Synthesis of Breast Cancer Targeting Conjugate of Temporin-SHa Analog and its Effect on Pro- and Anti-Apoptotic Protein Expression in MCF-7 Cells

Shaheen, Farzana, Nadeem-ul-Haque, Muhammad, Ahmed, Aqeel, Simjee, Shabana U., Ganesan, A., Jabeen, Almas, Shah, Zafar Ali and Choudhary, M. Iqbal (2018) Synthesis of Breast Cancer Targeting Conjugate of Temporin-SHa Analog and its Effect on Pro- and Anti-Apoptotic Protein Expression in MCF-7 Cells. Peptides, 106. pp. 68-82. ISSN 0196-9781

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Abstract

The frog natural product temporin-SHa (FLSGIVGMLGKLFamide) is a potent antimicrobial peptide, as is the analog [S3K]SHa. By solid-phase synthesis, we prepared temporin-SHa and several temporin-SHa analogs with one or more D-alanine residues incorporated. The natural product and the analog [G10a]SHa were found to be cytotoxic in mammalian cell lines and induce cell death. To achieve selectivity, we conjugated the analog [G10a]SHa with a breast cancer targeting peptide (BCTP). The resulting peptide temporin [G10a]SHa-BCTP conjugate was selectively active against the MCF-7 breast cancer cell line with no cytotoxicity in NIH-3T3 fibroblasts. Unlike the natural product or [G10a]SHa, the conjugated peptide induced apoptosis, down regulating the expression of Bcl-2 and survivin and up regulating Bax and caspase-3.

Item Type: Article
Uncontrolled Keywords: antimicrobial peptides,temporin-sha analogs,breast cancer targeting peptide conjugate,apoptosis,bcl-2,survivin,caspase-3
Faculty \ School: Faculty of Science > School of Pharmacy
Related URLs:
Depositing User: LivePure Connector
Date Deposited: 13 Jul 2018 09:31
Last Modified: 18 Mar 2020 01:42
URI: https://ueaeprints.uea.ac.uk/id/eprint/67613
DOI: 10.1016/j.peptides.2018.07.002

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