ArticleJournal of medicinal chemistry2015
Exploration of cyanine compounds as selective inhibitors of protein arginine methyltransferases: synthesis and biological evaluation.
Article in Journal of medicinal chemistry, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed, 43 citations in OpenAlex.
- Dysregulation of arginine methylation in tumorigenesis.Frontiers in molecular biosciences · 2024Review
- Chemical probes and methods for the study of protein arginine methylation.RSC chemical biology · 2023Review
- Protein Arginine Methyltransferases as Therapeutic Targets in Hematological Malignancies.Cancers · 2022Review
- Protein arginine methyltransferases: promising targets for cancer therapy.Experimental & molecular medicine · 2021Review
- Mechanisms and Inhibitors of Histone Arginine Methylation.Chemical record (New York, N.Y.) · 2018Review
- Defining the epigenetic status of blood cells using a cyanine-based fluorescent probe for PRMT1.Blood advances · 2018Article
- Recent advances in targeting protein arginine methyltransferase enzymes in cancer therapy.Expert opinion on therapeutic targets · 2018Review
- Inhibitors of Protein Methyltransferases and Demethylases.Chemical reviews · 2018Review
- Protein arginine methylation: an emerging regulator of the cell cycle.Cell division · 2018Review
- Transient Kinetics Define a Complete Kinetic Model for Protein Arginine Methyltransferase 1.The Journal of biological chemistry · 2016Article
- Protein Arginine Methylation and Citrullination in Epigenetic Regulation.ACS chemical biology · 2016Article
- Small Molecule Inhibitors of Protein Arginine Methyltransferases.Expert opinion on investigational drugs · 2016Review
- Benz[c,d]indolium-containing Monomethine Cyanine Dyes: Synthesis and Photophysical Properties.Molecules (Basel, Switzerland) · 2015Article
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Authors and funding
8 authors at 3 institutions in 1 country.
Funding
Abstract
Protein arginine methyltransferase 1 (PRMT1) is involved in many biological activities, such as gene transcription, signal transduction, and RNA processing. Overexpression of PRMT1 is related to cardiovascular diseases, kidney diseases, and cancers; therefore, selective PRMT1 inhibitors serve as chemical probes to investigate the biological function of PRMT1 and drug candidates for disease treatment. Our previous work found trimethine cyanine compounds that effectively inhibit PRMT1 activity. In our present study, we systematically investigated the structure-activity relationship of cyanine structures. A pentamethine compound, E-84 (compound 50), showed inhibition on PRMT1 at the micromolar level and 6- to 25-fold selectivity over CARM1, PRMT5, and PRMT8. The cellular activity suggests that compound 50 permeated the cellular membrane, inhibited cellular PRMT1 activity, and blocked leukemia cell proliferation. Additionally, our molecular docking study suggested compound 50 might act by occupying the cofactor binding site, which provided a roadmap to guide further optimization of this lead compound.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.