Name: 3-Pyridinecarboxaldehyde. I found the field of Pharmacology & Pharmacy; Chemistry very interesting. Saw the article Inhibition of 3-phosphoglycerate dehydrogenase (PHGDH) by indole amides abrogates de novo serine synthesis in cancer cells published in 2019.0, Reprint Addresses Mullarky, E; Cantley, LC (corresponding author), Weill Cornell Med Coll, Meyer Canc Ctr, New York, NY 10065 USA.; Mullarky, E; Cantley, LC (corresponding author), Weill Cornell Med Coll, Dept Med, New York, NY 10065 USA.. The CAS is 500-22-1. Through research, I have a further understanding and discovery of 3-Pyridinecarboxaldehyde.
Cancer cells reprogram their metabolism to support growth and to mitigate cellular stressors. The serine synthesis pathway has been identified as a metabolic pathway frequently altered in cancers and there has been considerable interest in developing pharmacological agents to target this pathway. Here, we report a series of indole amides that inhibit human 3-phosphoglycerate dehydrogenase (PHGDH), the enzyme that catalyzes the first committed step of the serine synthesis pathway. Using X-ray crystallography, we show that the indole amides bind the NAD(+) pocket of PHGDH. Through structure-based optimization we were able to develop compounds with low nanomolar affinities for PHGDH in an enzymatic IC50 assay. In cellular assays, the most potent compounds inhibited de novo serine synthesis with low micromolar to sub-micromolar activities and these compounds successfully abrogated the proliferation of cancer cells in serine free media. The indole amide series reported here represent an important improvement over previously published PHGDH inhibitors as they are markedly more potent and their mechanism of action is better defined.
Name: 3-Pyridinecarboxaldehyde. Welcome to talk about 500-22-1, If you have any questions, you can contact Mullarky, E; Xu, JY; Robin, AD; Huggins, DJ; Jennings, A; Noguchi, N; Olland, A; Lakshminarasimhan, D; Miller, M; Tomita, D; Michino, M; Su, TJF; Zhang, GA; Stamford, AW; Meinke, PT; Kargman, S; Cantley, LC or send Email.
Reference:
Pyridine – Wikipedia,
,Pyridine | C5H5N – PubChem