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Mendeley readers
Chapter title |
Strategies Employed for the Development of PARP Inhibitors
|
---|---|
Chapter number | 18 |
Book title |
Poly(ADP-Ribose) Polymerase
|
Published in |
Methods in molecular biology, July 2017
|
DOI | 10.1007/978-1-4939-6993-7_18 |
Pubmed ID | |
Book ISBNs |
978-1-4939-6992-0, 978-1-4939-6993-7
|
Authors |
Stacie Canan, Karen Maegley, Nicola J. Curtin |
Abstract |
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. |
Mendeley readers
The data shown below were compiled from readership statistics for 9 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
Country | Count | As % |
---|---|---|
Unknown | 9 | 100% |
Demographic breakdown
Readers by professional status | Count | As % |
---|---|---|
Student > Ph. D. Student | 3 | 33% |
Student > Bachelor | 2 | 22% |
Student > Doctoral Student | 1 | 11% |
Student > Master | 1 | 11% |
Researcher | 1 | 11% |
Other | 0 | 0% |
Unknown | 1 | 11% |
Readers by discipline | Count | As % |
---|---|---|
Chemistry | 5 | 56% |
Biochemistry, Genetics and Molecular Biology | 1 | 11% |
Pharmacology, Toxicology and Pharmaceutical Science | 1 | 11% |
Unknown | 2 | 22% |