Next-generation EGFR tyrosine kinase inhibitors to overcome C797S mutation in non-small cell lung cancer (2019-2024).
Das D, Xie L, Hong J.
RSC Med Chem · review-article; review; journal article · DOI 10.1039/d4md00384e PUBLICATION REGISTRY
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8 hitsFourth-generation epidermal growth factor receptor-tyrosine kinases inhibitors: hope and challenges.
Su C, Sun SY.
Transl Cancer Res · comment; editorial · DOI 10.21037/tcr-24-406Potential Utility of a 4th-Generation EGFR-TKI and Exploration of Resistance Mechanisms-An In Vitro Study.
Fukuda S, Suda K, Hamada A, Oiki H, Ohara S, Ito M, Soh J, Mitsudomi T, Tsutani Y.
Biomedicines · research-article; journal article · DOI 10.3390/biomedicines12071412Structural Analysis of the Macrocyclic Inhibitor BI-4020 Binding to EGFR Kinase.
Beyett TS, Rana JK, Schaeffner IK, Heppner DE, Eck MJ.
ChemMedChem · research-article; journal article; research support, n.i.h., extramural · DOI 10.1002/cmdc.202300343A macrocyclic kinase inhibitor overcomes triple resistant mutations in EGFR-positive lung cancer.
Suzuki M, Uchibori K, Oh-Hara T, Nomura Y, Suzuki R, Takemoto A, Araki M, Matsumoto S, Sagae Y, Kukimoto-Niino M, Kawase Y, Shirouzu M, Okuno Y, Nishio M, Fujita N, Katayama R.
NPJ Precis Oncol · research-article; journal article · DOI 10.1038/s41698-024-00542-9Rigid Scaffolds Are Promising for Designing Macrocyclic Kinase Inhibitors.
Zhao Z, Bourne PE.
ACS Pharmacol Transl Sci · research-article; journal article · DOI 10.1021/acsptsci.3c00078Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19.
Amrhein JA, Beyett TS, Feng WW, Krämer A, Weckesser J, Schaeffner IK, Rana JK, Jänne PA, Eck MJ, Knapp S, Hanke T.
J Med Chem · research support, non-u.s. gov't; research-article; research support, u.s. gov't, non-p.h.s.; journal article; research support, n.i.h., extramural · DOI 10.1021/acs.jmedchem.2c01041Start Selective and Rigidify: The Discovery Path toward a Next Generation of EGFR Tyrosine Kinase Inhibitors.
Engelhardt H, Böse D, Petronczki M, Scharn D, Bader G, Baum A, Bergner A, Chong E, Döbel S, Egger G, Engelhardt C, Ettmayer P, Fuchs JE, Gerstberger T, Gonnella N, Grimm A, Grondal E, Haddad N, Hopfgartner B, Kousek R, Krawiec M, Kriz M, Lamarre L, Leung J, Mayer M, Patel ND, Simov BP, Reeves JT, Schnitzer R, Schrenk A, Sharps B, Solca F, Stadtmüller H, Tan Z, Wunberg T, Zoephel A, McConnell DB.
J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.9b01169