PROTAC-mediated degradation of KRAS protein for anticancer therapeutics
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ADVERTISEMENT RETURN TO ISSUEPREVPatent HighlightNEXTPROTAC-Mediated Degradation of KRAS Protein for Anticancer TherapeuticsRobert B. Kargbo*Robert B. KargboUsona Institute, 277 Granada Drive, San Luis Obispo, California 93401-7337, United States*E-mail: [email protected]More by Robert B. Kargbohttp://orcid.org/0000-0002-5539-6343Cite this: ACS Med. Chem. Lett. 2020, 11, 1, 5–6Publication Date (Web):December 23, 2019Publication History Received8 December 2019Published online23 December 2019Published inissue 9 January 2020https://pubs.acs.org/doi/10.1021/acsmedchemlett.9b00584https://doi.org/10.1021/acsmedchemlett.9b00584editorialACS PublicationsCopyright © 2019 American Chemical Society. This publication is available under these Terms of Use. Request reuse permissions This publication is free to access through this site. Learn MoreArticle Views9200Altmetric-Citations18LEARN ABOUT THESE METRICSArticle Views are the COUNTER-compliant sum of full text article downloads since November 2008 (both PDF and HTML) across all institutions and individuals. These metrics are regularly updated to reflect usage leading up to the last few days.Citations are the number of other articles citing this article, calculated by Crossref and updated daily. Find more information about Crossref citation counts.The Altmetric Attention Score is a quantitative measure of the attention that a research article has received online. Clicking on the donut icon will load a page at altmetric.com with additional details about the score and the social media presence for the given article. Find more information on the Altmetric Attention Score and how the score is calculated. Share Add toView InAdd Full Text with ReferenceAdd Description ExportRISCitationCitation and abstractCitation and referencesMore Options Share onFacebookTwitterWechatLinked InRedditEmail PDF (528 KB) Get e-AlertscloseSUBJECTS:Cancer,Cells,Degradation,Genetics,Peptides and proteins Get e-Alerts
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Covalent KRASG12C PROTACs are not catalytic, and their advantages over covalent KRASG12C inhibitors are unclear.
“Covalent inhibitors that target KRASG12C in its GDP-bound “OFF” state have been successfully converted into PROTACs but such covalent PROTACs are not catalytic, and it is unclear what advantages they possess beyond covalent KRAS-G12C inhibitors (52, 53).”
From Expanding the Reach of Precision Oncology by Drugging All <i>KRAS</i> Mutants (2022) · cites this paper as [53]
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- Authors
- Kargbo, R. B.
- Affiliations
- Usona Institute (US)
- Corresponding author
- Kargbo, Robert B.
- ORCID
- Kargbo, Robert B.
- Venue
- ACS Medicinal Chemistry Letters
- Publisher
- American Chemical Society (ACS)
- Published
- 2019-12-23
- Volume
- 11
- Issue
- 1
- Pages
- 5-6
- ISSN
- 1948-5875 (ISSN-L)
- PMC
- PMC6956371
- OpenAlex
- W2997874238
- Cited by
- 30
- References
- 5
- Citations by year
- 2026: 1 · 2025: 7 · 2024: 4 · 2023: 7 · 2022: 5 · 2021: 6
- Type
- journal article
- Language
- en
- Open access
- green
- europepmc.org
- Licence
- Locations
- ACS Medicinal Chemistry Letters (publishedVersion)
- Europe PMC (PubMed Central) (publishedVersion)
- PubMed Central (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Degradation and Inhibitors
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Chemical Synthesis and Analysis
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Ubiquitin and proteasome pathways
- Keywords
- PROTACs, KRAS, protein degradation, targeted protein degradation, anticancer agents, cancer therapy
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