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Strategies employed for the development of PARP inhibitors

Lookup NU author(s): Professor Nicola CurtinORCiD


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This chapter describes the approaches taken in the development of the first PARP inhibitor to enter clinical trial, AG-014699, in 2003. We describe the general principles of crystal-based drug design, the purification and crystallisation of the PARP-1 catalytic domain and how this was used to develop highly potent PARP inhibitors, based on the nicotinamide pharmacophore. Several methods have been used to determine the inhibitory potency in cell-free and whole cell assays, each is described with reference to its advantages and disadvantages.

Publication metadata

Author(s): Canan S, Maegley K, Curtin N

Editor(s): Virag, A.

Publication type: Book Chapter

Publication status: Published

Book Title: Poly(ADP-ribose) Polymerase: Methods and Protocols

Year: 2011

Volume: 780

Pages: 463-89

Series Title: Methods in Molecular Biology

Publisher: Humana Press, Inc.

Place Published: New York, USA


DOI: 10.1007/978-1-61779-270-0_28

Library holdings: Search Newcastle University Library for this item

ISBN: 9781617792694