Selective and reversible modification of kinase cysteines with chlorofluoroacetamides
Selective and reversible modification of kinase cysteines with chlorofluoroacetamides
About this item
Full title
Author / Creator
Shindo, Naoya , Fuchida, Hirokazu , Sato, Mami , Watari, Kosuke , Shibata, Tomohiro , Kuwata, Keiko , Miura, Chizuru , Okamoto, Kei , Hatsuyama, Yuji , Tokunaga, Keisuke , Sakamoto, Seiichi , Morimoto, Satoshi , Abe, Yoshito , Shiroishi, Mitsunori , Caaveiro, Jose M. M. , Ueda, Tadashi , Tamura, Tomonori , Matsunaga, Naoya , Nakao, Takaharu , Koyanagi, Satoru , Ohdo, Shigehiro , Yamaguchi, Yasuchika , Hamachi, Itaru , Ono, Mayumi and Ojida, Akio
Publisher
New York: Nature Publishing Group US
Journal title
Language
English
Formats
Publication information
Publisher
New York: Nature Publishing Group US
Subjects
More information
Scope and Contents
Contents
Irreversible inhibition of disease-associated proteins with small molecules is a powerful approach for achieving increased and sustained pharmacological potency. Here, we introduce α-chlorofluoroacetamide (CFA) as a novel warhead of targeted covalent inhibitor (TCI). Despite weak intrinsic reactivity, CFA-appended quinazoline showed high reactivity...
Alternative Titles
Full title
Selective and reversible modification of kinase cysteines with chlorofluoroacetamides
Authors, Artists and Contributors
Author / Creator
Fuchida, Hirokazu
Sato, Mami
Watari, Kosuke
Shibata, Tomohiro
Kuwata, Keiko
Miura, Chizuru
Okamoto, Kei
Hatsuyama, Yuji
Tokunaga, Keisuke
Sakamoto, Seiichi
Morimoto, Satoshi
Abe, Yoshito
Shiroishi, Mitsunori
Caaveiro, Jose M. M.
Ueda, Tadashi
Tamura, Tomonori
Matsunaga, Naoya
Nakao, Takaharu
Koyanagi, Satoru
Ohdo, Shigehiro
Yamaguchi, Yasuchika
Hamachi, Itaru
Ono, Mayumi
Ojida, Akio
Identifiers
Primary Identifiers
Record Identifier
TN_cdi_proquest_miscellaneous_2179351093
Permalink
https://devfeature-collection.sl.nsw.gov.au/record/TN_cdi_proquest_miscellaneous_2179351093
Other Identifiers
ISSN
1552-4450
E-ISSN
1552-4469
DOI
10.1038/s41589-018-0204-3