Discovery of Potent and Selective PI3Kγ Inhibitors

The selective inhibition of the lipid signaling enzyme PI3Kγ constitutes an opportunity to mediate immunosuppression and inflammation within the tumor microenvironment but is difficult to achieve due to the high sequence homology across the class I PI3K isoforms. Here, we describe the design of a no...

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Veröffentlicht in:	Journal of medicinal chemistry 2020-10, Vol.63 (19), p.11235-11257
Hauptverfasser:	Drew, Samuel L, Thomas-Tran, Rhiannon, Beatty, Joel W, Fournier, Jeremy, Lawson, Kenneth V, Miles, Dillon H, Mata, Guillaume, Sharif, Ehesan U, Yan, Xuelei, Mailyan, Artur K, Ginn, Elaine, Chen, Jie, Wong, Kent, Soni, Divyank, Dhanota, Puja, Chen, Pei-Yu, Shaqfeh, Stefan G, Meleza, Cesar, Pham, Amber T, Chen, Ada, Zhao, Xiaoning, Banuelos, Jesus, Jin, Lixia, Schindler, Ulrike, Walters, Matthew J, Young, Stephen W, Walker, Nigel P, Leleti, Manmohan Reddy, Powers, Jay P, Jeffrey, Jenna L
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Class Ib Phosphatidylinositol 3-Kinase - drug effects Crystallography, X-Ray Drug Design Humans Molecular Docking Simulation Phosphoinositide-3 Kinase Inhibitors - chemistry Phosphoinositide-3 Kinase Inhibitors - pharmacokinetics Phosphoinositide-3 Kinase Inhibitors - pharmacology Rats Structure-Activity Relationship
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