Structural Basis for Inhibition of Mutant EGFR with Lazertinib (YH25448)
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Abstract
Lazertinib (YH25448) is a novel third-generation tyrosine kinase inhibitor (TKI) developed as a treatment for EGFR mutant non-small cell lung cancer. To better understand the nature of lazertinib inhibition, we determined crystal structures of lazertinib in complex with both WT and mutant EGFR and compared its binding mode to that of structurally related EGFR TKIs. We observe that lazertinib binds EGFR with a distinctive pyrazole moiety enabling hydrogen bonds and van der Waals interactions facilitated through hydrophilic amine and hydrophobic phenyl groups, respectively. Biochemical assays and cell studies confirm that lazertinib effectively targets EGFR(L858R/T790M) and to a lesser extent HER2. The molecular basis for lazertinib inhibition of EGFR reported here highlights previously unexplored binding interactions leading to improved medicinal chemistry properties compared to clinically approved osimertinib (AZD9291) and offers novel strategies for structure-guided design of tyrosine kinase inhibitors.
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A positive correlation between drug exposure and dose was observed for lazertinib, and no dose-limiting toxicity.
“A positive correlation between drug exposure and dose was observed, and no dose-limiting toxicity.142–145”
From Recent advances in targeting the “undruggable” proteins: from drug discovery to clinical trials (2023) · cites this paper as [145]
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- Authors
- Heppner, D. E., Wittlinger, F., Beyett, T. S., Shaurova, T., Urul, D. A., Buckley, B., Pham, C. D., Schaeffner, I. K., Yang, B., Ogboo, B. C., May, E. W., Schaefer, E. M., Eck, M. J., Laufer, S. A., & Hershberger, P. A.
- Affiliations
- Roswell Park Comprehensive Cancer Center (US)
- University of Tübingen (DE)
- Harvard University (US)
- AssayQuant Technologies, Inc., 260 Cedar Hill St., Marlboro, Massachusetts 01752, United States
- University at Buffalo, State University of New York (US)
- Corresponding author
- Heppner, David E.
- ORCID
- Venue
- ACS Medicinal Chemistry Letters
- Publisher
- American Chemical Society (ACS)
- Published
- 2022-11-10
- Volume
- 13
- Issue
- 12
- Pages
- 1856-1863
- ISSN
- 1948-5875 (ISSN-L)
- PMC
- PMC9743421
- OpenAlex
- W4308888442
- Cited by
- 64
- References
- 29
- Citations by year
- 2026: 18 · 2025: 26 · 2024: 10 · 2023: 10
- FWCI
- 7.42
- Type
- journal article
- Language
- en
- Open access
- green
- doi.org
- Licence
- Locations
- ACS Medicinal Chemistry Letters (publishedVersion)
- ChemRxiv (acceptedVersion, cc-by)
- PubMed Central (publishedVersion)
- PubMed (publishedVersion)
- Funders
- National Center for Advancing Translational Sciences (UL1TR001412-07)
- National Cancer Institute (5F32CA247198-02, R01CA116020, R01CA201049, R35CA242461)
- Deutsche Forschungsgemeinschaft (EXC 2180-390900677)
- Roswell Park Alliance Foundation, Roswell Park Cancer Institute
- State University of New York
- Topics
- Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Lung Cancer Treatments and Mutations
- Health Sciences › Medicine › Oncology › HER2/EGFR in Cancer Research
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Kinase Regulation and GTPase Signaling
- Keywords
- lazertinib, EGFR, tyrosine kinase inhibitors, EGFR L858R/T790M, non-small cell lung cancer, drug binding mode, osimertinib, HER2, structure-based drug design, crystal structure
About these checks
Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
Statistics and arithmetic are recomputed, not judged.
Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.
What counts as a claim ›How we measure confidence ›How we check this ›
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