Novotny, Chris J. published the artcileFarnesyltransferase-Mediated Delivery of a Covalent Inhibitor Overcomes Alternative Prenylation to Mislocalize K-Ras, Application In Synthesis of 57044-25-4, the publication is ACS Chemical Biology (2017), 12(7), 1956-1962, database is CAplus and MEDLINE.
Mutationally activated Ras is one of the most common oncogenic drivers found across all malignancies, and its selective inhibition has long been a goal in both pharma and academia. One of the oldest and most validated methods to inhibit overactive Ras signaling is by interfering with its post-translational processing and subsequent cellular localization. Previous attempts to target Ras processing led to the development of farnesyltransferase inhibitors, which can inhibit H-Ras localization but not K-Ras due to its ability to bypass farnesyltransferase inhibition though alternative prenylation by geranylgeranyltransferase. Here the authors present the creation of a neo-substrate for farnesyltransferase that prevents the alternative prenylation by geranylgeranyltransferase and mislocalizes oncogenic K-Ras in cells.
ACS Chemical Biology published new progress about 57044-25-4. 57044-25-4 belongs to alcohols-buliding-blocks, auxiliary class Epoxides,Chiral,Aliphatic hydrocarbon chain,Alcohol, name is (R)-Oxiran-2-ylmethanol, and the molecular formula is C3H6O2, Application In Synthesis of 57044-25-4.
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