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Target Class Profiling of Small-Molecule Methyltransferases.

Quinlin M Hanson¹, Nate Hoxie¹, Min Shen¹

¹National Center for Advancing Translational Science, National Institutes of Health, Rockville, Maryland 20850, United States.

ACS Chemical Biology

|March 28, 2023

Summary

Target class profiling identified novel inhibitors for small-molecule methyltransferases (SMMTases). This approach screened 27,574 compounds, leading to a selective inhibitor for histamine N-methyltransferase (HNMT).

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Area of Science:

Chemical Biology
Enzymology
Drug Discovery

Background:

Target class profiling (TCP) investigates understudied biological targets using generalizable assays and compound libraries.
Small-molecule methyltransferases (SMMTases) represent a largely unexplored enzyme subclass.
Previous efforts have not systematically profiled SMMTases for inhibitory activity.

Purpose of the Study:

To apply TCP to the SMMTase class to identify novel inhibitors.
To establish a scalable platform for interrogating SMMTase chemical space.
To develop a foundation for targeted drug discovery within this enzyme family.

Main Methods:

Optimized high-throughput screening (HTS)-amenable assays for six representative SMMTases: NNMT, PNMT, HNMT, GNMT, COMT, and GAMT.
Screened a library of 27,574 unique small molecules against all target enzymes.
Employed TCP principles to systematically investigate inhibitory potential across the SMMTase class.

Main Results:

Identified a novel small molecule exhibiting selective inhibitory activity against histamine N-methyltransferase (HNMT).
Demonstrated the utility of the TCP platform for uncovering SMMTase inhibitors.
Generated a dataset of compound interactions across multiple SMMTases.

Conclusions:

TCP is an effective strategy for exploring understudied target classes like SMMTases.
The developed platform enables efficient screening and identification of selective inhibitors.
This work provides a launchpad for targeted drug discovery campaigns, exemplified by HNMT inhibition.