Discovery of a potent and dual-selective bisubstrate inhibitor for protein arginine methyltransferase 4/5.

Al-Hamashi, Ayad A; Chen, Dongxing; Deng, Youchao; Dong, Guangping; Huang, Rong

Al-Hamashi, Ayad A; Chen, Dongxing; Deng, Youchao; Dong, Guangping; Huang, Rong.

Afiliação

Al-Hamashi AA; Department of Medicinal Chemistry and Molecular Pharmacology, Center for Cancer Research, Institute for Drug Discovery, Purdue University, West Lafayette, IN 47907, USA.
Chen D; Department of Pharmaceutical Chemistry, College of Pharmacy, University of Baghdad, Bab-almoadham, Baghdad 10047, Iraq.
Deng Y; Department of Medicinal Chemistry and Molecular Pharmacology, Center for Cancer Research, Institute for Drug Discovery, Purdue University, West Lafayette, IN 47907, USA.
Dong G; Department of Medicinal Chemistry and Molecular Pharmacology, Center for Cancer Research, Institute for Drug Discovery, Purdue University, West Lafayette, IN 47907, USA.
Huang R; Department of Medicinal Chemistry and Molecular Pharmacology, Center for Cancer Research, Institute for Drug Discovery, Purdue University, West Lafayette, IN 47907, USA.

Acta Pharm Sin B ; 11(9): 2709-2718, 2021 Sep.

Article em En | MEDLINE | ID: mdl-34589391

Palavras-chave

Bisubstrate analogue; Bisubstrate inhibitor; GAR, glycine and arginine; IC50, half-maximal inhibition concentration; NTMTs, N-terminal methyltransferases; PKMTs, protein lysine methyltransferases; PRMTs, protein arginine methyltransferases; Protein arginine methyltransferase; Protein arginine methyltransferase 4; Protein arginine methyltransferase 5; SAH, S-(5'-adenosyl)-l-homocysteine; SAM, S-adenosylmethionine; SNF, sinofungin; TLC, thin-layer chromatography

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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Idioma: En Ano de publicação: 2021 Tipo de documento: Article

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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Idioma: En Ano de publicação: 2021 Tipo de documento: Article