Small-molecule inhibitors of PARPS: from tools for investigating ADP-ribosylation to therapeutics

Ilsa T. Kirby, Michael S. Cohen

Research output: Chapter in Book/Report/Conference proceedingChapter

15 Scopus citations

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.

Original languageEnglish (US)
Title of host publicationCurrent Topics in Microbiology and Immunology
PublisherSpringer-Verlag
Pages211-231
Number of pages21
DOIs
StatePublished - 2019
Externally publishedYes

Publication series

NameCurrent Topics in Microbiology and Immunology
Volume420
ISSN (Print)0070-217X
ISSN (Electronic)2196-9965

ASJC Scopus subject areas

  • Immunology and Allergy
  • Microbiology
  • Immunology
  • Microbiology (medical)

Fingerprint

Dive into the research topics of 'Small-molecule inhibitors of PARPS: from tools for investigating ADP-ribosylation to therapeutics'. Together they form a unique fingerprint.

Cite this