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Recent advances toward the development of Hsp90 C-terminal inhibitors.

ABSTRACT: Heat shock protein 90 (Hsp90) is a dynamic protein which serves to ensure proper folding of nascent client proteins, regulate transcriptional responses to environmental stress and guide misfolded and damaged proteins to destruction via ubiquitin proteasome pathway. Recent advances in the field of Hsp90 have been made through development of isoform selective inhibitors, Hsp90 C-terminal inhibitors and disruption of protein-protein interactions. These approaches have led to alleviation of adverse off-target effects caused by pan-inhibition of Hsp90 using N-terminal inhibitors. In this review, we provide an overview of relevant advances on targeting the Hsp90 C-terminal Domain (CTD) and the development of Hsp90 C-terminal inhibitors (CTIs) since 2015.

SUBMITTER: Amatya E

PROVIDER: S-EPMC9869726 | biostudies-literature | 2023 Jan

REPOSITORIES: biostudies-literature

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Recent advances toward the development of Hsp90 C-terminal inhibitors.

Amatya Eva E Blagg Brian S J BSJ

Bioorganic & medicinal chemistry letters 20221219

Heat shock protein 90 (Hsp90) is a dynamic protein which serves to ensure proper folding of nascent client proteins, regulate transcriptional responses to environmental stress and guide misfolded and damaged proteins to destruction via ubiquitin proteasome pathway. Recent advances in the field of Hsp90 have been made through development of isoform selective inhibitors, Hsp90 C-terminal inhibitors and disruption of protein-protein interactions. These approaches have led to alleviation of adverse ...[more]

PMID: 36549397

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