Chemistries of bifunctional PROTAC degraders.
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DOI: 10.1039/d2cs00220e
Abstract: Proteolysis targeting chimeras (PROTACs) technology is a novel and promising therapeutic strategy using small molecules to induce ubiquitin-dependent degradation of proteins. It has received extensive attention from both academia and industry as it can potentially… read more here.
Keywords: development; chemistries bifunctional; protac degraders; optimization ... See more keywords
Discovery of small molecule ligands for the von Hippel-Lindau (VHL) E3 ligase and their use as inhibitors and PROTAC degraders
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DOI: 10.1039/d2cs00387b
Abstract: The von Hippel-Lindau (VHL) Cullin RING E3 ligase is an essential enzyme in the ubiquitin-proteasome system that recruits substrates such as the hypoxia inducible factor for ubiquitination and subsequent proteasomal degradation. The ubiquitin-proteasome pathway can… read more here.
Keywords: small molecule; molecule ligands; von hippel; protac degraders ... See more keywords
Abstract PR09: KRAS-targeted PROTAC degraders are broadly efficacious against KRAS-dependent tumor models
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DOI: 10.1158/1557-3125.ras23-pr09
Abstract: KRAS is genomically altered in about one third of all human tumors. Due to its central role in oncogenesis, many attempts have been made in the last four decades to drug mutant KRAS, either directly… read more here.
Keywords: kras dependent; targeted protac; mutant kras; kras targeted ... See more keywords