Discovery of [1,2,3]triazolo[4,5-<i>d</i>]pyrimidine derivatives as highly potent, selective, and cellularly active USP28 inhibitors.

Liu, Zhenzhen; Zhao, Taoqian; Li, Zhonghua; Sun, Kai; Fu, Yundong; Cheng, Ting; Guo, Jimin; Yu, Bin; Shi, Xiaojing; Liu, Hongmin

Discovery of [1,2,3]triazolo[4,5-d]pyrimidine derivatives as highly potent, selective, and cellularly active USP28 inhibitors.

Liu, Zhenzhen; Zhao, Taoqian; Li, Zhonghua; Sun, Kai; Fu, Yundong; Cheng, Ting; Guo, Jimin; Yu, Bin; Shi, Xiaojing; Liu, Hongmin.

Afiliación

Liu Z; School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China.
Zhao T; School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China.
Li Z; School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China.
Sun K; School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China.
Fu Y; School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China.
Cheng T; School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China.
Guo J; School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China.
Yu B; School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China.
Shi X; School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China.
Liu H; School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China.

Acta Pharm Sin B ; 10(8): 1476-1491, 2020 Aug.

Article en En | MEDLINE | ID: mdl-32963944

Palabras clave

BLI, biolayer interferometry technology; CHX, cycloheximide; DUBs, deubiquitinating enzymes; Deubiquitination; EMT, epithelial-mesenchymal transition; EdU, 5-ethynyl-2'-deoxyuridine; GAPDH, glyceraldehyde-3-phosphate dehydrogenase; Gastric cancer; IC50, half maximal inhibitory concentration; Kd, dissociation constant; LSD1, lysine specific demethylase 1; MG132, proteasome inhibitor; MTT, 3-(4,5-dimethylthiazol-2-yl)-2-5-diphenyltetrazoliumbromide; NSCLC, non-small cell lung cancer; Tris, 2-amino-2-(hydroxymethyl)-1,3-propanediol; USP28 inhibitors; USP28, ubiquitin specific peptidase 28; USP7, ubiquitin specific peptidase 7; Ub, ubiquitin; Ub-AMC, ubiquitin-7-amido-4-methylcoumarin; [1,2,3]Triazolo[4,5-d]pyrimidine derivatives

Texto completo

Añadir a Mi BVS

Imprimir

XML

PubMed Links

Buscar en Google

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: Acta Pharm Sin B Año: 2020 Tipo del documento: Article País de afiliación: China Pais de publicación: Países Bajos

Texto completo

Añadir a Mi BVS

Imprimir

XML

PubMed Links

Buscar en Google