Synthesis of breast cancer targeting conjugate of temporin-SHa analog and its effect on pro- and anti-apoptotic protein expression in MCF-7 cells

Farzana Shaheen, Muhammad Nadeem-ul-Haque, Aqeel Ahmed, Shabana U. Simjee, A. Ganesan, Almas Jabeen, Zafar Ali Shah, M. Iqbal Choudhary

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15 Citations (Scopus)
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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.
Original languageEnglish
Pages (from-to)68-82
Number of pages15
Early online date6 Jul 2018
Publication statusPublished - Aug 2018


  • antimicrobial peptides
  • temporin-SHa analogs
  • breast cancer targeting peptide conjugate
  • apoptosis
  • Bcl-2
  • survivin
  • caspase-3

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