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SAR study of small molecule inhibitors of the programmed cell death‐1/programmed cell death‐ligand 1 interaction

Chemical Biology & Drug Design, 2021
AbstractThe development of small molecule inhibitors of programmed cell death‐1/programmed cell death‐ligand 1 (PD‐1/PD‐L1) has drawn research interest for the treatment of cancer. Recently, we reported the discovery of a novel dimeric core small molecule PD‐1/PD‐L1 inhibitor.
Seiji Kawashita   +10 more
openaire   +2 more sources

Progress in programmed cell death-1/programmed cell death-ligand 1 pathway inhibitors and binding mode analysis

Molecular Diversity, 2022
Programmed cell death protein 1 (PD-1)/programmed cell death protein ligand 1 (PD-L1) plays an important role in negative regulating immunity. The search for effective PD-1/PD-L1 inhibitors has been at the cutting-edge of academic and industrial medicinal chemistry, leading to the emergence of 16 clinical candidate drugs and the launch of six ...
Xiaoyun Li   +4 more
openaire   +2 more sources

Alcohol induces programmed death receptor-1 and programmed death-ligand-1 differentially in neuroimmune cells

Alcohol, 2020
Engagement of programmed death-1 (PD-1) receptor by its ligands (PD-L1/PD-L2) in activated immune cells is known to be involved in inflammatory neurological disease via a co-inhibitory signal pathway. Interaction of PD-1/PD-L1 is believed to occur only in activated neuroimmune cells because there are undetectable levels of PD-1/PD-L1 in normal ...
Vikas Mishra   +4 more
openaire   +2 more sources

Programmed Cell Death–Ligand 1 Overexpression in Thyroid Cancer

Endocrine Practice, 2019
Programmed cell death-ligand 1 (PD-L1) expression on tumor tissue has been associated with favorable response to anti-programmed cell death-receptor 1/PD-L1 therapy in many human cancers. Studies have reported that PD-L1 is also expressed in thyroid cancer.
Guo-Qiang, Zhang   +8 more
openaire   +2 more sources

Discovery of the programmed cell death-1/programmed cell death-ligand 1 interaction inhibitors bearing an indoline scaffold

European Journal of Medicinal Chemistry, 2020
Inhibiting the programmed cell death-1 (PD-1)/programmed cell death-ligand 1 (PD-L1) pathway is an attractive strategy for tumor immunotherapy. Here, a novel series of indoline-containing compounds were developed, among which, A13 was identified as the most promising PD-1/PD-L1 pathway inhibitor.
Mingze, Qin   +13 more
openaire   +2 more sources

Expression of programmed cell death protein 1 and programmed cell death ligand 1 in feline injection site fibrosarcomas

Research in Veterinary Science
Feline injection site fibrosarcomas represent a unique challenge in veterinary oncology due to their association with injection sites and aggressive behaviour. The study explores the expression of immune checkpoints programmed cell death protein 1 and programmed cell death ligand 1 in the malignancy, aiming to unravel their potential significance in ...
Mateusz, Mikiewicz   +3 more
openaire   +2 more sources

Symmetry-based ligand design and evaluation of small molecule inhibitors of programmed cell death-1/programmed death-ligand 1 interaction

Bioorganic & Medicinal Chemistry Letters, 2019
The development of small molecule inhibitors of PD-1/PD-L1 is eagerly anticipated for treatment of cancer. We focused on the symmetry of the ternary complex structure of reported small molecule ligands and hPD-L1 homodimers, and designed partially- or fully-symmetric compounds for more potent inhibitors.
Seiji Kawashita   +10 more
openaire   +2 more sources

Expression of programmed cell death 1 and programmed cell death ligand 1 in extranodal NK/T-cell lymphoma, nasal type

Annals of Hematology, 2016
Programmed cell death-1 (PD-1) and programmed cell death-ligand 1 (PD-L1) are new therapeutic targets in cancer immunotherapy. The aim of this study was to investigate the clinicopathological characteristics of PD-1 and PD-L1 expression in extranodal natural killer/T‑cell lymphoma, nasal type (ENKTL).
Jae-Cheol, Jo   +7 more
openaire   +2 more sources

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