Overview of the development of protein arginine methyltransferase modulators: Achievements and future directions

Tong, Chao; Chang, Xiujin; Qu, Fangui; Bian, Jinlei; Wang, Jubo; Li, Zhiyu; Xu, Xi

doi:10.1016/j.ejmech.2024.116212

European Journal of Medicinal Chemistry

2024

DOI: 10.1016/j.ejmech.2024.116212

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Overview of the development of protein arginine methyltransferase modulators: Achievements and future directions

Chao Tong,

Xiujin Chang,

Fangui Qu

et al.

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2024

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Cited by 6 publications

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Overview of PRMT1 modulators: Inhibitors and degraders

Wu,

Li,

Wang

2024

European Journal of Medicinal Chemistry

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Overview of PRMT1 modulators: Inhibitors and degraders

Wu,

Li,

Wang

2024

European Journal of Medicinal Chemistry

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Methylation modification of non-histone proteins in breast cancer: An emerging targeted therapeutic strategy

Huang,

Jiang,

et al. 2024

Pharmacological Research

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Structure, Function, and Activity of Small Molecule and Peptide Inhibitors of Protein Arginine Methyltransferase 1

Hendrickson-Rebizant,

Sudhakar,

Rowley

et al. 2024

J. Med. Chem.

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Protein arginine N -methyltransferases (PRMT) are a family of S -adenosyl- l -methionine (SAM)-dependent enzymes that transfer methyl-groups to the ω-N of arginyl residues in proteins. PRMTs are involved in regulating gene expression, RNA splicing, and other activities. PRMT1 is responsible for most cellular arginine methylation, and its dysregulation is involved in many cancers. Accordingly, many groups have targeted PRMT1 using small molecules and peptide inhibitors. In this Perspective, we discuss the structure and function of selected peptide and small molecule inhibitors of PRMT1. We examine inhibitors that target the substrate arginyl peptide, SAM, or both binding sites, and the type of inhibition that results. Small molecules, and peptides that are bisubstrate, and/or PRMT transition state mimic inhibitors as well as inhibitors that alkylate PRMTs will be discussed. We define a structure–activity relationship for the aromatic/heteroaromatic N -methylethylenediamine inhibitors of PRMT1 and review current progress of PRMT1 inhibitors in clinical trials.

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Overview of the development of protein arginine methyltransferase modulators: Achievements and future directions

Cited by 6 publications

References 143 publications

Overview of PRMT1 modulators: Inhibitors and degraders

Overview of PRMT1 modulators: Inhibitors and degraders

Methylation modification of non-histone proteins in breast cancer: An emerging targeted therapeutic strategy

Structure, Function, and Activity of Small Molecule and Peptide Inhibitors of Protein Arginine Methyltransferase 1

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