Toward the development of potent and selective bisubstrate inhibitors of protein arginine methyltransferases

Bioorganic & Medicinal Chemistry Letters
2010.0

Abstract

Prototype inhibitors of protein arginine methyltransferases (PRMTs) have been constructed by attaching guanidine functionality via a variable linker to non-reactive amine analogues of the cellular co-factor (S)-adenosyl methionine (AdoMet). Potent inhibition of PRMT1 (IC(50) of approximately 3-6 microM) combined with weak inhibition of the lysine methyltransferase SET7 (approximately 50% of activity at 100 microM) was observed for two such compounds.

Knowledge Graph

Similar Paper

Toward the development of potent and selective bisubstrate inhibitors of protein arginine methyltransferases
Bioorganic & Medicinal Chemistry Letters 2010.0
Design and synthesis of novel PRMT1 inhibitors and investigation of their binding preferences using molecular modelling
Bioorganic & Medicinal Chemistry Letters 2017.0
Discovery of decamidine as a new and potent PRMT1 inhibitor
MedChemComm 2017.0
Discovery and Mechanistic Study of a Class of Protein Arginine Methylation Inhibitors
Journal of Medicinal Chemistry 2010.0
Development of rationally designed DNA N6 adenine methyltransferase inhibitors
Bioorganic & Medicinal Chemistry Letters 2012.0
Turning Nonselective Inhibitors of Type I Protein Arginine Methyltransferases into Potent and Selective Inhibitors of Protein Arginine Methyltransferase 4 through a Deconstruction–Reconstruction and Fragment-Growing Approach
Journal of Medicinal Chemistry 2022.0
Exploration of Cyanine Compounds as Selective Inhibitors of Protein Arginine Methyltransferases: Synthesis and Biological Evaluation
Journal of Medicinal Chemistry 2015.0
Discovery of new potent protein arginine methyltransferase 5 (PRMT5) inhibitors by assembly of key pharmacophores from known inhibitors
Bioorganic & Medicinal Chemistry Letters 2018.0
Discovery and structure–activity analysis of 4-((5-nitropyrimidin-4-yl)amino)benzimidamide derivatives as novel protein arginine methyltransferase 1 (PRMT1) inhibitors
Bioorganic & Medicinal Chemistry Letters 2015.0
Discovery of a Dual PRMT5–PRMT7 Inhibitor
ACS Medicinal Chemistry Letters 2015.0