Recent Progress in the Development of Transglutaminase 2 (TGase2) Inhibitors.
J Med Chem
; 60(2): 554-567, 2017 01 26.
Article
em En
| MEDLINE
| ID: mdl-28122456
ABSTRACT
Transglutaminase 2 (TGase2, TG2) activity has been implicated in the pathogenesis of a number of unrelated disorders, including celiac, neurological, and renal diseases, and various forms of cancer. It has been suggested that TGase2 activity, such as cross-linking, deamidation, and GTP-related activity, is associated with each disease. Continuing efforts to develop small molecule TG2 inhibitors are ongoing. To develop a new class of TG2 inhibitors, the factors impeding the development of TG2 inhibitors have been identified. Additionally, the conformational effect of TG2 enzyme in regard to its pathological roles, in vitro screening methods, recently discovered TG2 inhibitors, and preclinical evaluations are discussed with a brief summary of current TG2 inhibitor pipelines under the clinical setting.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Transglutaminases
/
Proteínas de Ligação ao GTP
/
Inibidores Enzimáticos
Idioma:
En
Ano de publicação:
2017
Tipo de documento:
Article