Covalent Small Molecules as Enabling Platforms for Drug Discovery
- Resource Type
- Authors
- Sebastien Andre Campos; Samuel E. Dalton
- Source
- ChemBioChem. 21:1080-1100
- Subject
- 010405 organic chemistry
Chemistry
Drug discovery
Chemistry, Pharmaceutical
Organic Chemistry
010402 general chemistry
01 natural sciences
Biochemistry
Combinatorial chemistry
Small molecule
Enzymes
0104 chemical sciences
Small Molecule Libraries
Nucleophile
Covalent bond
Drug Discovery
Animals
Humans
Molecular Medicine
Molecule
Reactivity (chemistry)
Molecular Targeted Therapy
Enzyme Inhibitors
Molecular Biology
- Language
- ISSN
- 1439-7633
1439-4227
Covalent drugs have experienced significant renewed interest in drug discovery. This resurgence has been accompanied by a better understanding of the reactivity relationships required to engage selective covalent bonds between nucleophilic proteins and electrophilic small molecules. As a result, researchers have come to the realisation that covalent molecules could also represent useful and novel tools aimed at supporting medicinal chemistry programmes. This review surveys the increasing number of drug discovery platforms employing covalent chemistries, and highlights the utility of these techniques for identifying and characterising small molecules and biological targets.