Design and synthesis of novel peptidomimetics for cancer immunotherapy

Ceyda Köse; Esra Uysal; Büşra Yazıcı; Zeynep Tuğay; Serap İpek Dingiş Birgül; Hamdullah Yanık; Ece Tavukçuoğlu; Sevgi Gülyüz; Atilla Akdemir; Güneş Esendağlı; Özgür Yılmaz; Onur Alptürk

doi:10.25135/acg.oc.86.20.09.1802

Design and synthesis of novel peptidomimetics for cancer immunotherapy

Ceyda Köse, Esra Uysal, Büşra Yazıcı, Zeynep Tuğay, Serap İpek Dingiş Birgül, Hamdullah Yanık, Ece Tavukçuoğlu, Sevgi Gülyüz, Atilla Akdemir, Güneş Esendağlı, Özgür Yılmaz^*, Onur Alptürk

^*Corresponding author for this work

Department of Chemistry

Research output: Contribution to journal › Article › peer-review

2 Citations (Scopus)

Abstract

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.

Original language	English
Pages (from-to)	89-102
Number of pages	14
Journal	Organic Communications
Volume	13
Issue number	3
DOIs	https://doi.org/10.25135/acg.oc.86.20.09.1802
Publication status	Published - 2020

Bibliographical note

Publisher Copyright:
©2020 ACG Publications. All right reserved.

Keywords

2-aminobenzothiazole
Immunotherapy
PD-1
PD-L1
peptidomimetics

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.25135/acg.oc.86.20.09.1802

Cite this

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title = "Design and synthesis of novel peptidomimetics for cancer immunotherapy",

abstract = "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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author = "Ceyda K{\"o}se and Esra Uysal and B{\"u}{\c s}ra Yazıcı and Zeynep Tuğay and Birg{\"u}l, {Serap İpek Dingi{\c s}} and Hamdullah Yanık and Ece Tavuk{\c c}uoğlu and Sevgi G{\"u}ly{\"u}z and Atilla Akdemir and G{\"u}ne{\c s} Esendağlı and {\"O}zg{\"u}r Yılmaz and Onur Alpt{\"u}rk",

year = "2020",

doi = "10.25135/acg.oc.86.20.09.1802",

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T1 - Design and synthesis of novel peptidomimetics for cancer immunotherapy

AU - Köse, Ceyda

AU - Uysal, Esra

AU - Yazıcı, Büşra

AU - Tuğay, Zeynep

AU - Birgül, Serap İpek Dingiş

AU - Yanık, Hamdullah

AU - Tavukçuoğlu, Ece

AU - Gülyüz, Sevgi

AU - Akdemir, Atilla

AU - Esendağlı, Güneş

AU - Yılmaz, Özgür

AU - Alptürk, Onur

PY - 2020

Y1 - 2020

N2 - 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.

AB - 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.

KW - 2-aminobenzothiazole

KW - Immunotherapy

KW - PD-1

KW - PD-L1

KW - peptidomimetics

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DO - 10.25135/acg.oc.86.20.09.1802

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SN - 1307-6175

VL - 13

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EP - 102

JO - Organic Communications

JF - Organic Communications

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ER -

Design and synthesis of novel peptidomimetics for cancer immunotherapy

Abstract

Bibliographical note

Keywords

UN SDGs

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