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10.1080/15384047.2017.1345384

http://scihub22266oqcxt.onion/10.1080/15384047.2017.1345384
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C5652972!5652972!28692379
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suck abstract from ncbi


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pmid28692379      Cancer+Biol+Ther 2017 ; 18 (8): 571-83
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  • Macrocyclic peptides decrease c-Myc protein levels and reduce prostate cancer cell growth #MMPMID28692379
  • Mukhopadhyay A; Hanold LE; Thayele Purayil H; Gisemba SA; Senadheera SN; Aldrich JV
  • Cancer Biol Ther 2017[]; 18 (8): 571-83 PMID28692379show ga
  • The oncoprotein c-Myc is often overexpressed in cancer cells, and the stability of this protein has major significance in deciding the fate of a cell. Thus, targeting c-Myc levels is an attractive approach for developing therapeutic agents for cancer treatment. In this study, we report the anti-cancer activity of the macrocyclic peptides [D-Trp]CJ-15,208 (cyclo[Phe-D-Pro-Phe-D-Trp]) and the natural product CJ-15,208 (cyclo[Phe-D-Pro-Phe-Trp]). [D-Trp]CJ-15,208 reduced c-Myc protein levels in prostate cancer cells and decreased cell proliferation with IC50 values ranging from 2.0 to 16 µM in multiple PC cell lines. [D-Trp]CJ-15,208 induced early and late apoptosis in PC-3 cells following 48 hours treatment, and growth arrest in the G2 cell cycle phase following both 24 and 48 hours treatment. Down regulation of c-Myc in PC-3 cells resulted in loss of sensitivity to [D-Trp]CJ-15,208 treatment, while overexpression of c-Myc in HEK-293 cells imparted sensitivity of these cells to [D-Trp]CJ-15,208 treatment. This macrocyclic tetrapeptide also regulated PP2A by reducing the levels of its phosphorylated form which regulates the stability of cellular c-Myc protein. Thus [D-Trp]CJ-15,208 represents a new lead compound for the potential development of an effective treatment of prostate cancer.
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