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Editorial
. 2016 Sep;26(9):973-7.
doi: 10.1080/13543776.2016.1206527. Epub 2016 Jul 6.

Inhibitors of programmed cell death 1 (PD-1): a patent review (2010-2015)

Affiliations
Editorial

Inhibitors of programmed cell death 1 (PD-1): a patent review (2010-2015)

Tryfon Zarganes-Tzitzikas et al. Expert Opin Ther Pat. 2016 Sep.
No abstract available

Keywords: PD-1; PD-L1; Programmed death-1; T-cell exhaustion; immune checkpoint; immune-oncology.

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Figures

Fig. 1
Fig. 1
Small-molecule antagonists of the PD-1 pathway.
Fig. 2
Fig. 2
PD-1/PD-L1 inhibitors synthesized by BMS.
Fig. 3
Fig. 3
False positive PD-1/PD-L1 inhibitors
Fig. 4
Fig. 4
Peptidomimetic inhibitors of the PD-1/PD-L1 interaction with oxa- and thiadiazole core moieties
Fig. 5
Fig. 5
a) Hydrolysis-resistant D-peptide antagonist to target the PD-1/PD-L1 b) Macrocyclic peptidic inhibitor c) Peptide antagonist of PD-L1 (10) along with its sequence similarities to PD-1

References

    1. Dömling A, Holak TA. Programmed Death-1: Therapeutic Success after More than 100 Years of Cancer Immunotherapy. Angewandte Chemie International Edition. 2014;53:2286–88. - PMC - PubMed
    1. Keir ME, Butte MJ, Freeman GJ, Sharpe AH. PD-1 and its ligands in tolerance and immunity. Annu Rev Immunol. 2008;26:677–04. - PMC - PubMed
    1. Day CL, Kaufmann DE, Kiepiela P, et al. PD-1 expression on HIV-specific T cells is associated with T-cell exhaustion and disease progression. Nature. 2006;443:350–54. An excellent paper about PD-1 expression on human immunodeficiency virus (HIV)-specific CD8 T-cells. - PubMed
    1. Carvahlo S, Levi-Schaffer F, Sela M, Yarden Y. Immunotherapy of cancer: from monoclonal to oligoclonal cocktails of anti-cancer antibodies: IUPHAR Review X. Br J Pharmacol. 2016;173:1407–24. - PMC - PubMed
    1. Wolchok JD. PD-1 Blockers. Cell. 2015;162:937. - PubMed

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