Selectivity profile of the poly(ADP-ribose) polymerase (PARP) inhibitor, A-966492

Thorsell, A.-G.; Schuler, H.

doi:10.1101/119818

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bioRxiv · 10.1101/119818

Selectivity profile of the poly(ADP-ribose) polymerase (PARP) inhibitor, A-966492

Thorsell, A.-G.·Schuler, H.

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Abstract

Among the clinical inhibitors of poly(ADP-ribose) polymerases (PARPs) and the commonly used PARP research tool compounds, veliparib and niraparib were recently identified as the most selective inhibitors of PARP1 and PARP2. We characterized the potency of A-966492, a PARP inhibitor with a chemical structure similar to veliparib and niraparib, in in vitro inhibition experiments of six PARP family enzymes. We find that the selectivity of A-966492 for PARP1 and PARP2 is intermediate between veliparib and niraparib.

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Thorsell, A.-G., Schuler, H.. 2017-03-23. Selectivity profile of the poly(ADP-ribose) polymerase (PARP) inhibitor, A-966492. https://doi.org/10.1101/119818

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