نتایج جستجو برای: druggability
تعداد نتایج: 302 فیلتر نتایج به سال:
Bromodomains are epigenetic reader domains that have recently become popular targets. In contrast to BET bromodomains, which have proven druggable, bromodomains from other regions of the phylogenetic tree have shallower pockets. We describe successful targeting of the challenging BAZ2B bromodomain using biophysical fragment screening and structure-based optimization of high ligand-efficiency fr...
Non-coding RNAs are crucial regulators for a vast array of cellular processes and have been implicated in human disease. These biological processes represent a hitherto untapped resource in our fight against disease. In this work we identify small molecule inhibitors of a non-coding RNA uridylylation pathway. The TUTase family of enzymes is important for modulating non-coding RNA pathways in bo...
Cyclins and cyclin-dependent kinases (CDKs) play versatile roles in promoting the hallmarks of cancer. Therefore, cyclins CDKs have been widely studied targeted cancer treatment, with four CDK4/6 inhibitors being approved by FDA many other examined clinical trials. The specific purpose this review is to delineate role therapeutic potential Cyclin K cancers. Studies shown that regulates essentia...
Lysine-specific demethylase 1 (LSD1) is a FAD-dependent enzyme, which has been proposed as promising target for therapeutic cancer. Herein, series of benzofuran derivatives were designed, synthesized and biochemical evaluated novel LSD1 inhibitors based on scaffold hopping conformational restriction strategy. Most the compounds potently suppressed enzymatic activities inhibited tumor cells prol...
Abstract Motivation The cost of drug development has dramatically increased in the last decades, with number new drugs approved per billion US dollars spent on R&D halving every year or less. selection and prioritization targets is one most influential decisions discovery. Here we present a Gaussian Process model for cast as problem learning only positive unlabeled examples. Results Since a...
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