Protacs: Chimeric molecules that target proteins to the Skp1–Cullin–F box complex for ubiquitination and degradation
By K. Sakamoto, K. Kim, A. Kumagai, F. Mercurio, C. Crews, R. Deshaies. Proceedings of the National Academy of Sciences of the United States of America, 2001
2,057 citations recorded by the source corpus.
Subfields: Molecular Biology, Oncology
View Paper: https://www.semanticscholar.org/paper/53e75ae544c5452ade95ef995e3e1566405ebce3
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In Molecular Biology
- Masato T. Kanemaki
- George M. Burslem
- C. Crews
- M. Pettersson
- Jose M. Duarte
- Stephen K. Burley
- Christine Zardecki
- David S. Goodsell
In Oncology
Citations in the corpus
- Proteolysis Targeting Chimeras as Therapeutics and Tools for Biological Discovery (2020, positive): “Beginning with proof-of-concept experiments in cell lysates with peptidic ligands (Sakamoto et al., 2001), the technology has matured and is routinely used in cultured cells, in vivo and has even entered clinical trials.”
- PROteolysis TArgeting Chimeras (PROTACs) - Past, Present and Future (2019, background): “Peptide ligands for E3s have also been used with some success – the very first PROTAC recruited ß-TRCP by use of a peptide ligand; and a more recent PROTAC that contains a Keap1-binding peptide was able to recruit the Keap1 E3 to successfully induce degradation of the Tau protein [30,33].”
- Lessons in PROTAC design from selective degradation with a promiscuous warhead (2017, background): “Since 2001, our laboratory and others have worked to develop an alternative targeting strategy that induces selective protein degradation (Sakamoto et al., 2001; Toure and Crews, 2016).”
- Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4. (2015, background): “…2015 ª2015 Elsevier Ltd All rights reserved 755 to the E3 ubiquitin ligase VHL (Von Hippel-Lindau) for ubiquitination and subsequent proteasome-mediated degradation (Buckley and Crews, 2014; Raina and Crews, 2010; Sakamoto et al., 2001, 2003; Schneekloth and Crews, 2005; Schneekloth et al., 2004).”
- RCSB Protein Data Bank: Enabling biomedical research and drug discovery (2019, background): “101 Recently deposited PDB MX structures have revealed at the atomic level how such a degrader links the chromatin-reader protein Brd4 (bromodomain-containing protein 4), a target for cancer therapy, with ubiquitin ligase complexes, such as von Hippel – Lindau disease tumor…”