ArticlePharmaceutics2019
Octreotide Conjugates for Tumor Targeting and Imaging.
Article in Pharmaceutics, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 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
11 citing papers in PubMed, 24 citations in OpenAlex.
- Octreotide-Mediated Co-Solubilization of Paclitaxel and Docetaxel: A Novel Targeted Formulation for Synergistic Anticancer Chemotherapy.Pharmaceutics · 2026Article
- Functional Peptide-Based Biomaterials for Pharmaceutical Application: Sequences, Mechanisms, and Optimization Strategies.Journal of functional biomaterials · 2026Review
- Cryptophycin unit B analogues.Beilstein journal of organic chemistry · 2025Article
- Optimizing the enzymatic release of MMAE fromFrontiers in pharmacology · 2023Article
- Design, fabrication, and preclinical testing of a miniaturized, multispectral, chip-on-tip, imaging probe for intraluminal fluorescence imaging of the gastrointestinal tract.Frontiers in photonics · 2023Article
- Peptide-Based Strategies for Targeted Tumor Treatment and Imaging.Pharmaceutics · 2021Review
- Linker Hydrophilicity Modulates the Anticancer Activity of RGD-Cryptophycin Conjugates.Chemistry (Weinheim an der Bergstrasse, Germany) · 2021Article
- Cetuximab Conjugated with Octreotide and Entrapped Calcium Alginate-beads for Targeting Somatostatin Receptors.Scientific reports · 2020Article
- Synthesis and Biological Characterization of Monomeric and Tetrameric RGD-Cryptophycin Conjugates.Chemistry (Weinheim an der Bergstrasse, Germany) · 2020Article
- Squaraine Dyes: Molecular Design for Different Applications and Remaining Challenges.Bioconjugate chemistry · 2020Review
- Synthesis and Biological Evaluation of RGD⁻Cryptophycin Conjugates for Targeted Drug Delivery.Pharmaceutics · 2019Article
Corrections and comments
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Authors and funding
15 authors at 4 institutions in 3 countries.
Funding
Abstract
Tumor targeting has emerged as an advantageous approach to improving the efficacy and safety of cytotoxic agents or radiolabeled ligands that do not preferentially accumulate in the tumor tissue. The somatostatin receptors (SSTRs) belong to the G-protein-coupled receptor superfamily and they are overexpressed in many neuroendocrine tumors (NETs). SSTRs can be efficiently targeted with octreotide, a cyclic octapeptide that is derived from native somatostatin. The conjugation of cargoes to octreotide represents an attractive approach for effective tumor targeting. In this study, we conjugated octreotide to cryptophycin, which is a highly cytotoxic depsipeptide, through the protease cleavable Val-Cit dipeptide linker using two different self-immolative moieties. The biological activity was investigated in vitro and the self-immolative part largely influenced the stability of the conjugates. Replacement of cryptophycin by the infrared cyanine dye Cy5.5 was exploited to elucidate the tumor targeting properties of the conjugates in vitro and in vivo. The compound efficiently and selectively internalized in cells overexpressing SSTR2 and accumulated in xenografts for a prolonged time. Our results on the in vivo properties indicate that octreotide may serve as an efficient delivery vehicle for tumor targeting.
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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.