Introduction to Chemical Proteomics for Drug Discovery and Development

Abstract

A fundamental goal of chemical proteomics is to identify target proteins for bioactive small molecules and then apply them to drug discovery and development as valid and drugable targets. Here, we introduce integrated technologies for the rapid identification of target proteins, methodologies for validating them as drugable targets, and applications of chemical proteomics in drug discovery and development.

In Silico and Ultrahigh‐Throughput Screenings (uHTS) in Drug Discovery: An Overview

“…There are two strategies for chemical proteomics techniques: (i) activity -based probe profi ling ( ABPP ), which is based on enzymatic activity of a particular class of enzyme, and (ii) the fragment -based approach, which facilitates the assembly of a large library of diverse molecules from a smaller number of building blocks [20] .…”

Intrinsic fluorescence properties of antimalarial pyrido[1,2-a]benzimidazoles facilitate subcellular accumulation and mechanistic studies in the human malaria parasite Plasmodium falciparum

“…This approach utilises integrated knowledge in chemistry, biology, structural biology, biochemistry and bioinformatics to obtain information about the binding site of bioactive molecules and to provide suitable starting points for the development of drug screening systems based on the structure of target proteins. 9,10 On the other hand, the genomics approach to target identification utilises the vast information obtained from the completion of the human genome sequencing project 11 and the genome sequencing of different organisms, to understand complex biological systems of human diseases and to help identify and validate new targets. 12,13 one of the useful techniques in genomics, tailored to understanding the mechanism of resistance (MoR) and the MoA of small molecules is resistance selection studies.…”

Identification of Vimentin Binding to the Derivative of Saurolactam with Antiresorptive Activity by Using Its Chemical Affinity Probe

“…Thus, correlation of a property or mechanism of the chemical with a specific biological process and, further, the discovery of new target proteins that bind to a class of chemicals or drugs with good efficacy could be starting points for the development of new therapeutics for diseases by using the screening systems based on the structure of the newly identified target protein. 1 The process to identify and validate the protein targets of bioactive small molecules discovered through cell-based assays is an important step in preclinical drug development. Several strategies have been developed to detect target protein(s) that can directly interact with the bioactive small molecule.…”