Targeting cancer metabolism in the era of precision oncology

Targeting ACSS2 with a transition state mimetic inhibits triple-negative breast cancer growth

(2021) Katelyn D. Miller et al.   CANCER RESEARCH

Acetyl-CoA Synthetase 2: A Critical Linkage in Obesity-Induced Tumorigenesis in Myeloma

(2021) Zongwei Li et al.   Cell Metabolism

The amino acid transporter SLC7A5 is required for efficient growth of KRAS-mutant colorectal cancer

(2021) Arafath K. Najumudeen et al.   NATURE GENETICS

Serine synthesis pathway inhibition cooperates with dietary serine and glycine limitation for cancer therapy

(2021) Mylène Tajan et al.   Nature Communications

CANTATA: Primary analysis of a global, randomized, placebo (Pbo)-controlled, double-blind trial of telaglenastat (CB-839) + cabozantinib versus Pbo + cabozantinib in advanced/metastatic renal cell carcinoma (mRCC) patients (pts) who progressed on immune checkpoint inhibitor (ICI) or anti-angiogenic therapies.

(2021) Nizar M. Tannir et al.   JOURNAL OF CLINICAL ONCOLOGY

Structure based discovery of novel hexokinase 2 inhibitors

(2020) Yang Liu et al.   BIOORGANIC CHEMISTRY

Role of monocarboxylate transporters in regulating metabolic homeostasis in the outer retina: Insight gained from cell‐specific Bsg deletion

(2020) John Y. S. Han et al.   FASEB JOURNAL

mTOR at the nexus of nutrition, growth, ageing and disease

(2020) Grace Y. Liu et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Lactate dehydrogenase inhibition synergizes with IL-21 to promote CD8+ T cell stemness and antitumor immunity

(2020) Dalton Hermans et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Dynamic Imaging of LDH Inhibition in Tumors Reveals Rapid In Vivo Metabolic Rewiring and Vulnerability to Combination Therapy

(2020) Nobu Oshima et al.   Cell Reports

Cryo-EM structures demonstrate human IMPDH2 filament assembly tunes allosteric regulation

(2020) Matthew C Johnson et al.   eLife

Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of a Liver‐Targeting Acetyl‐CoA Carboxylase Inhibitor (PF‐05221304): A Three‐Part Randomized Phase 1 Study

(2020) Arthur Bergman et al.   Clinical Pharmacology in Drug Development

Serine Catabolism Feeds NADH when Respiration Is Impaired

(2020) Lifeng Yang et al.   Cell Metabolism

SHMT inhibition is effective and synergizes with methotrexate in T-cell acute lymphoblastic leukemia

(2020) Juan C. García-Cañaveras et al.   LEUKEMIA

Repurposing leflunomide for relapsed/refractory multiple myeloma: a phase 1 study

(2020) Michael Rosenzweig et al.   LEUKEMIA & LYMPHOMA

Selective alanine transporter utilization creates a targetable metabolic niche in pancreatic cancer

(2020) Seth J Parker et al.   Cancer Discovery

Recent Advances in NAMPT Inhibitors: A Novel Immunotherapic Strategy

(2020) Ubaldina Galli et al.   Frontiers in Pharmacology

Structural Evidence for Isoform-Selective Allosteric Inhibition of Lactate Dehydrogenase A

(2020) Anders Friberg et al.   ACS Omega

In Vitro and In Vivo Efficacy of AZD3965 and Alpha-Cyano-4-Hydroxycinnamic Acid in the Murine 4T1 Breast Tumor Model

(2020) Xiaowen Guan et al.   AAPS Journal

Mitochondrial Metabolism as a Target for Cancer Therapy

(2020) Karthik Vasan et al.   Cell Metabolism

Monocarboxylate transporter 1 and 4 inhibitors as potential therapeutics for treating solid tumours: A review with structure-activity relationship insights

(2020) Sachin Puri et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Inhibitors of lipogenic enzymes as a potential therapy against cancer

(2020) Nicolás Montesdeoca et al.   FASEB JOURNAL

Targeting glutamine metabolism enhances tumor-specific immunity by modulating suppressive myeloid cells

