PARP inhibitors : polypharmacology versus selective inhibition
Ekblad, Torun ; Camaioni, Emidio ; Schüler, Herwig LU
and Macchiarulo, Antonio
(2013)
In The FEBS Journal
280(15).
p.75-3563
- Abstract
Inhibition of ADP-ribosyltransferases with diphtheria toxin homology (ARTD), widely known as the poly(ADP-ribose) polymerase (PARP) family, is a strategy under development for treatment of various conditions, including cancers and ischemia. Here, we give a brief summary of ARTD enzyme functions and the implications for their potential as therapeutic targets. We present an overview of the PARP inhibitors that have been used in clinical trials. Finally, we summarize recent insights from structural biology, and discuss the molecular aspects of PARP inhibitors in terms of broad-range versus selective inhibition of ARTD family enzymes.
Please use this url to cite or link to this publication:
https://lup.lub.lu.se/record/aec2aa08-bac3-4d20-9a32-ffa68440052a
- author
- Ekblad, Torun
; Camaioni, Emidio
; Schüler, Herwig
LU
and Macchiarulo, Antonio
- publishing date
- 2013-08
- type
- Contribution to journal
- publication status
- published
- keywords
- Amino Acid Motifs, Animals, Antineoplastic Agents/chemistry, Catalytic Domain, Clinical Trials as Topic, Dacarbazine/analogs & derivatives, Humans, Indoles/chemistry, Models, Molecular, Neoplasms/drug therapy, Poly (ADP-Ribose) Polymerase-1, Poly(ADP-ribose) Polymerase Inhibitors, Temozolomide
- in
- The FEBS Journal
- volume
- 280
- issue
- 15
- pages
- 13 pages
- publisher
- John Wiley & Sons Inc.
- external identifiers
-
- scopus:84880329307
- pmid:23601167
- ISSN
- 1742-464X
- DOI
- 10.1111/febs.12298
- language
- English
- LU publication?
- no
- additional info
- © 2013 The Authors Journal compilation © 2013 FEBS.
- id
- aec2aa08-bac3-4d20-9a32-ffa68440052a
- date added to LUP
- 2024-11-21 17:56:43
- date last changed
- 2025-07-05 12:28:15
@article{aec2aa08-bac3-4d20-9a32-ffa68440052a,
abstract = {{<p>Inhibition of ADP-ribosyltransferases with diphtheria toxin homology (ARTD), widely known as the poly(ADP-ribose) polymerase (PARP) family, is a strategy under development for treatment of various conditions, including cancers and ischemia. Here, we give a brief summary of ARTD enzyme functions and the implications for their potential as therapeutic targets. We present an overview of the PARP inhibitors that have been used in clinical trials. Finally, we summarize recent insights from structural biology, and discuss the molecular aspects of PARP inhibitors in terms of broad-range versus selective inhibition of ARTD family enzymes.</p>}},
author = {{Ekblad, Torun and Camaioni, Emidio and Schüler, Herwig and Macchiarulo, Antonio}},
issn = {{1742-464X}},
keywords = {{Amino Acid Motifs; Animals; Antineoplastic Agents/chemistry; Catalytic Domain; Clinical Trials as Topic; Dacarbazine/analogs & derivatives; Humans; Indoles/chemistry; Models, Molecular; Neoplasms/drug therapy; Poly (ADP-Ribose) Polymerase-1; Poly(ADP-ribose) Polymerase Inhibitors; Temozolomide}},
language = {{eng}},
number = {{15}},
pages = {{75--3563}},
publisher = {{John Wiley & Sons Inc.}},
series = {{The FEBS Journal}},
title = {{PARP inhibitors : polypharmacology versus selective inhibition}},
url = {{http://dx.doi.org/10.1111/febs.12298}},
doi = {{10.1111/febs.12298}},
volume = {{280}},
year = {{2013}},
}