Disease-related mutations in PI3Kγ disrupt regulatory C-terminal dynamics and reveal a path to selective inhibitors.
Elife
Rathinaswamy, Manoj K MK; Gaieb, Zied Z; Fleming, Kaelin D KD; Borsari, Chiara C; Harris, Noah J NJ; Moeller, Brandon E BE; Wymann, Matthias P MP; Amaro, Rommie E RE; Burke, John E JE
Disease-related mutations in PI3Kγ disrupt regulatory C-terminal dynamics and reveal a path to selective inhibitors.
Elife
Rathinaswamy, Manoj K MK; Gaieb, Zied Z; Fleming, Kaelin D KD; Borsari, Chiara C; Harris, Noah J NJ; Moeller, Brandon E BE; Wymann, Matthias P MP; Amaro, Rommie E RE; Burke, John E JE
Design of Selective Benzoxazepin PI3Kδ Inhibitors Through Control of Dihedral Angles.
Acs Medicinal Chemistry Letters
Safina, Brian S BS; Elliott, Richard L RL; Forrest, Andrew K AK; Heald, Robert A RA; Murray, Jeremy M JM; Nonomiya, Jim J; Pang, Jodie J; Salphati, Laurent L; Seward, Eileen M EM; Staben, Steven T ST; Ultsch, Mark M; Wei, Binqing B; Yang, Wenqian W; Sutherlin, Daniel P DP
A KRAS GTPase K104Q Mutant Retains Downstream Signaling by Offsetting Defects in Regulation.
The Journal Of Biological Chemistry
Yin, Guowei G; Kistler, Samantha S; George, Samuel D SD; Kuhlmann, Nora N; Garvey, Leslie L; Huynh, Minh M; Bagni, Rachel K RK; Lammers, Michael M; Der, Channing J CJ; Campbell, Sharon L SL