Discovery of an NAD<sup>+</sup> analogue with enhanced specificity for PARP1
Xiaonan Zhang, Albert T. Lam, Qinqin Cheng, Valentine V. Courouble, Timothy S. Strutzenberg, Jiawei Li, Yiling Wang, Hua Pei, Bangyan L. Stiles, Stan G. Louie, Patrick R. Griffin, Yong Zhang
Abstract
featuring an adenosyl 3'-azido substitution. Acting as an ADP-ribose donor with high activity and specificity for human PARP1, this compound enables labelling and profiling of possible protein substrates of endogenous PARP1. It provides a unique and valuable tool for studying PARP1 in biology and pathology and may shed light on the development of PARP isoform-specific modulators.
Topics & Concepts
NAD+ kinasePARP1ChemistryPhysicsBiochemistryEnzymePoly ADP ribose polymerasePolymerasePARP inhibition in cancer therapyElectrostatic Discharge in ElectronicsToxin Mechanisms and Immunotoxins