Gemcitabine anti-proliferative activity significantly enhanced upon conjugation with cell-penetrating peptides

• Type: Article in International Scientific Journal
• Date: 2017

Authors

Nuno Vale (Author) ICBAS; Ferreira, A (Author) Other; Iva Fernandes (Author) FCUP; Alves, C (Author) Other; Maria J Araujo (Author) FCUP; Nuno Mateus (Author) FCUP; Paula Gomes (Author) FCUP

Journal

Title: Bioorganic and Medicinal Chemistry Letters

Vol. 27

Pages: 2898-2901

ISSN: 0960-894X

Publisher: Elsevier

Indexing

ISI Web of Knowledge - 29 Citations

Scopus - 30 Citations

Other information

Authenticus ID: P-00N-23A

DOI: 10.1016/j.bmcl.2017.04.086

Abstract (EN): Gemcitabine proven efficiency against a wide range of solid tumors and undergoes deamination to its inactive uridine metabolite, which underlies its low bioavailability, and tumour resistance was also associated with nucleoside transporter alterations. Hence, we have conjugated gemcitabine to cell-penetrating peptides (CPP), in an effort to both mask its aniline moiety and facilitate its delivery into cancer cells. Two CPP-drug conjugates have been synthesized and studied regarding both the time-dependent kinetics of gemcitabine release and their anti-proliferative activity on three different human cancer cell lines. Results obtained reveal a dramatic increase in the anti-proliferative activity of gemcitabine in vitro, upon conjugation with the CPPs. As such, CPP-gemcitabine conjugates emerge as promising leads for cancer therapy.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 4