Toggle Main Menu Toggle Search

Open Access padlockePrints

Strategies Employed for the Development of PARP Inhibitors

Lookup NU author(s): Professor Nicola Curtin

Downloads

Full text for this publication is not currently held within this repository. Alternative links are provided below where available.


Abstract

© 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.


Publication metadata

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

Publication type: Book Chapter

Publication status: Published

Book Title: Methods in Molecular Biology

Year: 2017

Volume: 1608

Pages: 271-297

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

URL: https://doi.org/10.1007/978-1-4939-6993-7_18

DOI: 10.1007/978-1-4939-6993-7_18

Library holdings: Search Newcastle University Library for this item

ISBN: 9781493969937


Actions

Link to this publication


Share