SHP2 inhibition diminishes KRASG12C cycling and promotes tumor microenvironment remodeling

A12 The SHP2 Inhibitor RMC-4630 in Patients with KRAS-Mutant Non-Small Cell Lung Cancer: Preliminary Evaluation of a First-in-Man Phase 1 Clinical Trial

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

(2020) Jenny Y. Xue et al.   NATURE

Grail of RAS cancer drugs within reach

(2020) Cormac Sheridan   NATURE BIOTECHNOLOGY

Endothelial heterogeneity across distinct vascular beds during homeostasis and inflammation

(2020) Ankit Jambusaria et al.   eLife

The Frequency of Ras Mutations in Cancer

(2020) Ian A. Prior et al.   CANCER RESEARCH

Allosteric inhibition of SHP2 stimulates anti-tumor immunity by transforming the immunosuppressive environment

(2020) Elsa Quintana et al.   CANCER RESEARCH

Repression of the Type I Interferon Pathway Underlies MYC- and KRAS-Dependent Evasion of NK and B Cells in Pancreatic Ductal Adenocarcinoma

(2020) Nathiya Muthalagu et al.   Cancer Discovery

SHP2 Drives Adaptive Resistance to ERK Signaling Inhibition in Molecularly Defined Subsets of ERK-Dependent Tumors

(2019) Tamer A. Ahmed et al.   Cell Reports

KRAS-IRF2 Axis Drives Immune Suppression and Immune Therapy Resistance in Colorectal Cancer

(2019) Wenting Liao et al.   CANCER CELL

KRASG12C inhibition produces a driver-limited state revealing collateral dependencies

(2019) Kevin Lou et al.   Science Signaling

Direct Ras G12C inhibitors: crossing the rubicon

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Tumor intrinsic efficacy by SHP2 and RTK inhibitors in KRAS mutant cancers

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Vertical pathway inhibition overcomes adaptive feedback resistance to KRASG12C inhibition

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

(2019) Jude Canon et al.   NATURE

The KRASG12C Inhibitor MRTX849 Provides Insight toward Therapeutic Susceptibility of KRAS-Mutant Cancers in Mouse Models and Patients

(2019) Jill Hallin et al.   Cancer Discovery

A Convergence-Based Framework for Cancer Drug Resistance

(2018) David J. Konieczkowski et al.   CANCER CELL

CXCL9, CXCL10, CXCL11/CXCR3 axis for immune activation – A target for novel cancer therapy

(2018) Ryuma Tokunaga et al.   CANCER TREATMENT REVIEWS

Targeting KRAS Mutant Cancers with a Covalent G12C-Specific Inhibitor

(2018) Matthew R. Janes et al.   CELL

Assessing Therapeutic Efficacy of MEK Inhibition in a KRAS G12C-Driven Mouse Model of Lung Cancer

(2018) Shuai Li et al.   CLINICAL CANCER RESEARCH

Mutant KRAS-driven cancers depend on PTPN11/SHP2 phosphatase

(2018) Dietrich A. Ruess et al.   NATURE MEDICINE

Targeting wild-type KRAS-amplified gastroesophageal cancer through combined MEK and SHP2 inhibition

(2018) Gabrielle S. Wong et al.   NATURE MEDICINE

SHP2 is required for growth of KRAS-mutant non-small-cell lung cancer in vivo

(2018) Sara Mainardi et al.   NATURE MEDICINE

Understanding the tumor immune microenvironment (TIME) for effective therapy

(2018) Mikhail Binnewies et al.   NATURE MEDICINE

The reactivity-driven biochemical mechanism of covalent KRASG12C inhibitors

(2018) Rasmus Hansen et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

The reactivity-driven biochemical mechanism of covalent KRASG12C inhibitors

(2018) Rasmus Hansen et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Effect of CCL5 expression in the recruitment of immune cells in triple negative breast cancer

(2018) Jhajaira M. Araujo et al.   Scientific Reports

Targeting the MAPK Pathway in RAS Mutant Cancers

(2018) Sarah G. Hymowitz et al.   Cold Spring Harbor Perspectives in Medicine

RAS nucleotide cycling underlies the SHP2 phosphatase dependence of mutant BRAF-, NF1- and RAS-driven cancers

(2018) Robert J. Nichols et al.   NATURE CELL BIOLOGY

SHP2 Inhibition Prevents Adaptive Resistance to MEK Inhibitors in Multiple Cancer Models

(2018) Carmine Fedele et al.   Cancer Discovery

KRAS G12C NSCLC Models Are Sensitive to Direct Targeting of KRAS in Combination with PI3K Inhibition

(2018) Sandra Misale et al.   CLINICAL CANCER RESEARCH

Small Molecule Inhibitor that Stabilizes the Autoinhibited Conformation of the Oncogenic Tyrosine Phosphatase SHP2

(2018) Xiaoqin Wu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Therapeutic strategies to target RAS-mutant cancers

(2018) Meagan B. Ryan et al.   Nature Reviews Clinical Oncology

Mechanism of activating mutations and allosteric drug inhibition of the phosphatase SHP2

(2018) Ricardo A. P. Pádua et al.   Nature Communications

Structural reorganization of SHP2 by oncogenic mutations and implications for oncoprotein resistance to allosteric inhibition

(2018) Jonathan R. LaRochelle et al.   Nature Communications

The small GTPases K-Ras, N-Ras, and H-Ras have distinct biochemical properties determined by allosteric effects