(2020) Min-Hee Oh et al.   JOURNAL OF CLINICAL INVESTIGATION

Targeting Metabolism to Improve the Tumor Microenvironment for Cancer Immunotherapy

(2020) Jackie E. Bader et al.   MOLECULAR CELL

Mitochondrial ubiquinol oxidation is necessary for tumour growth

(2020) Inmaculada Martínez-Reyes et al.   NATURE

Limited Environmental Serine and Glycine Confer Brain Metastasis Sensitivity to PHGDH Inhibition

(2020) Bryan Ngo et al.   Cancer Discovery

Effects of a monocarboxylate transport 1 inhibitor, AZD3965, on retinal and visual function in the rat

(2020) Annette E. Allen et al.   BRITISH JOURNAL OF PHARMACOLOGY

Quantitative Analysis of the Physiological Contributions of Glucose to the TCA Cycle

(2020) Shiyu Liu et al.   Cell Metabolism

Pyrazole-Based Lactate Dehydrogenase Inhibitors with Optimized Cell Activity and Pharmacokinetic Properties

(2020) Ganesha Rai et al.   JOURNAL OF MEDICINAL CHEMISTRY

JPH203, a newly developed anti-cancer drug, shows a preincubation inhibitory effect on L-type amino acid transporter 1 function

(2020) Kentaro Okunushi et al.   JOURNAL OF PHARMACOLOGICAL SCIENCES

Selective Vulnerability to Pyrimidine Starvation in Hematologic Malignancies Revealed by AG-636, a Novel Clinical-Stage Inhibitor of Dihydroorotate Dehydrogenase

(2020) Gabrielle McDonald et al.   MOLECULAR CANCER THERAPEUTICS

Functional genomic landscape of cancer-intrinsic evasion of killing by T cells

(2020) Keith A. Lawson et al.   NATURE

Disturbed mitochondrial dynamics in CD8+ TILs reinforce T cell exhaustion

(2020) Yi-Ru Yu et al.   NATURE IMMUNOLOGY

A powerful drug combination strategy targeting glutamine addiction for the treatment of human liver cancer

(2020) Haojie Jin et al.   eLife

Potent human dihydroorotate dehydrogenase inhibitory activity of new quinoline-4-carboxylic acids derived from phenolic aldehydes: Synthesis, cytotoxicity, lipophilicity and molecular docking studies

(2020) Milena M. Petrović et al.   BIOORGANIC CHEMISTRY

Structural basis of human monocarboxylate transporter 1 inhibition by anti-cancer drug candidates

(2020) Nan Wang et al.   CELL

Determinants of Tissue-Specific Metabolic Adaptation of T Cells

(2020) Siva Karthik Varanasi et al.   Cell Metabolism

Functional Genomics In Vivo Reveal Metabolic Dependencies of Pancreatic Cancer Cells

(2020) Xiphias Ge Zhu et al.   Cell Metabolism

Functional Genomics Identifies Metabolic Vulnerabilities in Pancreatic Cancer

(2020) Douglas E. Biancur et al.   Cell Metabolism

In crystallo screening for proline analog inhibitors of the proline cycle enzyme PYCR1

(2020) Emily M. Christensen et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Leflunomide Suppresses the Growth of LKB1-Inactivated Tumors in the Immune-Competent Host and Attenuates Distant Cancer Metastasis

(2020) Rui Jin et al.   MOLECULAR CANCER THERAPEUTICS

Repurposing the Antidepressant Sertraline as SHMT Inhibitor to Suppress Serine/Glycine Synthesis–Addicted Breast Tumor Growth

(2020) Shauni Lien Geeraerts et al.   MOLECULAR CANCER THERAPEUTICS

IMU-838, a Developmental DHODH Inhibitor in Phase II for Autoimmune Disease, Shows Anti-SARS-CoV-2 and Broad-Spectrum Antiviral Efficacy In Vitro

(2020) Friedrich Hahn et al.   Viruses-Basel

Characteristics of the Tumor Microenvironment That Influence Immune Cell Functions: Hypoxia, Oxidative Stress, Metabolic Alterations

(2020) Ryan C. Augustin et al.   Cancers

Selective glutamine metabolism inhibition in tumor cells improves antitumor T lymphocyte activity in triple-negative breast cancer

