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The KRAS inhibitor MRTX1133 elucidates KRAS-mediated oncogenesis.

出版信息

Nat Med. 2022 Oct;28(10):2017-2018. doi: 10.1038/s41591-022-02008-6.

DOI:10.1038/s41591-022-02008-6

PMID:36207523

Abstract

摘要

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The KRAS inhibitor MRTX1133 elucidates KRAS-mediated oncogenesis.

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J Med Chem. 2022 Feb 24;65(4):3123-3133. doi: 10.1021/acs.jmedchem.1c01688. Epub 2021 Dec 10.

Inhibition mechanism of MRTX1133 on KRAS: a molecular dynamics simulation and Markov state model study.

J Comput Aided Mol Des. 2023 Mar;37(3):157-166. doi: 10.1007/s10822-023-00498-1. Epub 2023 Feb 28.

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Front Immunol. 2024 Sep 6;15:1420463. doi: 10.3389/fimmu.2024.1420463. eCollection 2024.

Role of molecular biology in the management of pancreatic cancer.

World J Gastrointest Oncol. 2024 Jul 15;16(7):2902-2914. doi: 10.4251/wjgo.v16.i7.2902.

The relationship of KRAS expression with KRAS status, prognosis, and tumor-infiltrated T lymphocytes in colorectal cancer.

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本文引用的文献

ras oncogenes in human cancer: a review.

Cancer Res. 1989 Sep 1;49(17):4682-9.

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The KRAS inhibitor MRTX1133 elucidates KRAS-mediated oncogenesis.

Nat Med. 2022 Oct;28(10):2017-2018. doi: 10.1038/s41591-022-02008-6.

Anti-tumor efficacy of a potent and selective non-covalent KRAS inhibitor.

Nat Med. 2022 Oct;28(10):2171-2182. doi: 10.1038/s41591-022-02007-7. Epub 2022 Oct 10.

KRAS inhibition reprograms the microenvironment of early and advanced pancreatic cancer to promote FAS-mediated killing by CD8 T cells.

Cancer Cell. 2023 Sep 11;41(9):1606-1620.e8. doi: 10.1016/j.ccell.2023.07.002. Epub 2023 Aug 24.

Feedback activation of EGFR/wild-type RAS signaling axis limits KRAS inhibitor efficacy in KRAS-mutated colorectal cancer.

Oncogene. 2023 May;42(20):1620-1633. doi: 10.1038/s41388-023-02676-9. Epub 2023 Apr 5.

Important role of Nfkb2 in the Kras-driven carcinogenesis in the pancreas.

Pancreatology. 2021 Aug;21(5):912-919. doi: 10.1016/j.pan.2021.03.012. Epub 2021 Mar 26.

Pathways and mechanism of MRTX1133 binding to KRAS G12D elucidated by molecular dynamics simulations and Markov state models.

Int J Biol Macromol. 2024 Aug;274(Pt 2):133374. doi: 10.1016/j.ijbiomac.2024.133374. Epub 2024 Jun 24.

Characterization of the binding of MRTX1133 as an avenue for the discovery of potential KRAS inhibitors for cancer therapy.

Sci Rep. 2022 Oct 22;12(1):17796. doi: 10.1038/s41598-022-22668-1.

Identification of MRTX1133, a Noncovalent, Potent, and Selective KRAS Inhibitor.

J Med Chem. 2022 Feb 24;65(4):3123-3133. doi: 10.1021/acs.jmedchem.1c01688. Epub 2021 Dec 10.

Inhibition mechanism of MRTX1133 on KRAS: a molecular dynamics simulation and Markov state model study.

J Comput Aided Mol Des. 2023 Mar;37(3):157-166. doi: 10.1007/s10822-023-00498-1. Epub 2023 Feb 28.

Metabolomic, Proteomic, and Single-Cell Proteomic Analysis of Cancer Cells Treated with the KRAS Inhibitor MRTX1133.

J Proteome Res. 2023 Dec 1;22(12):3703-3713. doi: 10.1021/acs.jproteome.3c00212. Epub 2023 Nov 20.

引用本文的文献

The complex journey of targeting RAS in oncology.

BMC Cancer. 2025 Jul 1;25(1):1053. doi: 10.1186/s12885-025-14033-y.

A first-in-class EGFR-directed KRAS G12V selective inhibitor.

Cancer Cell. 2025 Jun 16. doi: 10.1016/j.ccell.2025.05.016.

Response and Resistance to RAS Inhibition in Cancer.

Cancer Discov. 2025 Jul 3;15(7):1325-1349. doi: 10.1158/2159-8290.CD-25-0349.

Pancreatic Cancer: Pathogenesis and Clinical Studies.

MedComm (2020). 2025 Apr 2;6(4):e70162. doi: 10.1002/mco2.70162. eCollection 2025 Apr.

Genomic landscape of clinically acquired resistance alterations in patients treated with KRAS inhibitors.

Ann Oncol. 2025 Jun;36(6):682-692. doi: 10.1016/j.annonc.2025.01.020. Epub 2025 Feb 4.

, a New Target for Precision Medicine in Colorectal Cancer?

Cancers (Basel). 2024 Oct 12;16(20):3455. doi: 10.3390/cancers16203455.

Combined KRAS Inhibition and Immune Therapy Generates Durable Complete Responses in an Autochthonous PDAC Model.

Cancer Discov. 2025 Jan 13;15(1):162-178. doi: 10.1158/2159-8290.CD-24-0489.

Photonanozyme-Kras-ribosome combination treatment of non-small cell lung cancer after COVID-19.

Front Immunol. 2024 Sep 6;15:1420463. doi: 10.3389/fimmu.2024.1420463. eCollection 2024.

Role of molecular biology in the management of pancreatic cancer.

World J Gastrointest Oncol. 2024 Jul 15;16(7):2902-2914. doi: 10.4251/wjgo.v16.i7.2902.

The relationship of KRAS expression with KRAS status, prognosis, and tumor-infiltrated T lymphocytes in colorectal cancer.

Therap Adv Gastroenterol. 2024 May 15;17:17562848241249387. doi: 10.1177/17562848241249387. eCollection 2024.

本文引用的文献

ras oncogenes in human cancer: a review.

Cancer Res. 1989 Sep 1;49(17):4682-9.

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The KRAS inhibitor MRTX1133 elucidates KRAS-mediated oncogenesis.

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