Structure-guided design of an Hsp90β N-terminal isoform-selective inhibitor
The molecular chaperone Hsp90 oversees the folding of many proteins associated with cancer progression but existing small-molecule inhibitors of this pathway are not isoform-selective. Here, the authors rationally design an Hsp90 inhibitor that displays high selectivity for the Hsp90β isoform.
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Nature Portfolio
2018
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oai:doaj.org-article:22d6d57dbf0548efa5ef84106a4676a42021-12-02T16:49:38ZStructure-guided design of an Hsp90β N-terminal isoform-selective inhibitor10.1038/s41467-017-02013-12041-1723https://doaj.org/article/22d6d57dbf0548efa5ef84106a4676a42018-01-01T00:00:00Zhttps://doi.org/10.1038/s41467-017-02013-1https://doaj.org/toc/2041-1723The molecular chaperone Hsp90 oversees the folding of many proteins associated with cancer progression but existing small-molecule inhibitors of this pathway are not isoform-selective. Here, the authors rationally design an Hsp90 inhibitor that displays high selectivity for the Hsp90β isoform.Anuj KhandelwalCaitlin N. KentMaurie BalchShuxia PengSanket J. MishraJunpeng DengVictor W. DayWeiya LiuChitra SubramanianMark CohenJeffery M. HolzbeierleinRobert MattsBrian S. J. BlaggNature PortfolioarticleScienceQENNature Communications, Vol 9, Iss 1, Pp 1-7 (2018) |
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EN |
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Science Q |
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Science Q Anuj Khandelwal Caitlin N. Kent Maurie Balch Shuxia Peng Sanket J. Mishra Junpeng Deng Victor W. Day Weiya Liu Chitra Subramanian Mark Cohen Jeffery M. Holzbeierlein Robert Matts Brian S. J. Blagg Structure-guided design of an Hsp90β N-terminal isoform-selective inhibitor |
description |
The molecular chaperone Hsp90 oversees the folding of many proteins associated with cancer progression but existing small-molecule inhibitors of this pathway are not isoform-selective. Here, the authors rationally design an Hsp90 inhibitor that displays high selectivity for the Hsp90β isoform. |
format |
article |
author |
Anuj Khandelwal Caitlin N. Kent Maurie Balch Shuxia Peng Sanket J. Mishra Junpeng Deng Victor W. Day Weiya Liu Chitra Subramanian Mark Cohen Jeffery M. Holzbeierlein Robert Matts Brian S. J. Blagg |
author_facet |
Anuj Khandelwal Caitlin N. Kent Maurie Balch Shuxia Peng Sanket J. Mishra Junpeng Deng Victor W. Day Weiya Liu Chitra Subramanian Mark Cohen Jeffery M. Holzbeierlein Robert Matts Brian S. J. Blagg |
author_sort |
Anuj Khandelwal |
title |
Structure-guided design of an Hsp90β N-terminal isoform-selective inhibitor |
title_short |
Structure-guided design of an Hsp90β N-terminal isoform-selective inhibitor |
title_full |
Structure-guided design of an Hsp90β N-terminal isoform-selective inhibitor |
title_fullStr |
Structure-guided design of an Hsp90β N-terminal isoform-selective inhibitor |
title_full_unstemmed |
Structure-guided design of an Hsp90β N-terminal isoform-selective inhibitor |
title_sort |
structure-guided design of an hsp90β n-terminal isoform-selective inhibitor |
publisher |
Nature Portfolio |
publishDate |
2018 |
url |
https://doaj.org/article/22d6d57dbf0548efa5ef84106a4676a4 |
work_keys_str_mv |
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_version_ |
1718383264929939456 |