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Opioid Tripeptides Hybridized with trans ‐1‐Cinnamylpiperazine as Proliferation Inhibitors of Pancreatic Cancer Cells in Two‐ and Three‐Dimensional in vitro Models
Author(s) -
Laskowska Anna K.,
Puszko Anna K.,
Sosnowski Piotr,
Różycki Krzysztof,
Kosson Piotr,
Matalińska Joanna,
Durlik Marek,
Misicka Aleksandra
Publication year - 2017
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201700453
Subject(s) - pancreatic cancer , tripeptide , gemcitabine , peptidomimetic , in vitro , cancer , cancer research , cancer stem cell , malignancy , cancer cell , autophagy , chemistry , medicine , pharmacology , apoptosis , biology , biochemistry , peptide
According to the World Health Organization, the mortality rate among patients with pancreatic cancer will increase in the upcoming years. Gemcitabine is the first choice for treatment of pancreatic malignancy, but increasing resistance to this drug is decreasing its overall efficacy. Studies on new therapies that target metabolic pathways, growth factor inhibitors, and tumor stroma or tumor stem cells are currently underway in many research groups. Herein we report the bioactive properties (cytotoxicity and hemolytic activity) of synthetic peptidomimetics containing an opioid tripeptide fragment (Tyr‐R 1 ‐R 2 ‐; where R 1 is d ‐Ala or d ‐Thr, and R 2 is Phe or Trp) hybridized with trans ‐1‐cinnamylpiperazine. These compounds are stable in plasma up to 96 h and exhibit low hemotoxicity and good inhibitory effects on cancer cell growth in two‐ and three‐dimensional in vitro models of pancreatic cancer.