Literature DB >> 19354255

Structural basis for inhibitor specificity in human poly(ADP-ribose) polymerase-3.

Lari Lehtiö1, Ann-Sofie Jemth, Ruairi Collins, Olga Loseva, Andreas Johansson, Natalia Markova, Martin Hammarström, Alex Flores, Lovisa Holmberg-Schiavone, Johan Weigelt, Thomas Helleday, Herwig Schüler, Tobias Karlberg.   

Abstract

Poly(ADP-ribose) polymerases (PARPs) activate DNA repair mechanisms upon stress- and cytotoxin-induced DNA damage, and inhibition of PARP activity is a lead in cancer drug therapy. We present a structural and functional analysis of the PARP domain of human PARP-3 in complex with several inhibitors. Of these, KU0058948 is the strongest inhibitor of PARP-3 activity. The presented crystal structures highlight key features for potent inhibitor binding and suggest routes for creating isoenzyme-specific PARP inhibitors.

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Year:  2009        PMID: 19354255     DOI: 10.1021/jm900052j

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  36 in total

1.  Crystal structure of human ADP-ribose transferase ARTD15/PARP16 reveals a novel putative regulatory domain.

Authors:  Tobias Karlberg; Ann-Gerd Thorsell; Åsa Kallas; Herwig Schüler
Journal:  J Biol Chem       Date:  2012-06-01       Impact factor: 5.157

2.  Poly(ADP-ribose) polymerase 3 (PARP3), a newcomer in cellular response to DNA damage and mitotic progression.

Authors:  Christian Boehler; Laurent R Gauthier; Oliver Mortusewicz; Denis S Biard; Jean-Michel Saliou; Anne Bresson; Sarah Sanglier-Cianferani; Susan Smith; Valérie Schreiber; François Boussin; Françoise Dantzer
Journal:  Proc Natl Acad Sci U S A       Date:  2011-01-26       Impact factor: 11.205

3.  PARP-3 is a mono-ADP-ribosylase that activates PARP-1 in the absence of DNA.

Authors:  Olga Loseva; Ann-Sofie Jemth; Helen E Bryant; Herwig Schüler; Lari Lehtiö; Tobias Karlberg; Thomas Helleday
Journal:  J Biol Chem       Date:  2010-01-11       Impact factor: 5.157

Review 4.  PARP inhibition: PARP1 and beyond.

Authors:  Michèle Rouleau; Anand Patel; Michael J Hendzel; Scott H Kaufmann; Guy G Poirier
Journal:  Nat Rev Cancer       Date:  2010-03-04       Impact factor: 60.716

Review 5.  Poly(ADP-ribose) polymerase inhibitors as promising cancer therapeutics.

Authors:  Jin-xue He; Chun-hao Yang; Ze-hong Miao
Journal:  Acta Pharmacol Sin       Date:  2010-08-02       Impact factor: 6.150

6.  Structural basis for lack of ADP-ribosyltransferase activity in poly(ADP-ribose) polymerase-13/zinc finger antiviral protein.

Authors:  Tobias Karlberg; Mirjam Klepsch; Ann-Gerd Thorsell; C David Andersson; Anna Linusson; Herwig Schüler
Journal:  J Biol Chem       Date:  2015-01-29       Impact factor: 5.157

7.  Structural Basis for Potency and Promiscuity in Poly(ADP-ribose) Polymerase (PARP) and Tankyrase Inhibitors.

Authors:  Ann-Gerd Thorsell; Torun Ekblad; Tobias Karlberg; Mirjam Löw; Ana Filipa Pinto; Lionel Trésaugues; Martin Moche; Michael S Cohen; Herwig Schüler
Journal:  J Med Chem       Date:  2016-12-21       Impact factor: 7.446

8.  Family-wide chemical profiling and structural analysis of PARP and tankyrase inhibitors.

Authors:  Elisabet Wahlberg; Tobias Karlberg; Ekaterina Kouznetsova; Natalia Markova; Antonio Macchiarulo; Ann-Gerd Thorsell; Ewa Pol; Åsa Frostell; Torun Ekblad; Delal Öncü; Björn Kull; Graeme Michael Robertson; Roberto Pellicciari; Herwig Schüler; Johan Weigelt
Journal:  Nat Biotechnol       Date:  2012-02-19       Impact factor: 54.908

Review 9.  Beyond DNA repair, the immunological role of PARP-1 and its siblings.

Authors:  Maria Manuela Rosado; Elisabetta Bennici; Flavia Novelli; Claudio Pioli
Journal:  Immunology       Date:  2013-08       Impact factor: 7.397

Review 10.  PARP-1 mechanism for coupling DNA damage detection to poly(ADP-ribose) synthesis.

Authors:  Marie-France Langelier; John M Pascal
Journal:  Curr Opin Struct Biol       Date:  2013-01-16       Impact factor: 6.809

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