Small Molecule Neuropilin-1 Antagonists Combine Antiangiogenic and Antitumor Activity with Immune Modulation through Reduction of Transforming Growth Factor Beta (TGFβ) Production in Regulatory T-Cells

[Image: see text] We report the design, synthesis, and biological evaluation of some potent small-molecule neuropilin-1 (NRP1) antagonists. NRP1 is implicated in the immune response to tumors, particularly in Treg cell fragility, required for PD1 checkpoint blockade. The design of these compounds wa...

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Detalhes bibliográficos
Publicado no:J Med Chem
Main Authors: Powell, Jonathan, Mota, Filipa, Steadman, David, Soudy, Christelle, Miyauchi, Jeremy T., Crosby, Stuart, Jarvis, Ashley, Reisinger, Tifelle, Winfield, Natalie, Evans, Graham, Finniear, Aled, Yelland, Tamas, Chou, Yi-Tai, Chan, A.W. Edith, O’Leary, Andrew, Cheng, Lili, Liu, Dan, Fotinou, Constantina, Milagre, Carla, Martin, John F., Jia, Haiyan, Frankel, Paul, Djordjevic, Snezana, Tsirka, Stella E., Zachary, Ian C, Selwood, David L.
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2018
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC5957473/
https://ncbi.nlm.nih.gov/pubmed/29648813
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.8b00210
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