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Comment
. 2020 Apr 3;368(6486):30-31.
doi: 10.1126/science.abb1462.

Tuning drug binding

Dea Slade  1 , Sebastian Eustermann  2
Affiliations
Comment

Tuning drug binding

Dea Slade et al. Science. .
No abstract available

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Figures

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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.

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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