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- W4313236769 abstract "Targeted protein degradation (TPD) strategies open up new avenues for therapeutics and provide powerful tools for biological inquiry. Herein, we present a brand-new approach, termed heat shock protein 90 (HSP90)–mediated targeting chimeras (HEMTACs), to induce intracellular protein degradation by bridging a target protein to HSP90 to drive the downregulation of proteins. We successfully showcase HEMTACs for cyclin-dependent kinase 4 and 6 (CDK4/6) by using a flexible linker to connect the targeting warhead of CDK4/6 with the HSP90 ligand. Overall, our study delivers a series of evidence that HEMTACs can serve as a valuable addition to TPD strategies, most prominently proteolysis-targeting chimera technology." @default.
- W4313236769 created "2023-01-06" @default.
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- W4313236769 date "2022-12-27" @default.
- W4313236769 modified "2023-10-11" @default.
- W4313236769 title "Targeted Protein Degradation Induced by HEMTACs Based on HSP90" @default.
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- W4313236769 doi "https://doi.org/10.1021/acs.jmedchem.2c01648" @default.
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