Allosteric Inhibitor TREA-0236 Containing Non-hydrolysable Quinazoline-4-one for EGFR T790M/C797S Mutants Inhibition
Seoyoung Lee
Bio & Drug Discovery Division, Korea Research Institute of Chemical Technology, Daejeon 34114, South Korea
Medicinal Chemistry & Pharmacology, Korea University of Science & Technology, Daejeon 34113, South Korea
Search for more papers by this authorJiwon Kim
Bio & Drug Discovery Division, Korea Research Institute of Chemical Technology, Daejeon 34114, South Korea
Medicinal Chemistry & Pharmacology, Korea University of Science & Technology, Daejeon 34113, South Korea
Search for more papers by this authorKrishna Babu Duggirala
Bio & Drug Discovery Division, Korea Research Institute of Chemical Technology, Daejeon 34114, South Korea
Medicinal Chemistry & Pharmacology, Korea University of Science & Technology, Daejeon 34113, South Korea
Search for more papers by this authorAreum Go
Bio & Drug Discovery Division, Korea Research Institute of Chemical Technology, Daejeon 34114, South Korea
Medicinal Chemistry & Pharmacology, Korea University of Science & Technology, Daejeon 34113, South Korea
Search for more papers by this authorInji Shin
Bio & Drug Discovery Division, Korea Research Institute of Chemical Technology, Daejeon 34114, South Korea
Medicinal Chemistry & Pharmacology, Korea University of Science & Technology, Daejeon 34113, South Korea
Search for more papers by this authorByoung Chul Cho
Yonsei Cancer Center, Yonsei University College of Medicine, Seoul 03722, South Korea
Search for more papers by this authorGildon Choi
Bio & Drug Discovery Division, Korea Research Institute of Chemical Technology, Daejeon 34114, South Korea
Medicinal Chemistry & Pharmacology, Korea University of Science & Technology, Daejeon 34113, South Korea
Search for more papers by this authorChong Hak Chae
Bio & Drug Discovery Division, Korea Research Institute of Chemical Technology, Daejeon 34114, South Korea
Search for more papers by this authorCorresponding Author
Kwangho Lee
Bio & Drug Discovery Division, Korea Research Institute of Chemical Technology, Daejeon 34114, South Korea
Medicinal Chemistry & Pharmacology, Korea University of Science & Technology, Daejeon 34113, South Korea
Search for more papers by this authorSeoyoung Lee
Bio & Drug Discovery Division, Korea Research Institute of Chemical Technology, Daejeon 34114, South Korea
Medicinal Chemistry & Pharmacology, Korea University of Science & Technology, Daejeon 34113, South Korea
Search for more papers by this authorJiwon Kim
Bio & Drug Discovery Division, Korea Research Institute of Chemical Technology, Daejeon 34114, South Korea
Medicinal Chemistry & Pharmacology, Korea University of Science & Technology, Daejeon 34113, South Korea
Search for more papers by this authorKrishna Babu Duggirala
Bio & Drug Discovery Division, Korea Research Institute of Chemical Technology, Daejeon 34114, South Korea
Medicinal Chemistry & Pharmacology, Korea University of Science & Technology, Daejeon 34113, South Korea
Search for more papers by this authorAreum Go
Bio & Drug Discovery Division, Korea Research Institute of Chemical Technology, Daejeon 34114, South Korea
Medicinal Chemistry & Pharmacology, Korea University of Science & Technology, Daejeon 34113, South Korea
Search for more papers by this authorInji Shin
Bio & Drug Discovery Division, Korea Research Institute of Chemical Technology, Daejeon 34114, South Korea
Medicinal Chemistry & Pharmacology, Korea University of Science & Technology, Daejeon 34113, South Korea
Search for more papers by this authorByoung Chul Cho
Yonsei Cancer Center, Yonsei University College of Medicine, Seoul 03722, South Korea
Search for more papers by this authorGildon Choi
Bio & Drug Discovery Division, Korea Research Institute of Chemical Technology, Daejeon 34114, South Korea
Medicinal Chemistry & Pharmacology, Korea University of Science & Technology, Daejeon 34113, South Korea
Search for more papers by this authorChong Hak Chae
Bio & Drug Discovery Division, Korea Research Institute of Chemical Technology, Daejeon 34114, South Korea
Search for more papers by this authorCorresponding Author
Kwangho Lee
Bio & Drug Discovery Division, Korea Research Institute of Chemical Technology, Daejeon 34114, South Korea
Medicinal Chemistry & Pharmacology, Korea University of Science & Technology, Daejeon 34113, South Korea
Search for more papers by this authorGraphical Abstract
Supporting Information
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- 19EGFR kinase assay was performed using the europium labeled antibody that specifically recognizes phosphotyrosine as donor dye and streptavidin protein labeled with a small molecular weight fluorophore acceptor dye XL665 provided by Cisbio, Inc. Recombinant EGFR L858R/T790M/C797S mutant was purchased from SignalChem, Inc. All reaction components except ATP were added to the wells first and the reaction was started by adding ATP to the assay mixture containing the enzyme and peptide substrate. After 1 h incubation, the FRET signal between europium cryptate and XL665 was measured to quantify the phosphorylation of the substrate peptide. Envision multilabel reader (Perkin Elmer) was used to measure the fluorescence of the samples at 620 nm (europium-labeled antibody) and 665 nm (XL665 labeled streptavidin) after excitation at 320 nm.
