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Photocaged Histone Deacetylase Inhibitors as Prodrugs in Targeted Cancer Therapy
(2023-02-25)
Histone deacetylases (HDACs) play a key role in the control of transcription, cell prolifer-
ation, and migration. FDA-approved histone deacetylase inhibitors (HDACi) demonstrate clinical
efficacy in the treatment of ...
Structure-affinity and structure-residence time relationships of macrocyclic Gαq protein inhibitors
(2023-04-21)
The macrocyclic depsipeptides YM-254890 (YM) and FR900359 (FR) are potent inhibitors of Gαq/11 proteins. They are important pharmacological tools and have potential as therapeutic drugs. The hydrogenated, ...
Development of the first geldanamycin-based HSP90 degraders
(2023-06-28)
Despite the early clinical promise, adverse events such as acquired resistance and dose-limiting toxicities have barred the widespread use of HSP90 inhibitors as anticancer drugs. A new approach involving proteolysis-targeting ...
A Systematic Database Approach to Identify Companion Diagnostic Testing in Clinical Trials under the New In Vitro Diagnostic Medical Devices Regulation
(2023-06-12)
The European Union In Vitro Diagnostic Medical Devices Regulation (EU) 2017/746 (IVDR) introduces companion diagnostics (CDx) as a new legal term. CDx are applied in combination with a medicinal product to identify patient ...






