Chapter title |
Small-Molecule Inhibitors of PARPs: From Tools for Investigating ADP-Ribosylation to Therapeutics
|
---|---|
Chapter number | 137 |
Book title |
Activity-Based Protein Profiling
|
Published in |
Current topics in microbiology and immunology, September 2018
|
DOI | 10.1007/82_2018_137 |
Pubmed ID | |
Book ISBNs |
978-3-03-011142-7, 978-3-03-011143-4
|
Authors |
Ilsa T. Kirby, Michael S. Cohen, Kirby, Ilsa T., Cohen, Michael S. |
Abstract |
Over the last 60 years, poly-ADP-ribose polymerases (PARPs, 17 family members in humans) have emerged as important regulators of physiology and disease. Small-molecule inhibitors have been essential tools for unraveling PARP function, and recently the first PARP inhibitors have been approved for the treatment of various human cancers. However, inhibitors have only been developed for a few PARPs and in vitro profiling has revealed that many of these exhibit polypharmacology across the PARP family. In this review, we discuss the history, development, and current state of the field, highlighting the limitations and opportunities for PARP inhibitor development. |
X Demographics
Geographical breakdown
Country | Count | As % |
---|---|---|
United States | 4 | 100% |
Demographic breakdown
Type | Count | As % |
---|---|---|
Scientists | 4 | 100% |
Mendeley readers
Geographical breakdown
Country | Count | As % |
---|---|---|
Unknown | 26 | 100% |
Demographic breakdown
Readers by professional status | Count | As % |
---|---|---|
Student > Bachelor | 5 | 19% |
Student > Ph. D. Student | 4 | 15% |
Student > Postgraduate | 2 | 8% |
Student > Master | 2 | 8% |
Student > Doctoral Student | 1 | 4% |
Other | 4 | 15% |
Unknown | 8 | 31% |
Readers by discipline | Count | As % |
---|---|---|
Chemistry | 6 | 23% |
Biochemistry, Genetics and Molecular Biology | 3 | 12% |
Pharmacology, Toxicology and Pharmaceutical Science | 2 | 8% |
Agricultural and Biological Sciences | 1 | 4% |
Unspecified | 1 | 4% |
Other | 2 | 8% |
Unknown | 11 | 42% |