'Design, synthesis, and strategic use of small chemical probes toward identification of novel targets for drug development'

Curr Opin Chem Biol. 2020 Jun:56:91-97. doi: 10.1016/j.cbpa.2020.03.003. Epub 2020 May 3.

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.

Keywords: CETSA; Chemical probes; Chemical proteomics; Chemogenomics libraries; LiP; Molecular glues; Phenotypic screens; Target identification.

Publication types

  • Review

MeSH terms

  • Clustered Regularly Interspaced Short Palindromic Repeats / genetics
  • Drug Evaluation, Preclinical
  • Humans
  • Limonins / chemistry
  • Limonins / pharmacology
  • Machine Learning
  • Molecular Targeted Therapy
  • Proteomics
  • Small Molecule Libraries / chemistry*
  • Small Molecule Libraries / pharmacology*
  • Structure-Activity Relationship
  • Thalidomide / chemistry
  • Thalidomide / pharmacology
  • Ubiquitin-Protein Ligases / metabolism

Substances

  • Limonins
  • Small Molecule Libraries
  • nimbolide
  • Thalidomide
  • Ubiquitin-Protein Ligases