A preprint is online where we studied multiple bacterial Arr enzymes that ADP-ribosylate and inactivate rifamycins. Several #PARP inhibitor scaffolds inhibit these enzymes. We also found one that is selective to Arrs.

www.biorxiv.org/content/10.1...

FEBS Press We reveal that PTEN and its conserved putative tankyrase-binding motif (pTBM) originated before tankyrases in evolution. We demonstrate that the pTBM shows no binding to tankyrase ARC domains, but it...

A paper online where we used a range of methods to show that PTEN does not bind tankyrases. Tricky to show that something does not happen. #PARP #tankyrase

febs.onlinelibrary.wiley.com/doi/10.1111/...

Substitutions at the C-8 position of quinazolin-4-ones improve the potency of nicotinamide site binding tankyrase inhibitors Human diphtheria toxin-like ADP-ribosyltransferases, PARPs and tankyrases, transfer ADP-ribosyl groups to other macromolecules, thereby controlling va…

First update from our team in Bluesky. Paper online on tankyrase inhibitors where we explores the nicotinamide site surroundings with the help of Kostakis and Waaler teams. Congrats to Chiara for the meticulous work! #PARP #tankyrase #drugdiscovery

www.sciencedirect.com/science/arti...