(2020) Deanna N. Edwards et al.   JOURNAL OF CLINICAL INVESTIGATION

Novel selective hexokinase 2 inhibitor Benitrobenrazide blocks cancer cells growth by targeting glycolysis

(2020) Mengzhu Zheng et al.   PHARMACOLOGICAL RESEARCH

Suppression of hepatocellular carcinoma by mycophenolic acid in experimental models and in patients

(2019) Kan Chen et al.   TRANSPLANTATION

High-fructose corn syrup enhances intestinal tumor growth in mice

(2019) Marcus D. Goncalves et al.   SCIENCE

Safety and Efficacy of Bempedoic Acid to Reduce LDL Cholesterol

(2019) Kausik K. Ray et al.   NEW ENGLAND JOURNAL OF MEDICINE

Tumor-Targeted Delivery of 6-Diazo-5-oxo-l-norleucine (DON) Using Substituted Acetylated Lysine Prodrugs

(2019) Lukáš Tenora et al.   JOURNAL OF MEDICINAL CHEMISTRY

An HK2 antisense oligonucleotide induces synthetic lethality in HK1-HK2+ multiple myeloma

(2019) Shili Xu et al.   CANCER RESEARCH

Acyl-CoA-Binding Protein Drives Glioblastoma Tumorigenesis by Sustaining Fatty Acid Oxidation

(2019) Ceren Duman et al.   Cell Metabolism

Structural basis of inhibition of the human serine hydroxymethyltransferase SHMT 2 by antifolate drugs

(2019) Emma Scaletti et al.   FEBS LETTERS

Phase I trial of IACS-010759 (IACS), a potent, selective inhibitor of complex I of the mitochondrial electron transport chain, in patients (pts) with advanced solid tumors.

(2019) Timothy A Yap et al.   JOURNAL OF CLINICAL ONCOLOGY

An allosteric mechanism for potent inhibition of human ATP-citrate lyase

(2019) Jia Wei et al.   NATURE

The landscape of cancer cell line metabolism

(2019) Haoxin Li et al.   NATURE MEDICINE

Inhibition of 3-phosphoglycerate dehydrogenase (PHGDH) by indole amides abrogates de novo serine synthesis in cancer cells

(2019) Edouard Mullarky et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

A fragment-like approach to PYCR1 inhibition

(2019) Kirsty Milne et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Intracellular Trapping of the Selective Phosphoglycerate Dehydrogenase (PHGDH) Inhibitor BI-4924 Disrupts Serine Biosynthesis

(2019) Harald Weinstabl et al.   JOURNAL OF MEDICINAL CHEMISTRY

Novel pyrrolo[3,2-d]pyrimidine compounds target mitochondrial and cytosolic one-carbon metabolism with broad-spectrum antitumor efficacy

(2019) Aamod S. Dekhne et al.   MOLECULAR CANCER THERAPEUTICS

Targeting Mitochondrial Proline Dehydrogenase with a Suicide Inhibitor to Exploit Synthetic Lethal Interactions with p53 Upregulation and Glutaminase Inhibition

(2019) Gary K. Scott et al.   MOLECULAR CANCER THERAPEUTICS

Inhibition of ACSS2 for Treatment of Cancer and Neuropsychiatric Diseases

(2019) Robert B. Kargbo   ACS Medicinal Chemistry Letters

Targeting Glycolysis through Inhibition of Lactate Dehydrogenase Impairs Tumor Growth in Preclinical Models of Ewing Sarcoma

(2019) Choh Yeung et al.   CANCER RESEARCH

Hallmarks of Endothelial Cell Metabolism in Health and Disease

(2019) Xuri Li et al.   Cell Metabolism

The MYC Oncogene Cooperates with Sterol-Regulated Element-Binding Protein to Regulate Lipogenesis Essential for Neoplastic Growth

(2019) Arvin M. Gouw et al.   Cell Metabolism

A Phase III open-label trial to evaluate efficacy and safety of CPI-613 plus modified FOLFIRINOX (mFFX) versus FOLFIRINOX (FFX) in patients with metastatic adenocarcinoma of the pancreas

