Click chemistry enables preclinical evaluation of targeted epigenetic therapies-Reference-Cited by-同舟云学术

Click chemistry enables preclinical evaluation of targeted epigenetic therapies

Published:2017-06-30 Issue:6345 Volume:356 Page:1397-1401
ISSN:0036-8075
Container-title:Science
language:en
Short-container-title:Science

Author:

Tyler Dean S.¹²,Vappiani Johanna³^ORCID,Cañeque Tatiana⁴⁵⁶^ORCID,Lam Enid Y. N.¹²^ORCID,Ward Aoife³^ORCID,Gilan Omer¹²,Chan Yih-Chih¹^ORCID,Hienzsch Antje⁴⁵⁶^ORCID,Rutkowska Anna³^ORCID,Werner Thilo³^ORCID,Wagner Anne J.³^ORCID,Lugo Dave⁷^ORCID,Gregory Richard⁷^ORCID,Ramirez Molina Cesar⁷^ORCID,Garton Neil⁷^ORCID,Wellaway Christopher R.⁷^ORCID,Jackson Susan¹^ORCID,MacPherson Laura¹²,Figueiredo Margarida¹^ORCID,Stolzenburg Sabine¹^ORCID,Bell Charles C.¹²^ORCID,House Colin¹^ORCID,Dawson Sarah-Jane¹²⁸^ORCID,Hawkins Edwin D.⁹,Drewes Gerard³,Prinjha Rab K.⁷^ORCID,Rodriguez Raphaël⁴⁵⁶,Grandi Paola³^ORCID,Dawson Mark A.¹²⁸¹⁰^ORCID

Affiliation:

1. Cancer Research Division, Peter MacCallum Cancer Centre, Melbourne, Victoria, Australia.

2. Sir Peter MacCallum Department of Oncology, University of Melbourne, Melbourne, Victoria, Australia.

3. Cellzome GmbH, GlaxoSmithKline, Meyerhofstrasse 1, Heidelberg, Germany.

4. Chemical Cell Biology Group, Institut Curie, Paris Sciences et Lettres Research University, 26 Rue d’Ulm, 75248 Paris Cedex 05, France.

5. CNRS UMR3666, 75005 Paris, France.

6. INSERM U1143, 75005 Paris, France.

7. Epigenetics Discovery Performance Unit, Immuno-Inflammation Therapy Area Unit, GlaxoSmithKline, Stevenage, UK.

8. Centre for Cancer Research, University of Melbourne, Melbourne, Victoria, Australia.

9. The Walter and Eliza Hall Institute of Medical Research, Parkville, Victoria, Australia.

10. Department of Haematology, Peter MacCallum Cancer Centre, Melbourne, Victoria, Australia.

Abstract

Are better drugs just a click away? Drugs that show promise in preclinical models often fail in the clinic, in part because of limited information on drug localization within cells and across tissues. In a proof-of-concept study, Tyler et al. applied click chemistry methods to study the localization of bromodomain inhibitors. These are cancer drugs that alter chromatin structure and gene expression. Clickable derivatives of the drugs localized within chromatin and showed that the drugs exhibit distinct modes of binding at responsive and unresponsive genes. In a mouse leukemia model, the click-probes revealed that the drugs accumulate to different extents in the spleen and bone marrow, which are two tissue sources of leukemic cells. Science , this issue p. 1397

Funder

National Health and Medical Research Council of Australia

Publisher

American Association for the Advancement of Science (AAAS)

Subject

Multidisciplinary

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