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Lookup NU author(s): Professor Nicola CurtinORCiD
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© 2017, Springer Science+Business Media LLC. This chapter describes the approaches taken in the development of the first PARP inhibitor to enter clinical trial, rucaparib (now called Rubraca), in 2003. We describe the general principles of crystal-based drug design, the purification and crystallization 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 described with reference to its advantages and disadvantages.
Author(s): Canan S, Maegley K, Curtin NJ
Publication type: Book Chapter
Publication status: Published
Book Title: Methods in Molecular Biology
Online publication date: 11/07/2017
Acceptance date: 02/04/2016
Series Title: Methods in Molecular Biology
Publisher: Humana Press Inc.
Place Published: New York
Library holdings: Search Newcastle University Library for this item