(2019) Philip A Philip et al.   Future Oncology

Devimistat in combination with high dose cytarabine and mitoxantrone compared with high dose cytarabine and mitoxantrone in older patients with relapsed/refractory acute myeloid leukemia: ARMADA 2000 Phase III study

(2019) Timothy S Pardee et al.   Future Oncology

Safety and Efficacy of Mitapivat in Pyruvate Kinase Deficiency

(2019) Rachael F. Grace et al.   NEW ENGLAND JOURNAL OF MEDICINE

GLS2 is protumorigenic in breast cancers

(2019) Marilia M. Dias et al.   ONCOGENE

Cellular Pharmacodynamics of a Novel Pyrrolo[3,2-d]pyrimidine Inhibitor Targeting Mitochondrial and Cytosolic One-Carbon Metabolism

(2019) Aamod S. Dekhne et al.   MOLECULAR PHARMACOLOGY

Glutamine blockade induces divergent metabolic programs to overcome tumor immune evasion

(2019) Robert D. Leone et al.   SCIENCE

Orally bioavailable glutamine antagonist prodrug JHU-083 penetrates mouse brain and suppresses the growth of MYC-driven medulloblastoma

(2019) Allison R. Hanaford et al.   Translational Oncology

Liver-Type Glutaminase GLS2 Is a Druggable Metabolic Node in Luminal-Subtype Breast Cancer

(2019) Michael J. Lukey et al.   Cell Reports

Metabolic Consequences of T-cell Costimulation in Anticancer Immunity

(2019) Alvaro Teijeira et al.   Cancer Immunology Research

Mechanism-Specific Pharmacodynamics of a Novel Complex-I Inhibitor Quantified by Imaging Reversal of Consumptive Hypoxia with [18F]FAZA PET In Vivo

(2019) Seth T. Gammon et al.   Cells

Regulation of Tumor Initiation by the Mitochondrial Pyruvate Carrier

(2019) Claire L. Bensard et al.   Cell Metabolism

Mitochondria in cancer metabolism, an organelle whose time has come?

(2018) Rebecca G. Anderson et al.   BIOCHIMICA ET BIOPHYSICA ACTA-REVIEWS ON CANCER

Discovery and optimization of piperazine-1-thiourea-based human phosphoglycerate dehydrogenase inhibitors

(2018) Jason M. Rohde et al.   BIOORGANIC & MEDICINAL CHEMISTRY

As Extracellular Glutamine Levels Decline, Asparagine Becomes an Essential Amino Acid

(2018) Natalya N. Pavlova et al.   Cell Metabolism

Increased Tumor Glycolysis Characterizes Immune Resistance to Adoptive T Cell Therapy

(2018) Tina Cascone et al.   Cell Metabolism

A Phase I Study of CPI-613 in Combination with High-Dose Cytarabine and Mitoxantrone for Relapsed or Refractory Acute Myeloid Leukemia

(2018) Timothy S. Pardee et al.   CLINICAL CANCER RESEARCH

Targeting cancer metabolism to develop human lactate dehydrogenase ( h LDH)5 inhibitors

(2018) Shao-Lin Zhang et al.   DRUG DISCOVERY TODAY

Serine Catabolism by SHMT2 Is Required for Proper Mitochondrial Translation Initiation and Maintenance of Formylmethionyl-tRNAs

(2018) Denise R. Minton et al.   MOLECULAR CELL

Aspartate is a limiting metabolite for cancer cell proliferation under hypoxia and in tumours

(2018) Javier Garcia-Bermudez et al.   NATURE CELL BIOLOGY

Aspartate is an endogenous metabolic limitation for tumour growth

(2018) Lucas B. Sullivan et al.   NATURE CELL BIOLOGY

An inhibitor of oxidative phosphorylation exploits cancer vulnerability

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

Understanding the tumor immune microenvironment (TIME) for effective therapy

(2018) Mikhail Binnewies et al.   NATURE MEDICINE

Pharmacological blockade of ASCT2-dependent glutamine transport leads to antitumor efficacy in preclinical models

(2018) Michael L Schulte et al.   NATURE MEDICINE

Therapeutic potential of CPI-613 for targeting tumorous mitochondrial energy metabolism and inhibiting autophagy in clear cell sarcoma

(2018) Yuki Egawa et al.   PLoS One

A major chromatin regulator determines resistance of tumor cells to T cell–mediated killing

