'Design, synthesis, and strategic use of small chemical probes toward identification of novel targets for drug development'. (June 2020)

• Record Type: Journal Article
• Authors: Castaldi, Maria Paola; Hendricks, James Adam; Zhang, Andrew X.
• Is Part Of: Current opinion in chemical biology. Volume 56(2020)
• Page Start: 91
• Page End: 97
• Publication Date: 2020-06
• Subjects: Chemical probes -- Target identification -- Chemogenomics libraries -- Phenotypic screens -- Molecular glues -- Chemical proteomics -- CETSA -- LiP; ABPP Activity-based Proteome Profiling -- ARC activity-regulated cytoskeleton -- CRISPR clusters of regularly interspaced short palindromic repeats -- PROTAC Proteolysis Targeting Chimeras -- isoTOP isotopic tandem orthogonal proteolysis-enabled activity-based proteome profiling -- ML Machine Learning; -- AI artificial intelligence; Bioorganic chemistry -- Periodicals; Biology -- Periodicals; Biochemistry -- Periodicals; Clinical biochemistry -- Periodicals; Biochemistry -- Periodicals; Chimie bio-organique -- Périodiques; Biologie -- Périodiques; 572.05
• DOI: 10.1016/j.cbpa.2020.03.003
• Languages: English
• ISSNs: 1367-5931

Abstract

Abstract: Chemical probes are essential tools used to study and modulate biological systems. Here, we describe some of the recent scientific advancement in the field of chemical biology, as well as how the advent of new technologies is redefining the criteria of 'good' chemical probes and influencing the discovery of valuable drug leads. In this review, we report selected examples of the usage of linkered and linker-free chemical probes for target identification, biological discovery, and general mechanistic understanding. We also discuss the promises of chemogenomics libraries in phenotypic screens, as well as the limitation of their usage to identify the modulation of new targets and biology.