1 Berndt JD, Gough NR. 2013: Signaling Breakthroughs of the Year. Sci Signal. 2014, 7 (307). http://doi: 10.1126/scisignal.aam5681.
2 Messenheimer DJ, Jensen SM, Afentoulis ME, Wegmann KW, Feng, ZP, Friedman DJ, Gough MJ, Urba WJ, Fox BA. Timing of PD-1 Blockade Is Critical to Effective Combination Immunotherapy with Anti-OX40. Clin Cancer Res. 2017, 23 (20), 6165-6177. http://doi: 10.1158/1078-0432.Ccr-16-2677.
3 Iwai Y, Hamanishi J, Chamoto K, Honjo T. Cancer immunotherapies targeting the PD-1 signaling pathway. J Biomed Sci. 2017, 24. http://doi: 10.1186/s12929-017-0329-9.
4 Salmaninejad A, Valilou SF, Shabgah AG, Aslani S, Alimardani M, Pasdar A, Sahebkar A. PD-1/PD-L1 pathway: Basic biology and role in cancer immunotherapy. J Cell Physiol. 2019, 234 (10), 16824-16837. http://doi: 10.1002/jcp.28358.
5 Freeman GJ, Long AJ, Iwai Y, Bourque K, Chernova T, Nishimura H, Fitz LJ, Malenkovich N, Okazaki T, Byrne MC, Horton HF, Fouser L, Carter L, Ling V, Bowman MR, Carreno BM, Collins M, Wood CR, Honjo T. En-gagement of the PD-1 immunoinhibitory receptor by a novel B7 family member leads to negative regulation of lymphocyte activation. J Exp Med. 2000, 192 (7), 1027-1034. http://doi: 10.1084/jem.192.7.1027.
6 Agata Y, Kawasaki A, Nishimura H, Ishida Y, Tsubata T, Yagita H, Honjo T. Expression of the PD-1 antigen on the surface of stimulated mouse T and B lymphocytes. Int Immunol. 1996, 8 (5), 765-772.
http://doi: 10.1093/intimm/8.5.765.
7 Dong HD, Strome SE, Salomao DR, Tamura H, Hirano F, Flies DB, Roche PC, Lu J, Zhu GF, Tamada K, Lennon VA, Celis E, Chen LP. Tumor-associated B7-H1 promotes T-cell apoptosis: A potential mechanism of immune evasion. Nat Med. 2002, 8 (8), 793-800. http://doi: 10.1038/nm730.
8 Flies DB, Sandler BJ, Sznol M, Chen L. Blockade of the B7-H1/PD-1 pathway for cancer immunotherapy. Yale J Biol Med. 2011;84(4):409-21.
9 Hematology/Oncology (Cancer) Approvals & Safety Notifications. Available from: https://www.fda.gov/drugs/resources-information-approved-drugs/hematologyoncology-cancer-approvals-safety-notifications.
10 Yan Y, Zhang L, Zuo Y, Qian H, Liu C. Immune Checkpoint Blockade in Cancer Immunotherapy: Mechanisms, Clinical Outcomes, and Safety Profiles of PD-1/PD-L1 Inhibitors. Arch Immunol Ther Exp. (Warsz). 2020;68(6):36. http://doi: 10.1007/s00005-020-00601-6
11 Hoos A. Development of immuno-oncology drugs - from CTLA4 to PD1 to the next generations. Nat Rev Drug Discov. 2016;15(4):235-47.
http://doi: 10.1038/nrd.2015.35
12 Lin X, Lu X, Luo G, Xiang H. Progress in PD-1/PD-L1 pathway inhibitors: From biomacromolecules to small molecules. Eur J Med Chem. 2020;186:111876. http://doi: 10.1016/j.ejmech.2019.111876
13 Postow MA. Managing immune checkpoint-blocking antibody side effects. Am Soc Clin Oncol Educ Book. 2015:76-83.
http://doi: 10.14694/EdBook_AM.2015.35.76
14 Tan SG, Zhang CWH, Gao GF. Seeing is believing: anti-PD-1/PD-L1 monoclonal antibodies in action for checkpoint blockade tumor immunotherapy. Signal Transduct Tar. 2016, 1. http://doi: 10.1038/sigtrans.2016.29.
