biosynthesis, the intracellular bifunctional UDP-N-acetylglucosamine epimerase/N-acetylmannosamine kinase (GNE/MNK). Here, the authors present low-mol.-weight inhibitors of MNK activity based on picolinic acid derivatives They were identified in a fragment screening using 19F NMR and validated in a biochem. inhibition assay followed by a structure-activity relation anal. and docking. The optimized compound, 6-carbamoylpicolinic acid, inhibited MNK with a double-digit micromolar affinity. Its low mol. weight (166 Da) rendered this picolinic acid derivative an exquisite starting point for the development of high-affinity MNK inhibitors, which may serve as mol. probes or lead candidates in future. In the experiment, the researchers used many compounds, for example, 6-Acetylpicolinic acid (cas: 122637-39-2Application of 122637-39-2).
6-Acetylpicolinic acid (cas: 122637-39-2) belongs to pyridine derivatives. The ring atoms in the pyridine molecule are sp2-hybridized. The nitrogen is involved in the π-bonding aromatic system using its unhybridized p orbital. The lone pair is in an sp2 orbital, projecting outward from the ring in the same plane as the σ bonds. Pyridine groups exist in countless molecules, and their applications include catalysis, drug design, molecular recognition, and natural product synthesis.Application of 122637-39-2