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Literature DB >> 32001483

Overcoming Adaptive Resistance to KRAS Inhibitors Through Vertical Pathway Targeting.

Abstract

KRAS G12C inhibitors have shown promise in KRAS G12C-mutant lung cancer but intrinsic and acquired resistance are common. Cotreatment with inhibitors of the protein phosphatase SHP2 can abrogate the adaptive response of cancer cells to KRAS inhibitors resulting in greater suppression of MAPK signaling and enhanced tumor growth inhibition.See related article by Ryan et al., p. 1633. ©2020 American Association for Cancer Research.

Entities: Chemical Disease Gene Mutation Species

Mesh：

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Year: 2020 PMID： 32001483 PMCID： PMC7453631 DOI： 10.1158/1078-0432.CCR-19-4060

Source DB: PubMed Journal: Clin Cancer Res ISSN： 1078-0432 Impact factor: 12.531

4 in total

1. Vertical Pathway Inhibition Overcomes Adaptive Feedback Resistance to KRAS^G12C Inhibition.

Authors: Meagan B Ryan; Ferran Fece de la Cruz; Sarah Phat; David T Myers; Edmond Wong; Heather A Shahzade; Catriona B Hong; Ryan B Corcoran
Journal: Clin Cancer Res Date: 2019-11-27 Impact factor: 12.531

2. Combined BRAF, EGFR, and MEK Inhibition in Patients with BRAF^V600E-Mutant Colorectal Cancer.

Authors: Ryan B Corcoran; Thierry André; Chloe E Atreya; Jan H M Schellens; Takayuki Yoshino; Johanna C Bendell; Antoine Hollebecque; Autumn J McRee; Salvatore Siena; Gary Middleton; Kei Muro; Michael S Gordon; Josep Tabernero; Rona Yaeger; Peter J O'Dwyer; Yves Humblet; Filip De Vos; A Scott Jung; Jan C Brase; Savina Jaeger; Severine Bettinger; Bijoyesh Mookerjee; Fatima Rangwala; Eric Van Cutsem
Journal: Cancer Discov Date: 2018-02-05 Impact factor: 39.397

3. Relief of profound feedback inhibition of mitogenic signaling by RAF inhibitors attenuates their activity in BRAFV600E melanomas.

Authors: Piro Lito; Christine A Pratilas; Eric W Joseph; Madhavi Tadi; Ensar Halilovic; Matthew Zubrowski; Alan Huang; Wai Lin Wong; Margaret K Callahan; Taha Merghoub; Jedd D Wolchok; Elisa de Stanchina; Sarat Chandarlapaty; Poulikos I Poulikakos; James A Fagin; Neal Rosen
Journal: Cancer Cell Date: 2012-11-13 Impact factor: 31.743

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

Authors: Piro Lito; Martha Solomon; Lian-Sheng Li; Rasmus Hansen; Neal Rosen
Journal: Science Date: 2016-01-14 Impact factor: 47.728

4 in total

11 in total

Review 1. Stem Cell Models for Cancer Therapy.

Authors: Nitin Telang
Journal: Int J Mol Sci Date: 2022-06-24 Impact factor: 6.208

Review 2. The treatment of advanced non-small cell lung cancer harboring KRAS mutation: a new class of drugs for an old target-a narrative review.

Authors: Alessia Spagnuolo; Paolo Maione; Cesare Gridelli
Journal: Transl Lung Cancer Res Date: 2022-06

Review 9. Adaptive chromatin remodeling and transcriptional changes of the functional kinome in tumor cells in response to targeted kinase inhibition.

Authors: Michael P East; Gary L Johnson
Journal: J Biol Chem Date: 2021-12-24 Impact factor: 5.157

10. Focal Adhesion Kinase (FAK) Inhibition Synergizes with KRAS G12C Inhibitors in Treating Cancer through the Regulation of the FAK-YAP Signaling.

Authors: Baoyuan Zhang; Yan Zhang; Jiangwei Zhang; Ping Liu; Bo Jiao; Zaiqi Wang; Ruibao Ren
Journal: Adv Sci (Weinh) Date: 2021-06-20 Impact factor: 16.806

Overcoming Adaptive Resistance to KRAS Inhibitors Through Vertical Pathway Targeting.

1. Vertical Pathway Inhibition Overcomes Adaptive Feedback Resistance to KRAS^G12C Inhibition.

2. Combined BRAF, EGFR, and MEK Inhibition in Patients with BRAF^V600E-Mutant Colorectal Cancer.

3. Relief of profound feedback inhibition of mitogenic signaling by RAF inhibitors attenuates their activity in BRAFV600E melanomas.

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

Review 1. Stem Cell Models for Cancer Therapy.

Review 2. The treatment of advanced non-small cell lung cancer harboring KRAS mutation: a new class of drugs for an old target-a narrative review.

Review 3. Glycogen Synthase Kinase 3β in Cancer Biology and Treatment.

Review 4. Structure-based inhibitor design of mutant RAS proteins-a paradigm shift.

Review 5. Targeting KRAS in Non-Small Cell Lung Cancer.

Review 6. KRAS mutation: from undruggable to druggable in cancer.

7. Overcoming Resistance to Drugs Targeting KRAS^G12C Mutation.

Review 8. Growth Inhibitory Efficacy of Chinese Herbs in a Cellular Model for Triple-Negative Breast Cancer.

Review 9. Adaptive chromatin remodeling and transcriptional changes of the functional kinome in tumor cells in response to targeted kinase inhibition.

10. Focal Adhesion Kinase (FAK) Inhibition Synergizes with KRAS G12C Inhibitors in Treating Cancer through the Regulation of the FAK-YAP Signaling.

Overcoming Adaptive Resistance to KRAS Inhibitors Through Vertical Pathway Targeting.

1. Vertical Pathway Inhibition Overcomes Adaptive Feedback Resistance to KRASG12C Inhibition.

2. Combined BRAF, EGFR, and MEK Inhibition in Patients with BRAFV600E-Mutant Colorectal Cancer.

3. Relief of profound feedback inhibition of mitogenic signaling by RAF inhibitors attenuates their activity in BRAFV600E melanomas.

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

Review 1. Stem Cell Models for Cancer Therapy.

Review 2. The treatment of advanced non-small cell lung cancer harboring KRAS mutation: a new class of drugs for an old target-a narrative review.

Review 3. Glycogen Synthase Kinase 3β in Cancer Biology and Treatment.

Review 4. Structure-based inhibitor design of mutant RAS proteins-a paradigm shift.

Review 5. Targeting KRAS in Non-Small Cell Lung Cancer.

Review 6. KRAS mutation: from undruggable to druggable in cancer.

7. Overcoming Resistance to Drugs Targeting KRASG12C Mutation.

Review 8. Growth Inhibitory Efficacy of Chinese Herbs in a Cellular Model for Triple-Negative Breast Cancer.

Review 9. Adaptive chromatin remodeling and transcriptional changes of the functional kinome in tumor cells in response to targeted kinase inhibition.

10. Focal Adhesion Kinase (FAK) Inhibition Synergizes with KRAS G12C Inhibitors in Treating Cancer through the Regulation of the FAK-YAP Signaling.

1. Vertical Pathway Inhibition Overcomes Adaptive Feedback Resistance to KRAS^G12C Inhibition.

2. Combined BRAF, EGFR, and MEK Inhibition in Patients with BRAF^V600E-Mutant Colorectal Cancer.

7. Overcoming Resistance to Drugs Targeting KRAS^G12C Mutation.