ArticleAngewandte Chemie (International ed. in English)2016
Integrin-Targeting Knottin Peptide-Drug Conjugates Are Potent Inhibitors of Tumor Cell Proliferation.
Article in Angewandte Chemie (International ed. in English), 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 40 papers.
What it found
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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
40 citing papers in PubMed, 81 citations in OpenAlex.
- Tangled Tail of Mechanically Interlocked Peptides.Journal of the American Chemical Society · 2026Review
- Targeted drug conjugates and molecular mechanisms in overcoming lung cancer drug resistance.Discover oncology · 2025Review
- Recent Advances in Augmenting the Therapeutic Efficacy of Peptide-Drug Conjugates.Journal of medicinal chemistry · 2025Review
- Triscysteine disulfide-directing motifs enabling design and discovery of multicyclic peptide binders.Nature communications · 2024Article
- Plant peptides - redefining an area of ribosomally synthesized and post-translationally modified peptides.Natural product reports · 2024Review
- A humanized trivalent Nectin-4-targeting nanobody drug conjugate displays potent antitumor activity in gastric cancer.Journal of nanobiotechnology · 2024Article
- Drug conjugates for the treatment of lung cancer: from drug discovery to clinical practice.Experimental hematology & oncology · 2024Review
- Extracellular targeted protein degradation: an emerging modality for drug discovery.Nature reviews. Drug discovery · 2024Review
- Advancing Ovarian Cancer Therapeutics: The Role of Targeted Drug Delivery Systems.International journal of nanomedicine · 2024Review
- Research advances in peptide‒drug conjugates.Acta pharmaceutica Sinica. B · 2023Review
- Synthesis and Evaluation of a Monomethyl Auristatin E─Integrin αJournal of medicinal chemistry · 2023Article
- Targeted TLR9 Agonist Elicits Effective Antitumor Immunity against Spontaneously Arising Breast Tumors.Journal of immunology (Baltimore, Md. : 1950) · 2023Article
- The Role of Integrins for Mediating Nanodrugs to Improve Performance in Tumor Diagnosis and Treatment.Nanomaterials (Basel, Switzerland) · 2023Review
- Targeted Drug Delivery Using a Plug-to-Direct Antibody-Nanogel Conjugate.Biomacromolecules · 2023Article
- In Silico Analysis of aPathogens (Basel, Switzerland) · 2023Article
- Protein scaffolds: antibody alternatives for cancer diagnosis and therapy.RSC chemical biology · 2022Review
- Peptides to Overcome the Limitations of Current Anticancer and Antimicrobial Nanotherapies.Pharmaceutics · 2022Review
- Cystine Knot Peptides with Tuneable Activity and Mechanism.Angewandte Chemie (International ed. in English) · 2022Article
- Systemic delivery of a targeted synthetic immunostimulant transforms the immune landscape for effective tumor regression.Cell chemical biology · 2022Article
- Protease-Resistant Peptides for Targeting and Intracellular Delivery of Therapeutics.Pharmaceutics · 2021Review
Corrections and comments
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Authors and funding
5 authors at 2 institutions in 1 country.
Funding
Abstract
Antibody-drug conjugates (ADCs) offer increased efficacy and reduced toxicity compared to systemic chemotherapy. Less attention has been paid to peptide-drug delivery, which has the potential for increased tumor penetration and facile synthesis. We report a knottin peptide-drug conjugate (KDC) and demonstrate that it can selectively deliver gemcitabine to malignant cells expressing tumor-associated integrins. This KDC binds to tumor cells with low-nanomolar affinity, is internalized by an integrin-mediated process, releases its payload intracellularly, and is a highly potent inhibitor of brain, breast, ovarian, and pancreatic cancer cell lines. Notably, these features enable this KDC to bypass a gemcitabine-resistance mechanism found in pancreatic cancer cells. This work expands the therapeutic relevance of knottin peptides to include targeted drug delivery, and further motivates efforts to expand the drug-conjugate toolkit to include non-antibody protein scaffolds.
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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.