(2017) Christian W. Johnson et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Mutational landscape of metastatic cancer revealed from prospective clinical sequencing of 10,000 patients

(2017) Ahmet Zehir et al.   NATURE MEDICINE

Affinity purification mass spectrometry analysis of PD-1 uncovers SAP as a new checkpoint inhibitor

(2017) Michael Peled et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

T cell costimulatory receptor CD28 is a primary target for PD-1–mediated inhibition

(2017) Enfu Hui et al.   SCIENCE

Enhancer Remodeling during Adaptive Bypass to MEK Inhibition Is Attenuated by Pharmacologic Targeting of the P-TEFb Complex

(2017) Jon S. Zawistowski et al.   Cancer Discovery

A Landscape of Therapeutic Cooperativity in KRAS Mutant Cancers Reveals Principles for Controlling Tumor Evolution

(2017) Grace R. Anderson et al.   Cell Reports

Strategies for monitoring and combating resistance to combination kinase inhibitors for cancer therapy

(2017) Leanne G. Ahronian et al.   Genome Medicine

Deconstruction of the Ras switching cycle through saturation mutagenesis

(2017) Pradeep Bandaru et al.   eLife

Sticking It to Cancer with Molecular Glue for SHP2

(2016) Hao Ran et al.   CANCER CELL

RAS isoforms and mutations in cancer at a glance

(2016) G. Aaron Hobbs et al.   JOURNAL OF CELL SCIENCE

Allosteric Inhibition of SHP2: Identification of a Potent, Selective, and Orally Efficacious Phosphatase Inhibitor

(2016) Jorge Garcia Fortanet et al.   JOURNAL OF MEDICINAL CHEMISTRY

Allosteric inhibition of SHP2 phosphatase inhibits cancers driven by receptor tyrosine kinases

(2016) Ying-Nan P. Chen et al.   NATURE

A combinatorial strategy for treating KRAS-mutant lung cancer

(2016) Eusebio Manchado et al.   NATURE

Direct small-molecule inhibitors of KRAS: from structural insights to mechanism-based design

(2016) Jonathan M. L. Ostrem et al.   NATURE REVIEWS DRUG DISCOVERY

Antigen clasping by two antigen-binding sites of an exceptionally specific antibody for histone methylation

(2016) Takamitsu Hattori et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

(2016) P. Lito et al.   SCIENCE

Selective Inhibition of Oncogenic KRAS Output with Small Molecules Targeting the Inactive State

(2016) M. P. Patricelli et al.   Cancer Discovery

Biochemical and Structural Analysis of Common Cancer-Associated KRAS Mutations

(2015) J. C. Hunter et al.   MOLECULAR CANCER RESEARCH

The Hippo effector YAP promotes resistance to RAF- and MEK-targeted cancer therapies

(2015) Luping Lin et al.   NATURE GENETICS

Oncogenic and RASopathy-associated K-RAS mutations relieve membrane-dependent occlusion of the effector-binding site

(2015) Mohammad T. Mazhab-Jafari et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Dragging Ras Back in the Ring

(2014) Andrew G. Stephen et al.   CANCER CELL

Integrated RAS signaling defined by parallel NMR detection of effectors and regulators

(2014) Matthew J Smith et al.   Nature Chemical Biology

ColonyArea: An ImageJ Plugin to Automatically Quantify Colony Formation in Clonogenic Assays

(2014) Camilo Guzmán et al.   PLoS One

Intrinsic Resistance to MEK Inhibition in KRAS Mutant Lung and Colon Cancer through Transcriptional Induction of ERBB3

(2014) Chong Sun et al.   Cell Reports

Chemokines in Cancer

(2014) M. T. Chow et al.   Cancer Immunology Research

Inflammatory networks and immune surveillance of pancreatic carcinoma

(2013) Robert H Vonderheide et al.   CURRENT OPINION IN IMMUNOLOGY

Mutational landscape and significance across 12 major cancer types

(2013) Cyriac Kandoth et al.   NATURE

Emerging landscape of oncogenic signatures across human cancers

(2013) Giovanni Ciriello et al.   NATURE GENETICS

Microenvironmental regulation of tumor progression and metastasis

(2013) Daniela F Quail et al.   NATURE MEDICINE

Endothelial Cell Heterogeneity

(2013) W. C. Aird   Cold Spring Harbor Perspectives in Medicine

IRF-3, IRF-5, and IRF-7 Coordinately Regulate the Type I IFN Response in Myeloid Dendritic Cells Downstream of MAVS Signaling

(2013) Helen M. Lazear et al.   PLoS Pathogens

Dynamic Reprogramming of the Kinome in Response to Targeted MEK Inhibition in Triple-Negative Breast Cancer

(2012) James S. Duncan et al.   CELL

Programmed cell death 1 forms negative costimulatory microclusters that directly inhibit T cell receptor signaling by recruiting phosphatase SHP2

(2012) Tadashi Yokosuka et al.   JOURNAL OF EXPERIMENTAL MEDICINE

Germline KRAS mutations cause aberrant biochemical and physical properties leading to developmental disorders

(2010) Lothar Gremer et al.   HUMAN MUTATION

Melanomas acquire resistance to B-RAF(V600E) inhibition by RTK or N-RAS upregulation

(2010) Ramin Nazarian et al.   NATURE

Detection of Mycoplasma in cell cultures

(2010) Lesley Young et al.   Nature Protocols

V600EBRAF is associated with disabled feedback inhibition of RAF-MEK signaling and elevated transcriptional output of the pathway

(2009) C. A. Pratilas et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA