4.8 Article

Chemical remodeling of a cellular chaperone to target the active state of mutant KRAS

相关参考文献

注意:仅列出部分参考文献,下载原文获取全部文献信息。
Article Oncology

Discovery, Preclinical Characterization, and Early Clinical Activity of JDQ443, a Structurally Novel, Potent, and Selective Covalent Oral Inhibitor of KRASG12C

Andreas Weiss et al.

Summary: JDQ443 is a structurally unique covalent inhibitor of KRAS(G12C) that demonstrates potent and selective antitumor activity in cell lines and in vivo models. In preclinical models and patients with KRAS(G12C)-mutated malignancies, JDQ443 shows potent antitumor activity as monotherapy and in combination with the SHP2 inhibitor TNO155.

CANCER DISCOVERY (2022)

Article Medicine, General & Internal

Adagrasib in Non-Small-Cell Lung Cancer Harboring a KRASG12C Mutation

Pasi A. Jaenne et al.

Summary: Adagrasib demonstrated clinical efficacy without new safety signals in previously treated KRAS(G12C)-mutated NSCLC patients.

NEW ENGLAND JOURNAL OF MEDICINE (2022)

Article Oncology

HER2 mediates clinical resistance to the KRASG12C inhibitor sotorasib, which is overcome by co-targeting SHP2

Cassandra S. L. Ho et al.

Summary: The study demonstrates that HER2 copy number gain is a clinically relevant resistance mechanism to pharmacological KRASG12C inhibition in lung cancer patients. Co-targeting SHP2 can overcome this resistance mechanism effectively.

EUROPEAN JOURNAL OF CANCER (2021)

Article Multidisciplinary Sciences

Diverse alterations associated with resistance to KRAS(G12C) inhibition

Yulei Zhao et al.

Summary: Resistance to KRAS(G12C) inhibitors demonstrates a heterogeneous pattern with multiple subclonal events emerging during treatment. Co-targeting of ERK signaling intermediates can enhance the antiproliferative effect of G12C inhibitor treatment in models with acquired RAS or BRAF mutations.

NATURE (2021)

Article Multidisciplinary Sciences

The G protein signaling regulator RGS3 enhances the GTPase activity of KRAS

Chuanchuan Li et al.

Summary: This study reveals that RGS3 enhances the GTPase activity of both mutant and wild-type KRAS proteins, leading to the inactivation of KRAS and explaining its vulnerability to emerging clinically effective therapies.

SCIENCE (2021)

Article Multidisciplinary Sciences

KRAS interaction with RAF1 RAS-binding domain and cysteine-rich domain provides insights into RAS-mediated RAF activation

Timothy H. Tran et al.

Summary: This study presents molecular details of the RAS-RAF interaction, including the crystal structures of KRAS binding with RAF1 and a proposed model of membrane-bound RAS-RAF complex formation.

NATURE COMMUNICATIONS (2021)

Article Oncology

Clinical Acquired Resistance to KRASG12C Inhibition through a novel KRAS Switch-II Pocket Mutation and Polyclonal Alterations Converging on RAS-MAPK Reactivation

Noritaka Tanaka et al.

Summary: This study described a patient with KRAS(G12C) non-small cell lung cancer who developed polyclonal acquired resistance to MRTX849 treatment. The research identified 10 heterogeneous resistance alterations that converged to reactivate the RAS-MAPK signaling pathway. Additionally, a novel KRAS(Y96D) mutation affecting key protein-drug interactions and driving resistance was discovered.

CANCER DISCOVERY (2021)

Article Medicine, General & Internal

Acquired Resistance to KRASG12C Inhibition in Cancer

M. M. Awad et al.

Summary: A study of 38 patients with KRAS(G12C)-mutant cancers treated with adagrasib revealed diverse mechanisms of acquired resistance in 45% of them, including various mutations and bypass mechanisms. New therapeutic strategies are needed to overcome this drug resistance.

NEW ENGLAND JOURNAL OF MEDICINE (2021)

Article Multidisciplinary Sciences

Rapid non-uniform adaptation to conformation-specific KRAS(G12C) inhibition

Jenny Y. Xue et al.

NATURE (2020)

Article Multidisciplinary Sciences

Genomic discovery of an evolutionarily programmed modality for small-molecule targeting of an intractable surface

Uddhav K. Shigdel et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2020)

Article Biochemistry & Molecular Biology

KRASG12C inhibition produces a driver-limited state revealing collateral dependencies

Kevin Lou et al.

SCIENCE SIGNALING (2019)

Article Biochemical Research Methods

Macromolecular structure determination using X-rays, neutrons and electrons: recent developments in Phenix

Dorothee Liebschner et al.

ACTA CRYSTALLOGRAPHICA SECTION D-STRUCTURAL BIOLOGY (2019)

Review Oncology

New Horizons in KRAS-Mutant Lung Cancer: Dawn After Darkness

Haitang Yang et al.

FRONTIERS IN ONCOLOGY (2019)

Article Chemistry, Multidisciplinary

Bifunctional Small-Molecule Ligands of K-Ras Induce Its Association with Immunophilin Proteins

Ziyang Zhang et al.

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2019)

Article Multidisciplinary Sciences

The clinical KRAS(G12C) inhibitor AMG 510 drives anti-tumour immunity

Jude Canon et al.

NATURE (2019)

Article Chemistry, Multidisciplinary

Rapamycin-inspired macrocycles with new target specificity

Zufeng Guo et al.

NATURE CHEMISTRY (2019)

Article Biochemistry & Molecular Biology

GEPIA: a web server for cancer and normal gene expression profiling and interactive analyses

Zefang Tang et al.

NUCLEIC ACIDS RESEARCH (2017)

Review Biochemistry & Molecular Biology

RAS Proteins and Their Regulators in Human Disease

Dhirendra K. Simanshu et al.

Article Multidisciplinary Sciences

Allele-specific inhibitors inactivate mutant KRAS G12C by a trapping mechanism

Piro Lito et al.

SCIENCE (2016)

Article Multidisciplinary Sciences

K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions

Jonathan M. Ostrem et al.

NATURE (2013)

Article Biochemical Research Methods

REFMAC5 for the refinement of macromolecular crystal structures

Garib N. Murshudov et al.

ACTA CRYSTALLOGRAPHICA SECTION D-STRUCTURAL BIOLOGY (2011)

Review Oncology

RAS oncogenes: weaving a tumorigenic web

Yuliya Pylayeva-Gupta et al.

NATURE REVIEWS CANCER (2011)

Article Biochemical Research Methods

XDS

Wolfgang Kabsch

ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY (2010)

Article Biochemical Research Methods

Features and development of Coot

P. Emsley et al.

ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY (2010)

Article Multidisciplinary Sciences

Hidden alternative structures of proline isomerase essential for catalysis

James S. Fraser et al.

NATURE (2009)

Article Biochemistry & Molecular Biology

Structural coupling between FKBP12 and buried water

Szilvia Szep et al.

PROTEINS-STRUCTURE FUNCTION AND BIOINFORMATICS (2009)

Article Chemistry, Multidisciplinary

Phaser crystallographic software

Airlie J. McCoy et al.

JOURNAL OF APPLIED CRYSTALLOGRAPHY (2007)

Article Chemistry, Multidisciplinary

Characterization of the FKBP•Rapamycin•FRB ternary complex

LA Banaszynski et al.

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2005)

Article Biochemistry & Molecular Biology

Structural analysis of autoinhibition in the Ras activator son of sevenless

H Sondermann et al.