Scientists have has pioneered antivirals targeting viral methyltransferases, offering a new strategy for treating RNA and DNA viruses. This breakthrough could complement existing therapies, offering r...

Scientists have has pioneered antivirals targeting viral methyltransferases, offering a new strategy for treating RNA and DNA viruses. This breakthrough could complement existing therapies, offering r...

The resurgence of phage therapy has renewed interest in the interplay between phage resistance and antibiotic susceptibility and has stimulated research in the emergent field of non-canonical cellular...

Carty et al. identify the H3K9 methyltransferases that restrict the size and position of the centromere protein A chromatin domain, maintaining functional centromeres.

Scientists have has pioneered antivirals targeting viral methyltransferases, offering a new strategy for treating RNA and DNA viruses. This breakthrough could complement existing therapies, offering r...

The Arabidopsis H3K27 mono-methyltransferases ATXR5 and ATXR6 repress crossovers within meiotic heterochromatin, are required for heterochromatin condensation and H3K27me1 establishment, and specific...

LMU researchers have developed a novel cofactor that broadens the use of methyltransferases – with great potential for research and applications.

Abstract. In many fungal phytopathogens, infection is regulated by accessory genomic regions enriched in facultative heterochromatin, but the precise role

Han et al. review how protein arginine methyltransferases (PRMTs) coordinate chromatin regulation, RNA metabolism, and immune signaling. They discuss emerging roles of PRMTs in tumor immunity and inflammaging and discuss catalytic and non-catalytic strategies for therapeutically targeting PRMT-dependent immune regulation.

Scientists have has pioneered antivirals targeting viral methyltransferases, offering a new strategy for treating RNA and DNA viruses. This breakthrough could complement existing therapies, offering r...

Target class profiling (TCP) is a chemical biology approach to investigate understudied biological target classes. TCP is achieved by developing a generalizable assay platform and screening curated compound libraries to interrogate the chemical biological space of members of an enzyme family. In this work, we took a TCP approach to investigate inhibitory activity across a set of small-molecule methyltransferases (SMMTases), a subclass of methyltransferase enzymes, with the goal of creating a launchpad to explore this largely understudied target class. Using the representative enzymes nicotinamide N-methyltransferase (NNMT), phenylethanolamine N-methyltransferase (PNMT), histamine N-methyltransferase (HNMT), glycine N-methyltransferase (GNMT), catechol O-methyltransferase (COMT), and guanidinoacetate N-methyltransferase (GAMT), we optimized high-throughput screening (HTS)-amenable assays to screen 27,574 unique small molecules against all targets. From this data set, we identified a novel inhibitor which selectively inhibits the SMMTase HNMT and demonstrated how this platform approach can be leveraged for a targeted drug discovery campaign using the example of HNMT.