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Partitioning of cancer therapeutics in nuclear condensates

Authors :
Arup K. Chakraborty
Jesse M. Platt
Ozgur Oksuz
Tim-Michael Decker
Nathanael S. Gray
Richard A. Young
Yang Eric Guo
Jonathan E. Henninger
John C. Manteiga
Mengyang Fan
Patrick M. McCall
Alicia V. Zamudio
Eliot L. Coffey
Alessandra Dall’Agnese
Phillip A. Sharp
Lena K. Afeyan
Isaac A. Klein
Nancy M. Hannett
Krishna Shrinivas
Victoria E. Clark
Benjamin R. Sabari
Ann Boija
Mrityunjoy Kar
Charles H. Li
Anthony A. Hyman
Dylan J. Taatjes
Jing-Ke Weng
Susana Wilson Hawken
Ido Sagi
Tinghu Zhang
Young-Tae Chang
Tong Ihn Lee
Source :
Science, PMC
Publication Year :
2020

Abstract

Drug partitioning in nuclear condensates There is increasing interest in the function of phase-separated biomolecular condensates in cells because of their distinct properties and expanding roles in important biological processes. Klein et al. considered the fate of small-molecule therapeutics in the context of nuclear condensates (see the Perspective by Viny and Levine). They show that certain antineoplastic drugs have physicochemical properties that cause them to concentrate preferentially in condensates, both in vitro and in cancer cells. This property influences drug activity, and protein mutations that alter condensate formation can lead to drug resistance. Optimizing condensate partitioning may be valuable in developing improved therapeutics. Science , this issue p. 1386 ; see also p. 1314

Details

Language :
English
Database :
OpenAIRE
Journal :
Science, PMC
Accession number :
edsair.doi.dedup.....58dbfd9ca343e2e0aae160b9eb4e7eba