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Comment
. 2020 Jun 19;368(6497):1314-1315.
doi: 10.1126/science.abc5318.

Drug modulation by nuclear condensates

Aaron D Viny  1   2 , Ross L Levine  3   2
Affiliations
Comment

Drug modulation by nuclear condensates

Aaron D Viny et al. Science. .
No abstract available

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Figures

None
Pharmacophore-specific condensates
Cisplatin and tamoxifen aggregate in transcriptional condensates, affecting their pharmacokinetics. Cisplatin freely diffuses through HP1-labeled heterochromatin and accumulates in MED1 condensates. The BRD4 inhibitor JQ.1 abrogates MED1 condensates and attenuates drug-induced platination. Tamoxifen displaces ERα from target genes, but mutations that induce tamoxifen resistance (mERα) shift affinity as tamoxifen is evicted from transcriptional condensates. BRD4, bromodomain-containing protein 4; ERα, estrogen receptor α; HP1, heterochromatin protein 1; MED1, mediator of RNA polymerase II transcription subunit 1.
See this image and copyright information in PMC

Comment on

  • Partitioning of cancer therapeutics in nuclear condensates.
    Klein IA, Boija A, Afeyan LK, Hawken SW, Fan M, Dall'Agnese A, Oksuz O, Henninger JE, Shrinivas K, Sabari BR, Sagi I, Clark VE, Platt JM, Kar M, McCall PM, Zamudio AV, Manteiga JC, Coffey EL, Li CH, Hannett NM, Guo YE, Decker TM, Lee TI, Zhang T, Weng JK, Taatjes DJ, Chakraborty A, Sharp PA, Chang YT, Hyman AA, Gray NS, Young RA. Klein IA, et al. Science. 2020 Jun 19;368(6497):1386-1392. doi: 10.1126/science.aaz4427. Science. 2020. PMID: 32554597 Free PMC article.

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Publication types