Inhibitors of nicotinamide N-methyltransferase designed to mimic the methylation reaction transition state

Author:

van Haren Matthijs J.12345,Taig Rebecca12345,Kuppens Jilles12345,Sastre Toraño Javier12345,Moret Ed E.12345,Parsons Richard B.6789,Sartini Davide10111213,Emanuelli Monica10111213,Martin Nathaniel I.12345ORCID

Affiliation:

1. Department of Chemical Biology & Drug Discovery

2. Utrecht Institute for Pharmaceutical Sciences

3. Utrecht University

4. 3584 CG Utrecht

5. The Netherlands

6. Institute of Pharmaceutical Science

7. King's College London

8. London SE1 9NH

9. UK

10. Department of Clinical Sciences

11. Universitá Politecnica delle Marche

12. Ancona

13. Italy

Abstract

Inhibitors designed to simultaneously occupy the different substrate binding pockets of the NNMT active site reveal key structural features required for potent inhibition.

Funder

Nederlandse Organisatie voor Wetenschappelijk Onderzoek

Publisher

Royal Society of Chemistry (RSC)

Subject

Organic Chemistry,Physical and Theoretical Chemistry,Biochemistry

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