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Drugging the catalytically inactive state of RET kinase in RET-rearranged tumors.
Plenker D, Riedel M, Brägelmann J, Dammert MA, Chauhan R, Knowles PP, Lorenz C, Keul M, Bührmann M, Pagel O, Tischler V, Scheel AH, Schütte D, Song Y, Stark J, Mrugalla F, Alber Y, Richters A, Engel J, Leenders F, Heuckmann JM, Wolf J, Diebold J, Pall G, Peifer M, Aerts M, Gevaert K, Zahedi RP, Buettner R, Shokat KM, McDonald NQ, Kast SM, Gautschi O, Thomas RK, Sos ML. Plenker D, et al. Among authors: engel j. Sci Transl Med. 2017 Jun 14;9(394):eaah6144. doi: 10.1126/scitranslmed.aah6144. Sci Transl Med. 2017. PMID: 28615362 Free PMC article.
Identification of type II and III DDR2 inhibitors.
Richters A, Nguyen HD, Phan T, Simard JR, Grütter C, Engel J, Rauh D. Richters A, et al. Among authors: engel j. J Med Chem. 2014 May 22;57(10):4252-62. doi: 10.1021/jm500167q. Epub 2014 May 5. J Med Chem. 2014. PMID: 24754677
Identification and further development of potent TBK1 inhibitors.
Richters A, Basu D, Engel J, Ercanoglu MS, Balke-Want H, Tesch R, Thomas RK, Rauh D. Richters A, et al. Among authors: engel j. ACS Chem Biol. 2015 Jan 16;10(1):289-98. doi: 10.1021/cb500908d. ACS Chem Biol. 2015. PMID: 25540906
Targeting Drug Resistance in EGFR with Covalent Inhibitors: A Structure-Based Design Approach.
Engel J, Richters A, Getlik M, Tomassi S, Keul M, Termathe M, Lategahn J, Becker C, Mayer-Wrangowski S, Grütter C, Uhlenbrock N, Krüll J, Schaumann N, Eppmann S, Kibies P, Hoffgaard F, Heil J, Menninger S, Ortiz-Cuaran S, Heuckmann JM, Tinnefeld V, Zahedi RP, Sos ML, Schultz-Fademrecht C, Thomas RK, Kast SM, Rauh D. Engel J, et al. J Med Chem. 2015 Sep 10;58(17):6844-63. doi: 10.1021/acs.jmedchem.5b01082. Epub 2015 Aug 31. J Med Chem. 2015. PMID: 26275028
Phenotypic Identification of a Novel Autophagy Inhibitor Chemotype Targeting Lipid Kinase VPS34.
Robke L, Laraia L, Carnero Corrales MA, Konstantinidis G, Muroi M, Richters A, Winzker M, Engbring T, Tomassi S, Watanabe N, Osada H, Rauh D, Waldmann H, Wu YW, Engel J. Robke L, et al. Among authors: engel j. Angew Chem Int Ed Engl. 2017 Jul 3;56(28):8153-8157. doi: 10.1002/anie.201703738. Epub 2017 Jun 12. Angew Chem Int Ed Engl. 2017. PMID: 28544137
Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor.
Engel J, Smith S, Lategahn J, Tumbrink HL, Goebel L, Becker C, Hennes E, Keul M, Unger A, Müller H, Baumann M, Schultz-Fademrecht C, Günther G, Hengstler JG, Rauh D. Engel J, et al. J Med Chem. 2017 Sep 28;60(18):7725-7744. doi: 10.1021/acs.jmedchem.7b00515. Epub 2017 Sep 18. J Med Chem. 2017. PMID: 28853575
Characterization of Covalent-Reversible EGFR Inhibitors.
Smith S, Keul M, Engel J, Basu D, Eppmann S, Rauh D. Smith S, et al. Among authors: engel j. ACS Omega. 2017 Apr 30;2(4):1563-1575. doi: 10.1021/acsomega.7b00157. Epub 2017 Apr 20. ACS Omega. 2017. PMID: 29963651 Free PMC article.
2,692 results