Research progress of the small molecule covalent inhibitors.
- Author:
Bo YANG
;
Wen-Jing WANG
;
Lin-Li LI
- Publication Type:Journal Article
- MeSH:
Amino Acids;
chemistry;
Antineoplastic Agents;
chemical synthesis;
chemistry;
therapeutic use;
Antiviral Agents;
chemical synthesis;
chemistry;
therapeutic use;
Drug Discovery;
Drug Resistance;
Enzyme Inhibitors;
chemical synthesis;
chemistry;
therapeutic use;
Hepatitis C;
drug therapy;
Humans;
Molecular Structure;
Neoplasms;
drug therapy;
Protein Binding;
Protein Kinase Inhibitors;
chemical synthesis;
chemistry;
therapeutic use;
Receptor, Epidermal Growth Factor;
antagonists & inhibitors;
Serine Proteinase Inhibitors;
chemical synthesis;
chemistry;
therapeutic use
- From:
Acta Pharmaceutica Sinica
2014;49(2):158-165
- CountryChina
- Language:Chinese
-
Abstract:
Small molecule covalent inhibitors, or called as irreversible inhibitors, are a type of inhibitors that exert their biological functions by irreversibly binding to target through covalent bonds. Compared with non-covalent inhibitors, covalent inhibitors have obvious advantages in bioactivity. Nevertheless, these agents may also exhibit larger toxicity once off-target effects arise. This "double-edged swords" property often leads drug researchers to avoid attaching them. In recent years, some problems such as drug resistance are difficult to be solved with reversible inhibitors leading researchers to pay more attention on the covalent inhibitors. In this review, we shall make a short summary to the recent research progress of covalent inhibitors and the interaction modes between covalent inhibitors and their target protein residues.
