Lookup NU author(s): Professor Nicola Curtin
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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.
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
Series Title: Methods in Molecular Biology
Publisher: Humana Press, Inc.
Place Published: New York, USA
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