Proceedings of the National Academy of Sciences of the United States of America published new progress about 944129-07-1. 944129-07-1 belongs to chlorides-buliding-blocks, auxiliary class Fluoride,Chloride,Boronic acid and ester,Benzene,Ether,Boronic Acids,Boronic acid and ester,, name is (4-Chloro-2-fluoro-3-methoxyphenyl)boronic acid, and the molecular formula is C7H7BClFO3, Computed Properties of 944129-07-1.
Cruz-Migoni, Abimael published the artcileStructure-based development of new RAS-effector inhibitors from a combination of active and inactive RAS-binding compounds, Computed Properties of 944129-07-1, the publication is Proceedings of the National Academy of Sciences of the United States of America (2019), 116(7), 2545-2550, database is CAplus and MEDLINE.
The RAS gene family is frequently mutated in human cancers, and the quest for compounds that bind to mutant RAS remains a major goal, as it also does for inhibitors of protein-protein interactions. We have refined crystallization conditions for KRAS169Q61H-yielding crystals suitable for soaking with compounds and exploited this to assess new RAS-binding compounds selected by screening a protein-protein interaction-focused compound library using surface plasmon resonance. Two compounds, referred to as PPIN-1 and PPIN-2, with related structures from 30 initial RAS binders showed binding to a pocket where compounds had been previously developed, including RAS effector protein-protein interaction inhibitors selected using an intracellular antibody fragment (called Abd compounds). Unlike the Abd series of RAS binders, PPIN-1 and PPIN-2 compounds were not competed by the inhibitory anti-RAS intracellular antibody fragment and did not show any RAS-effector inhibition properties. By fusing the common, anchoring part from the two new compounds with the inhibitory substituents of the Abd series, we have created a set of compounds that inhibit RAS-effector interactions with increased potency. These fused compounds add to the growing catalog of RAS protein-protein inhibitors and show that building a chem. series by crossing over two chem. series is a strategy to create RAS-binding small mols.
Proceedings of the National Academy of Sciences of the United States of America published new progress about 944129-07-1. 944129-07-1 belongs to chlorides-buliding-blocks, auxiliary class Fluoride,Chloride,Boronic acid and ester,Benzene,Ether,Boronic Acids,Boronic acid and ester,, name is (4-Chloro-2-fluoro-3-methoxyphenyl)boronic acid, and the molecular formula is C7H7BClFO3, Computed Properties of 944129-07-1.
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