Octreotide Conjugates for Tumor Targeting and Imaging
Abstract
:1. Introduction
2. Materials and Methods
2.1. Synthesis and Structural Characterization of Compounds 1–8
2.2. Biological Evaluation
3. Results and Discussion
3.1. Design and Synthesis of Octreotide-cryptophycin Conjugates
3.2. Binding Affinity
3.3. In Vitro Cytotoxicity
3.4. Plasma Stability
3.5. Receptor and Conjugate Internalization
3.6. In Vivo Tumor Imaging
3.7. In Vivo Antitumor Activity
3.8. Cathepsin B Stability
4. Conclusions
Supplementary Materials
Author Contributions
Funding
Acknowledgments
Conflicts of Interest
References
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Entry | Compound | Binding Affinity (IC50 in nM) | Cytotoxicity in AtT20 (IC50 in nM) | Plasma Stability (t1/2 in h) | |
---|---|---|---|---|---|
Murine | Human | ||||
1 | Cry-55 gly (3) | n.d. | 3.53 | > 24 [48] | > 24 [48] |
2 | Oct-PG-Cry (7) | 0.6 | 51.23 | 0.5 | 23 |
3 | Oct-GP-Cry (8) | 1.3 | 8.37 | > 24 | 24 |
4 | GP-Cry-55 gly | n.d. | 6.05 | n.d. | n.d. |
5 | Oct-GP-Cy5.5 (10) | 0.9 | n.d. | n.d. | n.d. |
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Figueras, E.; Martins, A.; Borbély, A.; Le Joncour, V.; Cordella, P.; Perego, R.; Modena, D.; Pagani, P.; Esposito, S.; Auciello, G.; et al. Octreotide Conjugates for Tumor Targeting and Imaging. Pharmaceutics 2019, 11, 220. https://doi.org/10.3390/pharmaceutics11050220
Figueras E, Martins A, Borbély A, Le Joncour V, Cordella P, Perego R, Modena D, Pagani P, Esposito S, Auciello G, et al. Octreotide Conjugates for Tumor Targeting and Imaging. Pharmaceutics. 2019; 11(5):220. https://doi.org/10.3390/pharmaceutics11050220
Chicago/Turabian StyleFigueras, Eduard, Ana Martins, Adina Borbély, Vadim Le Joncour, Paola Cordella, Raffaella Perego, Daniela Modena, Paolo Pagani, Simone Esposito, Giulio Auciello, and et al. 2019. "Octreotide Conjugates for Tumor Targeting and Imaging" Pharmaceutics 11, no. 5: 220. https://doi.org/10.3390/pharmaceutics11050220