Covalent drug discovery exploiting the new warheads

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Covalent drug forms a covalent bond with desease-related target proteins irreversibly inhibits their function. In order to develop a safe and non-toxic covalent drug, it is important to device new reaction chemistry that realizes a sufficient reactivity and high target selectivity for targeted protein under the complicated biological systems such as our body. Currently, new reaction chemistry is being actively developed all over the world to achieve excellent target selectivity of covalent drugs. In this essay, we intoroduce α-chlorofluoroacetamide and bicyclobutane amide as the new reactive groups for proteineous cysteine of targeted protein and their application to develop targeted covalent inhibitors for the treatment of cancer and infecsious deseases.

Original languageEnglish
Pages (from-to)361-365
Number of pages5
JournalFolia Pharmacologica Japonica
Issue number5
Publication statusPublished - 2022

All Science Journal Classification (ASJC) codes

  • Pharmacology


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