Targeting metabolic vulnerability in mitochondria conquers MEK inhibitor resistance in KRAS-mutant lung cancer

Discovery and Lead Optimization of Benzene-1,4-disulfonamides as Oxidative Phosphorylation Inhibitors

(2022) Ding Xue et al.   JOURNAL OF MEDICINAL CHEMISTRY

Multiparameter Optimization of Oxidative Phosphorylation Inhibitors for the Treatment of Pancreatic Cancer

(2022) Ding Xue et al.   JOURNAL OF MEDICINAL CHEMISTRY

Cancer Statistics, 2021

(2021) Rebecca L. Siegel et al.   CA-A CANCER JOURNAL FOR CLINICIANS

Cork-in-bottle mechanism of inhibitor binding to mammalian complex I

(2021) Injae Chung et al.   Science Advances

Oxidative phosphorylation is a metabolic vulnerability in chemotherapy-resistant triple negative breast cancer

(2021) Kurt W. Evans et al.   CANCER RESEARCH

Metabolic Enzyme DLST Promotes Tumor Aggression and Reveals a Vulnerability to OXPHOS Inhibition in High-Risk Neuroblastoma

(2021) Nicole M. Anderson et al.   CANCER RESEARCH

Acquired Resistance to KRASG12C Inhibition in Cancer

(2021) Mark M. Awad et al.   NEW ENGLAND JOURNAL OF MEDICINE

Targeting AKR1B1 inhibits glutathione de novo synthesis to overcome acquired resistance to EGFR-targeted therapy in lung cancer

(2021) Ke-Ren Zhang et al.   Science Translational Medicine

Phase I/II Trial of Immunotherapy with Durvalumab and Tremelimumab With Continuous or Intermittent MEK Inhibitor Selumetinib in NSCLC: Early trial report

(2020) Pierre-Olivier Gaudreau et al.   Clinical Lung Cancer

Targeting the MAPK Pathway in KRAS-Driven Tumors

(2020) Matthias Drosten et al.   CANCER CELL

IACS-010759, a potent inhibitor of glycolysis-deficient hypoxic tumor cells, inhibits mitochondrial respiratory complex I through a unique mechanism

(2020) Atsuhito Tsuji et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

MSC-induced lncRNA HCP5 drove fatty acid oxidation through miR-3619-5p/AMPK/PGC1α/CEBPB axis to promote stemness and chemo-resistance of gastric cancer

(2020) Honglei Wu et al.   Cell Death & Disease

RAS-targeted therapies: is the undruggable drugged?

(2020) Amanda R. Moore et al.   NATURE REVIEWS DRUG DISCOVERY

The protective effect of natural compounds against rotenone‐induced neurotoxicity

(2020) Fatemeh Yarmohammadi et al.   JOURNAL OF BIOCHEMICAL AND MOLECULAR TOXICOLOGY

Phosphorylation of PDHA by AMPK Drives TCA Cycle to Promote Cancer Metastasis

(2020) Zhen Cai et al.   MOLECULAR CELL

BI-3406, a potent and selective SOS1::KRAS interaction inhibitor, is effective in KRAS-driven cancers through combined MEK inhibition

(2020) Marco H Hofmann et al.   Cancer Discovery

Durable Suppression of Acquired MEK Inhibitor Resistance in Cancer by Sequestering MEK from ERK and Promoting Anti-Tumor T-cell Immunity

(2020) Aayoung Hong et al.   Cancer Discovery

Targeting the untargetable KRAS in cancer therapy

(2019) Pingyu Liu et al.   Acta Pharmaceutica Sinica B

Combination of Hypoglycemia and Metformin Impairs Tumor Metabolic Plasticity and Growth by Modulating the PP2A-GSK3β-MCL-1 Axis

(2019) Mohamed Elgendy et al.   CANCER CELL

SHOC2 phosphatase-dependent RAF dimerization mediates resistance to MEK inhibition in RAS-mutant cancers

(2019) Greg G. Jones et al.   Nature Communications

A novel mitochondrial inhibitor blocks MAPK pathway and overcomes MAPK inhibitor-resistance in melanoma.

(2019) Y.N. Vashisht Gopal et al.   CLINICAL CANCER RESEARCH

A Fatty Acid Oxidation-dependent Metabolic Shift Regulates the Adaptation of BRAF-mutated Melanoma to MAPK Inhibitors

(2019) Andrea Aloia et al.   CLINICAL CANCER RESEARCH

Metabolic Flexibility in Cancer: Targeting the Pyruvate Dehydrogenase Kinase:Pyruvate Dehydrogenase Axis

(2019) Benjamin L. Woolbright et al.   MOLECULAR CANCER THERAPEUTICS

MET Inhibition Elicits PGC1α-Dependent Metabolic Reprogramming in Glioblastoma

(2019) Yiru Zhang et al.   CANCER RESEARCH

Suppression of the SLC7A11/glutathione axis causes synthetic lethality in KRAS-mutant lung adenocarcinoma

