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Comment

. 2020 Apr 3;368(6486):30-31.

doi: 10.1126/science.abb1462.

Tuning drug binding

Dea Slade¹, Sebastian Eustermann²

Affiliations

Affiliations

¹ Max Perutz Labs, University of Vienna, Vienna Biocenter, Dr. Bohr-Gasse 9, 1030 Vienna, Austria. dea.slade@univie.ac.at sebastian.eustermann@embl.de.
² Structural and Computational Biology Unit, European Molecular Biology Laboratory (EMBL), Heidelberg, Germany. dea.slade@univie.ac.at sebastian.eustermann@embl.de.

PMID: 32241937
PMCID: PMC7612557
DOI: 10.1126/science.abb1462

Comment

Tuning drug binding

Dea Slade et al. Science. 2020.

. 2020 Apr 3;368(6486):30-31.

doi: 10.1126/science.abb1462.

Authors

Dea Slade¹, Sebastian Eustermann²

Affiliations

¹ Max Perutz Labs, University of Vienna, Vienna Biocenter, Dr. Bohr-Gasse 9, 1030 Vienna, Austria. dea.slade@univie.ac.at sebastian.eustermann@embl.de.
² Structural and Computational Biology Unit, European Molecular Biology Laboratory (EMBL), Heidelberg, Germany. dea.slade@univie.ac.at sebastian.eustermann@embl.de.

PMID: 32241937
PMCID: PMC7612557
DOI: 10.1126/science.abb1462

No abstract available

PubMed Disclaimer

Figures

None — Allosteric modulation
Poly(ADP-ribose) polymerase 1 (PARP-1) is allosterically activated upon binding to single-stranded DNA breaks. Pro-retention and pro-release PARP inhibitors differentially harness PARP-1 allostery to induce PARP-1 trapping or release from DNA, which can be applied in the clinic depending on whether cytotoxicity or cytoprotection is desirable.

See this image and copyright information in PMC

Comment on

Structural basis for allosteric PARP-1 retention on DNA breaks.
Zandarashvili L, Langelier MF, Velagapudi UK, Hancock MA, Steffen JD, Billur R, Hannan ZM, Wicks AJ, Krastev DB, Pettitt SJ, Lord CJ, Talele TT, Pascal JM, Black BE. Zandarashvili L, et al. Science. 2020 Apr 3;368(6486):eaax6367. doi: 10.1126/science.aax6367. Science. 2020. PMID: 32241924 Free PMC article.

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References

1. Slade D. Genes Dev. 2020;34:360. - PMC - PubMed
1. Eustermann S, et al. Mol Cell. 2015;60:742. - PMC - PubMed
1. Langelier MF, et al. Science. 2012;336:728. - PMC - PubMed
1. Hopkins TA, et al. Mol Cancer Res. 2015;13:1465. - PubMed
1. Murai J, et al. Cancer Res. 2012;72:5588. - PMC - PubMed

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