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Chemoproteomics-enabled development of novel cysteine and serine reactive small molecules: from target identification to inhibitor discovery

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Defense Thèse de doctorat : Univ. Genève, 2019 - Sc. 5323 - 2019/04/03
Abstract Covalent inactivation of proteins by small molecules is experiencing an increasing trend in pharmaceutical research. The growth of covalent drugs for targeting known or unknown class of proteins tremendously benefits the modern medications in treatment of human diseases. Chemical proteomics accelerates the discovery of activity-based chemotypes for covalently binding to the active site of nucleophilic amino acid within enzymes. In our work, novel electrophilic chemotypes have been designed and characterized as cysteine and serine reactive small molecules with high selectivity and potency. The research results discussed in this thesis could potentially facilitate our compounds being turned into new promising clinical agents for targeting key proteins involved in various human diseases.
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URN: urn:nbn:ch:unige-1177813
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WANG, Chao. Chemoproteomics-enabled development of novel cysteine and serine reactive small molecules: from target identification to inhibitor discovery. Université de Genève. Thèse, 2019. https://archive-ouverte.unige.ch/unige:117781

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Deposited on : 2019-05-20

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