(2019) Kewen Hu et al.   JOURNAL OF CLINICAL INVESTIGATION

Compartmentalized activities of the pyruvate dehydrogenase complex sustain lipogenesis in prostate cancer

(2018) Jingjing Chen et al.   NATURE GENETICS

An inhibitor of oxidative phosphorylation exploits cancer vulnerability

(2018) Jennifer R. Molina et al.   NATURE MEDICINE

Mutations in the SWI/SNF complex induce a targetable dependence on oxidative phosphorylation in lung cancer

(2018) Yonathan Lissanu Deribe et al.   NATURE MEDICINE

Targeting ERK, an Achilles' Heel of the MAPK pathway, in cancer therapy

(2018) Feifei Liu et al.   Acta Pharmaceutica Sinica B

Overcoming Resistance to Dual Innate Immune and MEK Inhibition Downstream of KRAS

(2018) Shunsuke Kitajima et al.   CANCER CELL

Therapeutic strategies to target RAS-mutant cancers

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

A Phase 1/1b Study Evaluating Trametinib Plus Docetaxel or Pemetrexed in Patients With Advanced Non–Small Cell Lung Cancer

(2017) David R. Gandara et al.   Journal of Thoracic Oncology

Study Design and Rationale for a Randomized, Placebo-Controlled, Double-Blind Study to Assess the Efficacy and Safety of Selumetinib in Combination With Docetaxel as Second-Line Treatment in Patients With KRAS-Mutant Advanced Non-Small Cell Lung Cancer (SELECT-1)

(2016) Pasi A. Jänne et al.   Clinical Lung Cancer

Targeting mitochondrial biogenesis to overcome drug resistance to MAPK inhibitors

(2016) Gao Zhang et al.   JOURNAL OF CLINICAL INVESTIGATION

Mitochondria-Translocated PGK1 Functions as a Protein Kinase to Coordinate Glycolysis and the TCA Cycle in Tumorigenesis

(2016) Xinjian Li et al.   MOLECULAR CELL

A combinatorial strategy for treating KRAS-mutant lung cancer

(2016) Eusebio Manchado et al.   NATURE

Fatty acid oxidation and carnitine palmitoyltransferase I: emerging therapeutic targets in cancer

(2016) Q Qu et al.   Cell Death & Disease

Targeting Tumor Mitochondrial Metabolism Overcomes Resistance to Antiangiogenics

(2016) Paloma Navarro et al.   Cell Reports

Targeting the leukemia cell metabolism by the CPT1a inhibition: functional preclinical effects in leukemias

(2015) M. R. Ricciardi et al.   BLOOD

An Essential Role of the Mitochondrial Electron Transport Chain in Cell Proliferation Is to Enable Aspartate Synthesis

(2015) Kıvanç Birsoy et al.   CELL

MYC/PGC-1α Balance Determines the Metabolic Phenotype and Plasticity of Pancreatic Cancer Stem Cells

(2015) Patricia Sancho et al.   Cell Metabolism

Pyruvate carboxylase is critical for non–small-cell lung cancer proliferation

(2015) Katherine Sellers et al.   JOURNAL OF CLINICAL INVESTIGATION

Metformin in patients with advanced pancreatic cancer: a double-blind, randomised, placebo-controlled phase 2 trial

(2015) Sil Kordes et al.   LANCET ONCOLOGY

Disruption of CRAF-Mediated MEK Activation Is Required for Effective MEK Inhibition in KRAS Mutant Tumors

(2014) Piro Lito et al.   CANCER CELL

Is Reliance on Mitochondrial Respiration a “Chink in the Armor” of Therapy-Resistant Cancer?

(2014) Dieter A. Wolf   CANCER CELL

The Pyruvate Dehydrogenase Complexes: Structure-based Function and Regulation

(2014) Mulchand S. Patel et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

ERK-mediated phosphorylation of TFAM downregulates mitochondrial transcription: Implications for Parkinson's disease

(2014) Kent Z.Q. Wang et al.   MITOCHONDRION

Oncogene ablation-resistant pancreatic cancer cells depend on mitochondrial function

(2014) Andrea Viale et al.   NATURE

Targeting Oxidative Phosphorylation: Why, When, and How

(2013) Michael Pollak   CANCER CELL

Oncogenic BRAF Regulates Oxidative Metabolism via PGC1α and MITF

(2013) Rizwan Haq et al.   CANCER CELL

A key role for mitochondrial gatekeeper pyruvate dehydrogenase in oncogene-induced senescence

(2013) Joanna Kaplon et al.   NATURE

Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers

(2013) Georgia Hatzivassiliou et al.   NATURE

Pyruvate dehydrogenase deficiency and the brain

(2012) GARRY BROWN   DEVELOPMENTAL MEDICINE AND CHILD NEUROLOGY

Imp2 controls oxidative phosphorylation and is crucial for preserving glioblastoma cancer stem cells

(2012) M. Janiszewska et al.   GENES & DEVELOPMENT

PI3K Pathway Activation Mediates Resistance to MEK Inhibitors in KRAS Mutant Cancers

(2009) S. Wee et al.   CANCER RESEARCH