ArticleBioorganic & medicinal chemistry2011
Synthesis and biological evaluation of a peptide-paclitaxel conjugate which targets the integrin αvβ₆.
Article in Bioorganic & medicinal chemistry, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers, 1 of them a synthesis that pooled it.
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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.
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Who cites it
14 citing papers in PubMed, 1 synthesis or guideline pooled it, 28 citations in OpenAlex.
- Nanocarrier-Based Drug Delivery Systems for Lung Cancer: A Systematic Review and Meta-Analysis of Preclinical Studies.Advances in respiratory medicine · 2026Pooled it
- Peptide Aptamer-Paclitaxel Conjugates for Tumor Targeted Therapy.Pharmaceutics · 2024Review
- Recent Advances in Targeted Drug Delivery Strategy for Enhancing Oncotherapy.Pharmaceutics · 2023Review
- Delivery of Theranostic Nanoparticles to Various Cancers by Means of Integrin-Binding Peptides.International journal of molecular sciences · 2022Review
- Synthesis and Feasibility Evaluation of a new Trastuzumab Conjugate Integrated with Paclitaxel andChemistryOpen · 2019Article
- Site-Specific Antibody Functionalization Using Tetrazine-Styrene Cycloaddition.Bioconjugate chemistry · 2018Article
- Tumor-targeting peptides from combinatorial libraries.Advanced drug delivery reviews · 2017Review
- Guidance of Signaling Activations by Cadherins and Integrins in Epithelial Ovarian Cancer Cells.International journal of molecular sciences · 2016Review
- Tumor-selective peptide-carrier delivery of Paclitaxel increases in vivo activity of the drug.Scientific reports · 2015Article
- Identification of a novel lysosomal trafficking peptide using phage display biopanning coupled with endocytic selection pressure.Bioconjugate chemistry · 2014Article
- Combinatorial peptide libraries: mining for cell-binding peptides.Chemical reviews · 2014Review
- Molecular imaging of integrin αvβ6 expression in living subjects.American journal of nuclear medicine and molecular imaging · 2014Review
- Tumor Targeting via Integrin Ligands.Frontiers in oncology · 2013Review
- A liposomal drug platform overrides peptide ligand targeting to a cancer biomarker, irrespective of ligand affinity or density.PloS one · 2013Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
The integrin α(v)β(6) is an emergent biomarker for non-small cell lung cancer (NSCLC) as well as other carcinomas. We previously developed a tetrameric peptide, referred to as H2009.1, which binds α(v)β(6) and displays minimal affinity for other RGD-binding integrins. Here we report the use of this peptide to actively deliver paclitaxel to α(v)β(6)-positive cells. We synthesized a water soluble paclitaxel-H2009.1 peptide conjugate in which the 2'-position of paclitaxel is attached to the tetrameric peptide via an ester linkage. The conjugate maintains its specificity for α(v)β(6)-expressing NSCLC cells, resulting in selective cytotoxicity. Treatment of α(v)β(6)-positive cells with the conjugate results in cell cycle arrest followed by induction of apoptosis in the same manner as free paclitaxel. However, initiation of apoptosis and the resultant cell death is delayed compared to free drug. The conjugate demonstrates anti-tumor activity in a H2009 xenograft model of NSCLC with efficacy comparable to treatment with free paclitaxel.
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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.