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Research progress of the small molecule covalent inhibitors / 药学学报
Yao Xue Xue Bao ; (12): 158-165, 2014.
Article em Zh | WPRIM | ID: wpr-297998
Biblioteca responsável: WPRO
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.
Assuntos
Texto completo: 1 Base de dados: WPRIM Assunto principal: Antivirais / Ligação Proteica / Resistência a Medicamentos / Estrutura Molecular / Inibidores de Serina Proteinase / Química / Hepatite C / Usos Terapêuticos / Inibidores de Proteínas Quinases / Tratamento Farmacológico Limite: Humans Idioma: Zh Revista: Yao Xue Xue Bao Ano de publicação: 2014 Tipo de documento: Article
Texto completo: 1 Base de dados: WPRIM Assunto principal: Antivirais / Ligação Proteica / Resistência a Medicamentos / Estrutura Molecular / Inibidores de Serina Proteinase / Química / Hepatite C / Usos Terapêuticos / Inibidores de Proteínas Quinases / Tratamento Farmacológico Limite: Humans Idioma: Zh Revista: Yao Xue Xue Bao Ano de publicação: 2014 Tipo de documento: Article