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BMS-202, a PD-1/PD-L1 inhibitor, decelerates the pro-fibrotic effects of fibroblasts derived from scar tissues via ERK and TGFbeta1/Smad signaling pathways.
Cai Y, Xiao M, Li X, Zhou S, Sun Y, Yu W, Zhao T. Cai Y, et al. Immun Inflamm Dis. 2022 Oct;10(10):e693. doi: 10.1002/iid3.693. Immun Inflamm Dis. 2022. PMID: 36169254 Free PMC article.
The effect of BMS-202 on alpha-SMA and collagen I expression, and transforming growth factor beta 1 (TGFbeta1)/Smad signaling in HFBs was also determined by WB and enzyme-linked immunosorbent assay. ...Finally, BMS-202 could reduce the phosphorylation …
The effect of BMS-202 on alpha-SMA and collagen I expression, and transforming growth factor beta 1 (TGFbeta1)/Smad signaling …
Structural Biology of the Immune Checkpoint Receptor PD-1 and Its Ligands PD-L1/PD-L2.
Zak KM, Grudnik P, Magiera K, Dömling A, Dubin G, Holak TA. Zak KM, et al. Structure. 2017 Aug 1;25(8):1163-1174. doi: 10.1016/j.str.2017.06.011. Structure. 2017. PMID: 28768162 Free article. Review.
Structural basis for blocking the PD-1/PD-L1 interaction by small molecules is illustrated with the compound BMS-202 that binds to and induces dimerization of PD-L1....
Structural basis for blocking the PD-1/PD-L1 interaction by small molecules is illustrated with the compound BMS-202 that bind …
The PD-1/PD-L1 binding inhibitor BMS-202 suppresses the synthesis and secretion of gonadotropins and enhances apoptosis via p38 MAPK signaling pathway.
Jiang Y, Zhang J, Qiu J, Cui S. Jiang Y, et al. Drug Dev Res. 2022 Feb;83(1):176-183. doi: 10.1002/ddr.21857. Epub 2021 Jul 26. Drug Dev Res. 2022. PMID: 34309063
To determine whether BMS-202 can disrupt the pituitary gland and reproductive system. BMS-202 (2.5 mg/kg) was injected intraperitoneally into adult female mice every 96 h for four times. ...
To determine whether BMS-202 can disrupt the pituitary gland and reproductive system. BMS-202 (2.5 mg/kg) was in …
N-glycosylation and ubiquitinylation of PD-L1 do not restrict interaction with BMS-202: A molecular modeling study.
Bailly C, Vergoten G. Bailly C, et al. Comput Biol Chem. 2020 Oct;88:107362. doi: 10.1016/j.compbiolchem.2020.107362. Epub 2020 Aug 19. Comput Biol Chem. 2020. PMID: 32871472
Here we have investigated the effect of N-glycosylation (at N35, N192, N200 and N219) and mono-ubiquitination (at K178) of PD-L1 on the interaction with BMS-202 by molecular modeling. Two complementary tridimensional models of PD-L1, based on available crystallograp …
Here we have investigated the effect of N-glycosylation (at N35, N192, N200 and N219) and mono-ubiquitination (at K178) of PD-L1 on the inte …
Antitumor activity of the PD-1/PD-L1 binding inhibitor BMS-202 in the humanized MHC-double knockout NOG mouse.
Ashizawa T, Iizuka A, Tanaka E, Kondou R, Miyata H, Maeda C, Sugino T, Yamaguchi K, Ando T, Ishikawa Y, Ito M, Akiyama Y. Ashizawa T, et al. Biomed Res. 2019;40(6):243-250. doi: 10.2220/biomedres.40.243. Biomed Res. 2019. PMID: 31839668 Free article.
BMS-202 inhibited the proliferation of strongly PD-L1-positive SCC-3 cells (IC(50) 15 muM) and anti-CD3 antibody-activated Jurkat cells (IC(50) 10 muM) in vitro. Additionally, BMS-202 had no regulatory effect on the PD-1 or PD-L1 expression level on th …
BMS-202 inhibited the proliferation of strongly PD-L1-positive SCC-3 cells (IC(50) 15 muM) and anti-CD3 antibody-activated Jur …
Metabolic remodeling by the PD-L1 inhibitor BMS-202 significantly inhibits cell malignancy in human glioblastoma.