15 Zhao JF, Chen AX, Gartrell RD, Silverman AM, Aparicio L, Chu T, Bordbar D, Shan D, Samanamud J, Mahajan A, Filip I, Orenbuch R, Goetz M, Yamaguchi JT, Cloney M, Horbinski C, Lukas RV, Raizer J, Rae AI, Yuan JZ, Canoll P, Bruce JN, Saenger YM, Sims P, Iwamoto FM, Sonabend AM, Rabadan R. Immune and genomic correlates of re-sponse to anti-PD-1 immunotherapy in glioblastoma (vol 25, pg 462, 2019). Nat Med. 2019, 25 (6), 1022-1022. http://doi: 10.1038/s41591-019-0449-8.
16 Guzik K, Tomala M, Muszak D, Konieczny M, Hec A, Blaszkiewicz U, Pustula M, Butera R, Domling A, Holak TA. Development of the Inhibitors that Target the PD-1/PD-L1 Interaction-A Brief Look at Progress on Small Molecules, Peptides and Macrocycles. Molecules. 2019, 24 (11).
http://doi: 10.3390/molecules24112071.
17 Wang T, Wu X, Guo C, Zhang K, Xu J, Li Z. et al. Development of Inhibitors of the Programmed Cell Death-1/Programmed Cell Death-Ligand 1 Signaling Pathway. J Med Chem. 2019;62(4):1715-30.
http://doi: 10.1021/acs.jmedchem.8b00990
18 Chen T, Li Q, Liu Z, Chen Y, Feng F, Sun H. Peptide-based and small synthetic molecule inhibitors on PD-1/PD-L1 pathway: A new choice for immunotherapy? Eur J Med Chem. 2019;161:378-98. http://doi: 10.1016/j.ejmech.2018.10.044
19 Wu Q, Jiang L, Li SC, He QJ, Yang B, Cao J. Small molecule inhibitors targeting the PD-1/PD-L1 signaling pathway. Acta Pharmacol Sin. 2021;42(1):1-9. http://doi: 10.1038/s41401-020-0366-x
20 Basu S, Yang J, Xu B, Magiera-Mularz K, Skalniak L, Musielak B, Kholodovych V, Holak TA, Hu L. Design, Synthesis, Evaluation, and Structural Studies of C2-Symmetric Small Molecule Inhibitors of Programmed Cell Death-1/Programmed Death-Ligand 1 Protein-Protein Interaction. J Med Chem. 2019, 62 (15), 7250-7263. http://doi: 10.1021/acs.jmedchem.9b00795.
21 Wu L, Yu Z, Zhang F, Yao W. N-PHENYL-PYRIDINE-2-CARBOXAMIDE DERIVATIVES AND THEIR USE AS PD-1/PD-L1 PROTEIN/PROTEIN INTERACTION MODULATORS. WO2017106634A1. 2017.
22 Wu L, Yu Z, Zhang F, Yao W. PYRIDINE DERIVATIVES AS IMMUNOMODULATORS. WO2018119221A1. 2018.
23 Chupak LS, Ding M, Martin SW, Zheng X, Hewawasam P, Connolly TP, Xu N, Yeung KS, Zhu J, Langley DR, TENNEY DJ, Scola PM. COMPOUNDS USEFUL AS IMMUNOMODULATORS. WO2015160641A2. 2015, October 22.
24 Qian JW, Wang C, Wang B, Yang J, Wang YD, Luo FF, Xu JY, Zhao CJ, Liu RH, Chu YW. The IFN-gamma/PD-L1 axis between T cells and tumor microenvironment: hints for glioma anti-PD-1/PD-L1 therapy. J Neuroinflamm. 2018, 15. http://doi: 10.1186/s12974-018-1330-2.
25 Zak KM, Grudnik P, Guzik K, Zieba BJ, Musielak B, Dömling A, Dubin G, Holak TA. Structural basis for small molecule targeting of the programmed death ligand 1 (PD-L1). Oncotarget. 2016, May 24;7(21):30323-35. http://doi: 10.18632/oncotarget.8730.
26 Villaseor R, Lampe J, Schwaninger M, Collin L. Intracellular transport and regulation of transcytosis across the blood–brain barrier. Cell Mol Life Sci. 2019, 76(6).