Front Cover: Identification of Novel Histone Deacetylase 6‐Selective Inhibitors Bearing 3,3,3‐Trifluorolactic Amide (TFLAM) Motif as a Zinc Binding Group (ChemBioChem 22/2021)

This picture shows the 3,3,3‐trifluorolactic amide (TFLAM) motif which chelates the zinc ion of histone deacetylase 6 (HDAC6). To identify non‐hydroxamate HDAC6 inhibitors for the treatment of cancer and immunological diseases, the TFMAL motif was discovered by screening a metal chelator chemical li...

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Bibliographic Details
Published inChembiochem : a European journal of chemical biology Vol. 22; no. 22; p. 3107
Main Authors Kurohara, Takashi, Tanaka, Keita, Takahashi, Daisuke, Ueda, Satoshi, Yamashita, Yasunobu, Takada, Yuri, Takeshima, Hirokazu, Yu, Shengwang, Itoh, Yukihiro, Hase, Koji, Suzuki, Takayoshi
Format Journal Article
LanguageEnglish
Published 16.11.2021
Subjects
drug discovery
fluorine
HDAC6
medicinal chemistry
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Summary:This picture shows the 3,3,3‐trifluorolactic amide (TFLAM) motif which chelates the zinc ion of histone deacetylase 6 (HDAC6). To identify non‐hydroxamate HDAC6 inhibitors for the treatment of cancer and immunological diseases, the TFMAL motif was discovered by screening a metal chelator chemical library. Subsequent structure‐based drug design led to the discovery of compounds that exhibit sufficient HDAC6 inhibitory activity and selectivity in both in vitro and in cellulo experiments. More information can be found in the Communication by T. Suzuki et al.
ISSN:1439-4227
1439-7633
DOI:10.1002/cbic.202100350