| Autor: |
Ziouziou, Hajer, Paris, Clément, Benizri, Sébastien, Le, Thi Khanh, Andrieu, Claudia, Nguyen, Dang Tan, Appavoo, Ananda, Taïeb, David, Brunel, Frédéric, Oueslati, Ridha, Siri, Olivier, Camplo, Michel, Barthélémy, Philippe, Rocchi, Palma, Cosco, Donato |
| Předmět: |
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| Zdroj: |
Pharmaceutics; May2021, Vol. 13 Issue 5, p623, 1p |
| Abstrakt: |
Heat shock protein 27 (Hsp27) has an established role in tumor progression and chemo-resistance of castration-resistant prostate cancer (CRPC). Hsp27 protects eukaryotic translation initiation factor 4E (eIF4E) from degradation, thereby maintaining survival during treatment. Phenazine derivative compound #14 was demonstrated to specifically disrupt Hsp27/eIF4E interaction and significantly delay castration-resistant tumor progression in prostate cancer xenografts. In the present work, various strategies of encapsulation of phenazine #14 with either DOTAU (N-[5′-(2′,3′-dioleoyl)uridine]-N′,N′,N′-trimethylammonium tosylate) and DOU-PEG2000 (5′-PEG2000-2′,3′-dioleoyluridine) nucleolipids (NLs) were developed in order to improve its solubilization, biological activity, and bioavailability. We observed that NLs-encapsulated phenazine #14-driven Hsp27-eIF4E interaction disruption increased cytotoxic effects on castration-resistant prostate cancer cell line and inhibited tumor growth in castration-resistant prostate cancer cell xenografted mice compared to phenazine #14 and NLs alone. Phenazine #14 NL encapsulation might represent an interesting nanostrategy for CRPC therapy. [ABSTRACT FROM AUTHOR] |
| Databáze: |
Complementary Index |
| Externí odkaz: |
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