ArticleJournal of peptide science : an official publication of the European Peptide Society2016
Degradation of Akt using protein-catalyzed capture agents.
Article in Journal of peptide science : an official publication of the European Peptide Society, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 29 papers.
What it found
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
29 citing papers in PubMed, 43 citations in OpenAlex.
- A renaissance in targeting the PI3K/AKT/mTOR pathway.Nature reviews. Drug discovery · 2026Review
- Review
- Protein-Based Degraders: From Chemical Biology Tools to Neo-Therapeutics.Chemical reviews · 2025Review
- Promising Proteolysis-Targeting Chimera for Mutant p53-R175H.ACS omega · 2024Article
- Characteristic roadmap of linker governs the rational design of PROTACs.Acta pharmaceutica Sinica. B · 2024Review
- Targeted Degradation of Protein Kinase A via a Stapled Peptide PROTAC.ACS chemical biology · 2024Article
- Opportunities and challenges of protein-based targeted protein degradation.Chemical science · 2023Review
- Beyond canonical PROTAC: biological targeted protein degradation (bioTPD).Biomaterials research · 2023Review
- Computer-Aided Identification of Kinase-Targeted Small Molecules for Cancer: A Review on AKT Protein.Pharmaceuticals (Basel, Switzerland) · 2023Review
- Stereochemical engineering yields a multifunctional peptide macrocycle inhibitor of Akt2 by fine-tuning macrocycle-cell membrane interactions.Communications chemistry · 2023Article
- PROTACs: Emerging Targeted Protein Degradation Approaches for Advanced Druggable Strategies.Molecules (Basel, Switzerland) · 2023Review
- Molecular Glues: The Adhesive Connecting Targeted Protein Degradation to the Clinic.Biochemistry · 2023Review
- An overview of PROTACs: a promising drug discovery paradigm.Molecular biomedicine · 2022Review
- Non-small molecule PROTACs (NSM-PROTACs): Protein degradation kaleidoscope.Acta pharmaceutica Sinica. B · 2022Review
- Protein Catalyzed Capture (PCC) Agents for Antigen Targeting.Methods in molecular biology (Clifton, N.J.) · 2022Article
- Review
- Kinase drug discovery 20 years after imatinib: progress and future directions.Nature reviews. Drug discovery · 2021Review
- The Potential of Proteolytic Chimeras as Pharmacological Tools and Therapeutic Agents.Molecules (Basel, Switzerland) · 2020Review
- The peptide PROTAC modality: a novel strategy for targeted protein ubiquitination.Theranostics · 2020Review
- Protein-Catalyzed Capture Agents.Chemical reviews · 2019Review
Corrections and comments
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Authors and funding
8 authors at 1 institution in 1 country.
Funding
Abstract
Abnormal signaling of the protein kinase Akt has been shown to contribute to human diseases such as diabetes and cancer, but Akt has proven to be a challenging target for drugging. Using iterative in situ click chemistry, we recently developed multiple protein-catalyzed capture (PCC) agents that allosterically modulate Akt enzymatic activity in a protein-based assay. Here, we utilize similar PCCs to exploit endogenous protein degradation pathways. We use the modularity of the anti-Akt PCCs to prepare proteolysis targeting chimeric molecules that are shown to promote the rapid degradation of Akt in live cancer cells. These novel proteolysis targeting chimeric molecules demonstrate that the epitope targeting selectivity of PCCs can be coupled with non-traditional drugging moieties to inhibit challenging targets.
Indexed as
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.