Yang X, Wang W, Ji T. Yang X, et al. Cell Death Dis. 2024 Mar 4;15(3):186. doi: 10.1038/s41419-024-06553-5. Cell Death Dis. 2024. PMID: 38438374 Free PMC article.
Recently, crystallographic studies have demonstrated that BMS-202, a small-molecule compound characterized by a methoxy-1-pyridine chemical structure, exhibits a high affinity to PD-L1 dimerization. ...Our findings indicate that BMS-202 apparently inhi …
Recently, crystallographic studies have demonstrated that BMS-202, a small-molecule compound characterized by a methoxy-1-pyri …
Paclitaxel derivative-based liposomal nanoplatform for potentiated chemo-immunotherapy.
Wang Y, Yu J, Li D, Zhao L, Sun B, Wang J, Wang Z, Zhou S, Wang M, Yang Y, Liu H, Zhang H, Lv Q, Jiang Q, He Z, Wang Y. Wang Y, et al. J Control Release. 2022 Jan;341:812-827. doi: 10.1016/j.jconrel.2021.12.023. Epub 2021 Dec 23. J Control Release. 2022. PMID: 34953979
The innovative liposomal nanosystem was rationally designed by a remote loading of BMS-202 (a small molecule PD-1/PD-L1 inhibitor) and PSN into the liposomes for a ROS-sensitive paclitaxel release and sustained BMS-202 release. ...The antitumor immunit …
The innovative liposomal nanosystem was rationally designed by a remote loading of BMS-202 (a small molecule PD-1/PD-L1 inhibi …
Flurbiprofen as a biphenyl scaffold for the design of small molecules binding to PD-L1 protein dimer.
Bailly C, Vergoten G. Bailly C, et al. Biochem Pharmacol. 2020 Aug;178:114042. doi: 10.1016/j.bcp.2020.114042. Epub 2020 May 21. Biochem Pharmacol. 2020. PMID: 32445869 Review.
Small molecules targeting the PD-1/PD-L1 immune checkpoint are actively searched to offer anticancer oral treatment modalities. Different small molecules have been designed, such as BMS-202 and BMS-1166 which potently bind to PD-L1, sequestering the protein dimer an …
Small molecules targeting the PD-1/PD-L1 immune checkpoint are actively searched to offer anticancer oral treatment modalities. Different sm …
Targeting HER2-positive breast cancer cells by a combination of dasatinib and BMS-202: Insight into the molecular pathways.
Kheraldine H, Gupta I, Cyprian FS, Vranic S, Al-Farsi HF, Merhi M, Dermime S, Al Moustafa AE. Kheraldine H, et al. Cancer Cell Int. 2024 Mar 2;24(1):94. doi: 10.1186/s12935-023-03195-z. Cancer Cell Int. 2024. PMID: 38431613 Free PMC article.
METHODS: Herein, we investigated the impact of DA and PD-L1 inhibitor (BMS-202) combination on HER2-positive breast cancer cell lines, SKBR3 and ZR75. ...CONCLUSION: Our findings implicate that a combination of DA and BMS-202 could have a significant i …
METHODS: Herein, we investigated the impact of DA and PD-L1 inhibitor (BMS-202) combination on HER2-positive breast cancer cel …
Dual-Pronged Attack: pH-Driven Membrane-Anchored NIR Dual-Type Nano-Photosensitizer Excites Immunogenic Pyroptosis and Sequester Immune Checkpoint for Enhanced Prostate Cancer Photo-Immunotherapy.
Wang H, He Z, Gao Y, Feng D, Wei X, Huang Y, Hou J, Li S, Zhang W. Wang H, et al. Adv Sci (Weinh). 2023 Oct;10(28):e2302422. doi: 10.1002/advs.202302422. Epub 2023 Aug 6. Adv Sci (Weinh). 2023. PMID: 37544896 Free PMC article.
The pH-responsive polymer equipped with the cell membrane anchoring peptide RKC is used as the carrier and further encapsulated with the near-infrared-activated semiconductor polymer photosensitizer YBS and a PD-1/PD-L1 complex small molecule inhibitor BMS-202. The …
The pH-responsive polymer equipped with the cell membrane anchoring peptide RKC is used as the carrier and further encapsulated with the nea …
39 results