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New Angiopep-Modified Doxorubicin (ANG1007) and Etoposide (ANG1009) Chemotherapeutics With Increased Brain Penetration
Abstract
This report describes the synthesis and preliminary biological characterization of 2 (ANG1007) and 3 (ANG1009), two new chemical entities under development for the treatment of primary and secondary brain cancers. 2 consists of three doxorubicin molecules conjugated to Angiopep-2, a 19-mer peptide that crosses the blood-brain barrier (BBB) by an LRP-1 receptor-mediated transcytosis mechanism. 3 has a similar structure, with the exception that three etoposide moieties are conjugated to Angiopep-2. Both agents killed cancer cell lines in vitro with similar IC(50) values and with apparently similar cytotoxic mechanisms as unconjugated doxorubicin and etoposide. 2 and 3 exhibited dramatically higher BBB influx rate constants than unconjugated doxorubicin and etoposide and pooled within brain parenchymal tissue. Passage through the BBB was similar in Mdr1a (-/-) and wild type mice. These results provide further evidence of the potential of this drug development platform in the isolation of novel therapeutics with increased brain penetration.
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Conjugation of An2 to small therapeutic molecules significantly increased their internalization across the BBTB upon systemic administration.
“Conjugation of this peptide to small therapeutic molecules such as paclitaxel, doxorubicin or etoposide significantly increased their internalization across the BBTB upon systemic administration [20,21].”
From MT1-MMP Expression Levels and Catalytic Functions Dictate LDL Receptor-Related Protein-1 Ligand Internalization Capacity in U87 Glioblastoma Cells (2022) · cites this paper as [20]
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Drug Transport across the Blood–Brain Barrier
Pardridge, W. M. (2012) · Journal of Cerebral Blood Flow & Metabolism · doi:10.1038/jcbfm.2012.126 · Cited by 1,994
A blood–brain barrier overview on structure, function, impairment, and biomarkers of integrity
Kadry, H., Noorani, B., & Cucullo, L. (2020) · Fluids and Barriers of the CNS · doi:10.1186/s12987-020-00230-3 · Cited by 1,853
Vieira, D., & Gamarra, L. (2016) · International Journal of Nanomedicine · doi:10.2147/ijn.s117210 · Cited by 427
Pratt, J., Haidara, K., & Annabi, B. (2022) · International Journal of Molecular Sciences · doi:10.3390/ijms232214214 · Cited by 8
Metadata
- Authors
- Ché, C., Yang, G., Thiot, C., Lacoste, M.-C., Currie, J.-C., Demeule, M., Régina, A., Béliveau, R., & Castaigne, J.-P.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2010-04-08
- Volume
- 53
- Issue
- 7
- Pages
- 2814-2824
- ISSN
- 0022-2623
- 1520-4804
- Cited by
- 123
- References
- 0
- Language
- en
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