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TitleDiscovery of RGT-018: A Potent, Selective, and Orally Bioavailable SOS1 Inhibitor for KRAS-Driven Cancers.
Journal, issue, pagesMol. Cancer Ther., Vol. 23, Page 1703-1716, Year 2024
Publish dateDec 21, 2023 (structure data deposition date)
AuthorsXiao, F. / Wang, K. / Wang, X. / Li, H. / Hu, Z. / Ren, X. / Huang, W. / Feng, T. / Yao, L. / Lin, J. ...Xiao, F. / Wang, K. / Wang, X. / Li, H. / Hu, Z. / Ren, X. / Huang, W. / Feng, T. / Yao, L. / Lin, J. / Li, C. / Zhang, Z. / Mei, L. / Zhu, X. / Zhong, W. / Xie, Z.
External linksMol. Cancer Ther. / PubMed:39087485
MethodsX-ray diffraction
Resolution2.1 Å
Structure data

PDB-8xjj:
Co-crystal structure of SOS-1 and a potent, selective and orally bioavailable SOS1 inhibitor RGT-018
Method: X-RAY DIFFRACTION / Resolution: 2.1 Å

Chemicals

PDB-1lvj:
STRUCTURE OF TAR RNA COMPLEXED WITH A TAT-TAR INTERACTION NANOMOLAR INHIBITOR THAT WAS IDENTIFIED BY COMPUTATIONAL SCREENING

ChemComp-EDO:
1,2-ETHANEDIOL

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsSIGNALING PROTEIN / SOS1 / selective inhibitor / KRAS-driven cancers

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