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Design and synthesis of novel peptidomimetics for cancer immunotherapy

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Kose, Ceyda
Uysal, Esra
Yazici, Busra
Dingis-Birgul, Serap Ipek
Yanik, Hamdullah
Tavukcuoglu, Ece
Gulyuz, Sevgi
AKDEMİR, ATİLLA
ESENDAĞLI, GÜNEŞ
Yilmaz, Ozgur

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Tumor cells benefit from some certain signals, which are referred to as -immune checkpoints-, to escape immune-mediated destruction. With that in mind, it is believed that the blockade of these points, such as programmed cell death Ligand-1 (PD-L1) and programmed cell death 1 (PD-1), can restore an adaptative immune response against tumoral cells. In this study, we have designed and synthesized some novel peptidomimetics with a 2-aminobenzathiazole scaffold, which targets the PD-1/PDL-1 pathway. In the viability assay, it was found that these compounds decreased the proliferation of peripheral blood mononuclear cells in the concentration of 10 uM. Overall, our results indicate that these novel compounds are potential checkpoint inhibitors for cancer immunotherapy.

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Kose C., Uysal E., Yazici B., Tugay Z., Dingis-Birgul S. I. , Yanik H., Tavukcuoglu E., Gulyuz S., AKDEMİR A., ESENDAĞLI G., et al., -Design and synthesis of novel peptidomimetics for cancer immunotherapy-, ORGANIC COMMUNICATIONS, cilt.13, ss.89-102, 2020

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