(2018) Deng Pan et al.   SCIENCE

Exploiting Metabolic Vulnerabilities of Cancer with Precision and Accuracy

(2018) Adam J. Wolpaw et al.   TRENDS IN CELL BIOLOGY

Preclinical evaluation of novel fatty acid synthase inhibitors in primary colorectal cancer cells and a patient-derived xenograft model of colorectal cancer

(2018) Yekaterina Y. Zaytseva et al.   Oncotarget

Early TCR Signaling Induces Rapid Aerobic Glycolysis Enabling Distinct Acute T Cell Effector Functions

(2018) Ashley V. Menk et al.   Cell Reports

Disruption of Amino Acid Homeostasis by Novel ASCT2 Inhibitors Involves Multiple Targets

(2018) Angelika Bröer et al.   Frontiers in Pharmacology

ATP citrate lyase (ACLY) inhibitors: An anti-cancer strategy at the crossroads of glucose and lipid metabolism

(2018) Carlotta Granchi   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of novel human inosine 5′-monophosphate dehydrogenase 2 (hIMPDH2) inhibitors as potential anticancer agents

(2018) Chetan P. Shah et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Double genetic disruption of lactate dehydrogenase A and B is required to ablate the ‘Warburg effect’ restricting tumor growth to oxidative metabolism

(2018) Maša Ždralević et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

We're Not “DON” Yet: Optimal Dosing and Prodrug Delivery of6-Diazo-5-oxo-L-norleucine

(2018) Kathryn M. Lemberg et al.   MOLECULAR CANCER THERAPEUTICS

ACSS2 promotes systemic fat storage and utilization through selective regulation of genes involved in lipid metabolism

(2018) Zhiguang Huang et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Distinct Regulation of Th17 and Th1 Cell Differentiation by Glutaminase-Dependent Metabolism

(2018) Marc O. Johnson et al.   CELL

Quantitative Analysis of the Whole-Body Metabolic Fate of Branched-Chain Amino Acids

(2018) Michael D. Neinast et al.   Cell Metabolism

Inhibiting Stearoyl-CoA Desaturase Ameliorates α-Synuclein Cytotoxicity

(2018) Benjamin M. Vincent et al.   Cell Reports

Potent immunosuppressive effects of the oncometabolite R-2-hydroxyglutarate

(2018) Lorenzo Galluzzi et al.   OncoImmunology

Discovery and Optimization of Potent, Cell-Active Pyrazole-Based Inhibitors of Lactate Dehydrogenase (LDH)

(2017) Ganesha Rai et al.   JOURNAL OF MEDICINAL CHEMISTRY

α-Ketothioamide Derivatives: A Promising Tool to Interrogate Phosphoglycerate Dehydrogenase (PHGDH)

(2017) Séverine Ravez et al.   JOURNAL OF MEDICINAL CHEMISTRY

Safety and tolerability of the first-in-class agent CPI-613 in combination with modified FOLFIRINOX in patients with metastatic pancreatic cancer: a single-centre, open-label, dose-escalation, phase 1 trial

(2017) Angela Alistar et al.   LANCET ONCOLOGY

Activation of the Unfolded Protein Response by Lipid Bilayer Stress

(2017) Kristina Halbleib et al.   MOLECULAR CELL

Modulating the therapeutic response of tumours to dietary serine and glycine starvation

(2017) Oliver D. K. Maddocks et al.   NATURE

Glucose feeds the TCA cycle via circulating lactate

(2017) Sheng Hui et al.   NATURE

Keap1 loss promotes Kras-driven lung cancer and results in dependence on glutaminolysis

(2017) Rodrigo Romero et al.   NATURE MEDICINE

Human SHMT inhibitors reveal defective glycine import as a targetable metabolic vulnerability of diffuse large B-cell lymphoma

(2017) Gregory S. Ducker et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Metabolic Interactions in the Tumor Microenvironment

(2017) Costas A. Lyssiotis et al.   TRENDS IN CELL BIOLOGY

Pre-clinical pharmacology of AZD3965, a selective inhibitor of MCT1: DLBCL, NHL and Burkitt’s lymphoma anti-tumor activity

