Drug modulation by nuclear condensates - PubMed (original) (raw)

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Drug modulation by nuclear condensates

Aaron D Viny et al. Science. 2020.

No abstract available

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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.

Comment on

• Partitioning of cancer therapeutics in nuclear condensates.
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