ArticleJournal of the American Chemical Society2011
Iterative in situ click chemistry assembles a branched capture agent and allosteric inhibitor for Akt1.
Article in Journal of the American Chemical Society, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
19 citing papers in PubMed, 56 citations in OpenAlex.
- Protein Catalyzed Capture (PCC) Agents for Antigen Targeting.Methods in molecular biology (Clifton, N.J.) · 2022Article
- Peptide-Peptide Co-Assembly: A Design Strategy for Functional Detection of C-peptide, A Biomarker of Diabetic Neuropathy.International journal of molecular sciences · 2020Article
- Protein-Catalyzed Capture Agents.Chemical reviews · 2019Review
- Protein catalyzed capture agents with tailored performance for in vitro and in vivo applications.Biopolymers · 2017Article
- Optimized syntheses of Fmoc azido amino acids for the preparation of azidopeptides.Journal of peptide science : an official publication of the European Peptide Society · 2017Article
- Exploitation of the Ornithine Effect Enhances Characterization of Stapled and Cyclic Peptides.Journal of the American Society for Mass Spectrometry · 2016Article
- Degradation of Akt using protein-catalyzed capture agents.Journal of peptide science : an official publication of the European Peptide Society · 2016Article
- Ribosome-Templated Azide-Alkyne Cycloadditions: Synthesis of Potent Macrolide Antibiotics by In Situ Click Chemistry.Journal of the American Chemical Society · 2016Article
- Approaches to Validate and Manipulate RNA Targets with Small Molecules in Cells.Annual review of pharmacology and toxicology · 2016Review
- Epitope targeting of tertiary protein structure enables target-guided synthesis of a potent in-cell inhibitor of botulinum neurotoxin.Angewandte Chemie (International ed. in English) · 2015Article
- A protein-targeting strategy used to develop a selective inhibitor of the E17K point mutation in the PH domain of Akt1.Nature chemistry · 2015Article
- Investigating fluorescent dyes in fluorescence-assisted screenings.Chemical communications (Cambridge, England) · 2014Article
- A chemical epitope-targeting strategy for protein capture agents: the serine 474 epitope of the kinase Akt2.Angewandte Chemie (International ed. in English) · 2013Article
- Observation of the controlled assembly of preclick components in the in situ click chemistry generation of a chitinase inhibitor.Proceedings of the National Academy of Sciences of the United States of America · 2013Article
- Probing the binding site of abl tyrosine kinase using in situ click chemistry.ACS medicinal chemistry letters · 2013Article
- In situ click chemistry: from small molecule discovery to synthetic antibodies.Integrative biology : quantitative biosciences from nano to macro · 2013Review
- Article
- Selective RNA versus DNA G-quadruplex targeting by in situ click chemistry.Angewandte Chemie (International ed. in English) · 2012Article
- Revolutionizing medicine in the 21st century through systems approaches.Biotechnology journal · 2012Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
13 authors at 4 institutions in 2 countries.
Funding
Abstract
We describe the use of iterative in situ click chemistry to design an Akt-specific branched peptide triligand that is a drop-in replacement for monoclonal antibodies in multiple biochemical assays. Each peptide module in the branched structure makes unique contributions to affinity and/or specificity resulting in a 200 nM affinity ligand that efficiently immunoprecipitates Akt from cancer cell lysates and labels Akt in fixed cells. Our use of a small molecule to preinhibit Akt prior to screening resulted in low micromolar inhibitory potency and an allosteric mode of inhibition, which is evidenced through a series of competitive enzyme kinetic assays. To demonstrate the efficiency and selectivity of the protein-templated in situ click reaction, we developed a novel QPCR-based methodology that enabled a quantitative assessment of its yield. These results point to the potential for iterative in situ click chemistry to generate potent, synthetically accessible antibody replacements with novel inhibitory properties.
Indexed as
Identifiers
What OpenQuestion holds
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.