TY - JOUR
T1 - Small-Molecule Inhibitors of PARPs
T2 - From Tools for Investigating ADP-Ribosylation to Therapeutics
AU - Kirby, Ilsa T.
AU - Cohen, Michael
PY - 2019/1/1
Y1 - 2019/1/1
N2 - 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.
AB - 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.
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U2 - 10.1007/82_2018_137
DO - 10.1007/82_2018_137
M3 - Article
C2 - 30242511
AN - SCOPUS:85059827534
VL - 420
SP - 211
EP - 231
JO - Ergebnisse der Hygiene, Bakteriologie, Immunitätsforschung und experimentellen Therapie
JF - Ergebnisse der Hygiene, Bakteriologie, Immunitätsforschung und experimentellen Therapie
SN - 0070-217X
ER -