2016: Signaling Breakthroughs of the Year

Adler, Elizabeth M.

doi:10.1126/scisignal.aam5681

Cited by 4 publications

(1 citation statement)

References 33 publications

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“…Immunotherapy is an emerging approach for oncological treatment [1]. Especially, the immune checkpoint inhibitors (ICIs) that target the PD-1/PD-L1 pathway get a lot of attention and have shown great improvement in the treatment of several tumors [2][3][4].…”

Section: Introductionmentioning

confidence: 99%

A comparative study of the recent most potent small-molecule PD-L1 inhibitors: what can we learn?

et al. 2021

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Immune checkpoint inhibitors targeting the PD-1/PD-L1 pathway have become a "game-changer" in the cancer treatment. However, none of the small molecular inhibitors has been approved yet. To explore the advantages and disadvantages of various scaffolds, different biological evaluations were performed on the three selected small inhibitors, namely Incyte-001, Incyte-011, and BMS-1001. In the HTRF assay, BMS-1001 showed the best binding activity for PD-L1 (IC 50 = 0.9 nM) while Incyte-011 (IC 50 = 5.293 nM) was twice more potent than the Incyte-001 (IC 50 = 11 nM). Also, only Incyte-011 increased the IFN-γ production. Notably, the Incyte-001 exhibited the high-est cytotoxicity (EC 50 = 1.635 μM). Interestingly, Incyte-001 (injected intravenously 2mg/kg) also displayed good blood-brain barrier permeability and reached a high concentration in the brain tissue. Finally, molecular docking and modeling studies suggested that the compounds bind in a pocket at the interface of two PD-L1 monomers. Overall, our work shows that PD-1/PD-L1 small molecular inhibitors have different biological characteristics depending on their unique skeletons, which can be further improved to better their clinical application.

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Section: Introductionmentioning

confidence: 99%

A comparative study of the recent most potent small-molecule PD-L1 inhibitors: what can we learn?

et al. 2021

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Light Guided In-vivo Activation of Innate Immune Cells with Photocaged TLR 2/6 Agonist

Ryu

McGonnigal

Moore

et al. 2017

Sci Rep

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The complexity of the immune system creates challenges in exploring its importance and robustness. To date, there have been few techniques developed to manipulate individual components of the immune system in an in vivo environment. Here we show a light-based dendritic cell (DC) activation allowing spatial and temporal control of immune activation in vivo. Additionally, we show time dependent changes in RNA profiles of the draining lymph node, suggesting a change in cell profile following DC migration and indicating that the cells migrating have been activated towards antigen presentation.

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Light GuidedIn-vivoActivation of Innate Immune Cells with Photocaged TLR 2/6 Agonist

Ryu

McGonnigal

Moore

et al. 2017

Preprint

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2016: Signaling Breakthroughs of the Year

Abstract: Signaling research advances in neuroscience, immunology, and cellular metabolism provide insight into both basic biology and human disease.

Cited by 4 publications

References 33 publications

A comparative study of the recent most potent small-molecule PD-L1 inhibitors: what can we learn?

A comparative study of the recent most potent small-molecule PD-L1 inhibitors: what can we learn?

Light Guided In-vivo Activation of Innate Immune Cells with Photocaged TLR 2/6 Agonist

Light GuidedIn-vivoActivation of Innate Immune Cells with Photocaged TLR 2/6 Agonist

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