小分子BI-2852诱导形成无功能的KRAS二聚体。 - Suppr

The small molecule BI-2852 induces a nonfunctional dimer of KRAS.

作者信息

Tran Timothy H, Alexander Patrick, Dharmaiah Srisathiyanarayanan, Agamasu Constance, Nissley Dwight V, McCormick Frank, Esposito Dominic, Simanshu Dhirendra K, Stephen Andrew G, Balius Trent E

机构信息

National Cancer Institute RAS Initiative, Cancer Research Technology Program, Frederick National Laboratory for Cancer Research, Leidos Biomedical Research, Inc., Frederick, MD 21702.

Helen Diller Comprehensive Cancer Center, University of California, San Francisco, CA 94158.

出版信息

Proc Natl Acad Sci U S A. 2020 Feb 18;117(7):3363-3364. doi: 10.1073/pnas.1918164117. Epub 2020 Feb 11.

DOI:10.1073/pnas.1918164117

PMID:32047043

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7035607/

Abstract

摘要

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/25e0/7035607/fcfb7897f98a/pnas.1918164117fig01.jpg

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本文引用的文献

Drugging an undruggable pocket on KRAS.

Proc Natl Acad Sci U S A. 2019 Aug 6;116(32):15823-15829. doi: 10.1073/pnas.1904529116. Epub 2019 Jul 22.

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The small molecule BI-2852 induces a nonfunctional dimer of KRAS.

作者信息

Tran Timothy H, Alexander Patrick, Dharmaiah Srisathiyanarayanan, Agamasu Constance, Nissley Dwight V, McCormick Frank, Esposito Dominic, Simanshu Dhirendra K, Stephen Andrew G, Balius Trent E

机构信息

National Cancer Institute RAS Initiative, Cancer Research Technology Program, Frederick National Laboratory for Cancer Research, Leidos Biomedical Research, Inc., Frederick, MD 21702.

Helen Diller Comprehensive Cancer Center, University of California, San Francisco, CA 94158.

出版信息

Proc Natl Acad Sci U S A. 2020 Feb 18;117(7):3363-3364. doi: 10.1073/pnas.1918164117. Epub 2020 Feb 11.

DOI:10.1073/pnas.1918164117

PMID:32047043

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7035607/

Abstract

摘要

相似文献

The small molecule BI-2852 induces a nonfunctional dimer of KRAS.

Proc Natl Acad Sci U S A. 2020 Feb 18;117(7):3363-3364. doi: 10.1073/pnas.1918164117. Epub 2020 Feb 11.

Researchers Reveal Another KRAS Inhibitor.

Cancer Discov. 2019 Sep;9(9):1152. doi: 10.1158/2159-8290.CD-NB2019-092. Epub 2019 Aug 6.

Significance of KRAS/PAK1/Crk pathway in non-small cell lung cancer oncogenesis.

BMC Cancer. 2015 May 9;15:381. doi: 10.1186/s12885-015-1360-4.

A Ras destabilizer KYA1797K overcomes the resistance of EGFR tyrosine kinase inhibitor in KRAS-mutated non-small cell lung cancer.

Sci Rep. 2019 Jan 24;9(1):648. doi: 10.1038/s41598-018-37059-8.

A Broad-Based Characterization of a Cell-Penetrating, Single Domain Camelid Bi-Specific Antibody Monomer That Targets STAT3 and KRAS Dependent Cancers.

Int J Mol Sci. 2022 Jul 8;23(14):7565. doi: 10.3390/ijms23147565.

Hexachlorophene, a selective SHP2 inhibitor, suppresses proliferation and metastasis of KRAS-mutant NSCLC cells by inhibiting RAS/MEK/ERK and PI3K/AKT signaling pathways.

Toxicol Appl Pharmacol. 2022 Apr 15;441:115988. doi: 10.1016/j.taap.2022.115988. Epub 2022 Mar 18.

MutT Homolog 1 (MTH1) maintains multiple KRAS-driven pro-malignant pathways.

Oncogene. 2015 May 14;34(20):2586-96. doi: 10.1038/onc.2014.195. Epub 2014 Jul 14.

BI-3406, a Potent and Selective SOS1-KRAS Interaction Inhibitor, Is Effective in KRAS-Driven Cancers through Combined MEK Inhibition.

Cancer Discov. 2021 Jan;11(1):142-157. doi: 10.1158/2159-8290.CD-20-0142. Epub 2020 Aug 19.

Tumor cells with KRAS or BRAF mutations or ERK5/MAPK7 amplification are not addicted to ERK5 activity for cell proliferation.

Cell Cycle. 2016;15(4):506-18. doi: 10.1080/15384101.2015.1120915.

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引用本文的文献

Biophysical and structural analysis of KRAS switch-II pocket inhibitors reveals allele-specific binding constraints.

J Biol Chem. 2025 Jun 3;301(7):110331. doi: 10.1016/j.jbc.2025.110331.

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Angew Chem Int Ed Engl. 2025 Jul 21;64(30):e202507092. doi: 10.1002/anie.202507092. Epub 2025 May 30.

Development of Receptor Desolvation Scoring and Covalent Sampling in DOCK 6: Methods Evaluated on a RAS Test Set.

J Chem Inf Model. 2025 Jan 27;65(2):722-748. doi: 10.1021/acs.jcim.4c01623. Epub 2025 Jan 6.

Capturing RAS oligomerization on a membrane.

Proc Natl Acad Sci U S A. 2024 Aug 20;121(34):e2405986121. doi: 10.1073/pnas.2405986121. Epub 2024 Aug 15.

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Front Oncol. 2024 May 22;14:1394702. doi: 10.3389/fonc.2024.1394702. eCollection 2024.

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Methods Mol Biol. 2024;2797:261-269. doi: 10.1007/978-1-0716-3822-4_19.

Membrane lipids drive formation of KRAS4b-RAF1 RBDCRD nanoclusters on the membrane.

Commun Biol. 2024 Feb 28;7(1):242. doi: 10.1038/s42003-024-05916-0.

Abnormalities in the KRAS Gene and Treatment Options for NSCLC Patients with the G12C Mutation in This Gene-A Literature Review and Single-Center Experience.

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Pathol Oncol Res. 2024 Jan 4;29:1611580. doi: 10.3389/pore.2023.1611580. eCollection 2023.

本文引用的文献

Drugging an undruggable pocket on KRAS.

Proc Natl Acad Sci U S A. 2019 Aug 6;116(32):15823-15829. doi: 10.1073/pnas.1904529116. Epub 2019 Jul 22.

The small molecule BI-2852 induces a nonfunctional dimer of KRAS.

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The small molecule BI-2852 induces a nonfunctional dimer of KRAS.

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