(2017) Nicola J. Curtis et al.   Oncotarget

FASN Inhibition and Taxane Treatment Combine to Enhance Anti-tumor Efficacy in Diverse Xenograft Tumor Models through Disruption of Tubulin Palmitoylation and Microtubule Organization and FASN Inhibition-Mediated Effects on Oncogenic Signaling and Gene Expression

(2017) Timothy S. Heuer et al.   EBioMedicine

2-Amino-4-bis(aryloxybenzyl)aminobutanoic acids: A novel scaffold for inhibition of ASCT2-mediated glutamine transport

(2016) Michael L. Schulte et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

mTORC1-Dependent Metabolic Reprogramming Underlies Escape from Glycolysis Addiction in Cancer Cells

(2016) Raju V. Pusapati et al.   CANCER CELL

Identification and Optimization of the First Highly Selective GLUT1 Inhibitor BAY-876

(2016) Holger Siebeneicher et al.   ChemMedChem

Discovery of 6-Diazo-5-oxo-l-norleucine (DON) Prodrugs with Enhanced CSF Delivery in Monkeys: A Potential Treatment for Glioblastoma

(2016) Rana Rais et al.   JOURNAL OF MEDICINAL CHEMISTRY

Pancreatic stellate cells support tumour metabolism through autophagic alanine secretion

(2016) Cristovão M. Sousa et al.   NATURE

A PHGDH inhibitor reveals coordination of serine synthesis and one-carbon unit fate

(2016) Michael E Pacold et al.   Nature Chemical Biology

SF2312 is a natural phosphonate inhibitor of enolase

(2016) Paul G Leonard et al.   Nature Chemical Biology

Metabolic plasticity underpins innate and acquired resistance to LDHA inhibition

(2016) Aaron Boudreau et al.   Nature Chemical Biology

Inhibition of acetyl-CoA carboxylase suppresses fatty acid synthesis and tumor growth of non-small-cell lung cancer in preclinical models

(2016) Robert U Svensson et al.   NATURE MEDICINE

Inhibition of fatty acid oxidation as a therapy for MYC-overexpressing triple-negative breast cancer

(2016) Roman Camarda et al.   NATURE MEDICINE

Identification of a small molecule inhibitor of 3-phosphoglycerate dehydrogenase to target serine biosynthesis in cancers

(2016) Edouard Mullarky et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Acetyl-CoA carboxylase inhibition by ND-630 reduces hepatic steatosis, improves insulin sensitivity, and modulates dyslipidemia in rats

(2016) Geraldine Harriman et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Tissue of origin dictates branched-chain amino acid metabolism in mutant Kras-driven cancers

(2016) J. R. Mayers et al.   SCIENCE

Pyruvate and Metabolic Flexibility: Illuminating a Path Toward Selective Cancer Therapies

(2016) Kristofor A. Olson et al.   TRENDS IN BIOCHEMICAL SCIENCES

Discovery of a Novel 2,6-Disubstituted Glucosamine Series of Potent and Selective Hexokinase 2 Inhibitors

(2016) Hong Lin et al.   ACS Medicinal Chemistry Letters

Liver-specific ATP-citrate lyase inhibition by bempedoic acid decreases LDL-C and attenuates atherosclerosis

(2016) Stephen L. Pinkosky et al.   Nature Communications

Targeting Cancer Metabolism: Dietary and Pharmacologic Interventions

(2016) C. Vernieri et al.   Cancer Discovery

Structural basis for exploring the allosteric inhibition of human kidney type glutaminase

(2016) Sarath Ramachandran et al.   Oncotarget

ATP-Citrate Lyase Controls a Glucose-to-Acetate Metabolic Switch

(2016) Steven Zhao et al.   Cell Reports

Suppressive effects of tumor cell-derived 5′-deoxy-5′-methylthioadenosine on human T cells

(2016) Frederik C. Henrich et al.   OncoImmunology

Fundamentals of cancer metabolism

(2016) R. J. DeBerardinis et al.   Science Advances

Acetyl-CoA Synthetase 2 Promotes Acetate Utilization and Maintains Cancer Cell Growth under Metabolic Stress

(2015) Zachary T. Schug et al.   CANCER CELL

Therapeutic Targeting of the Warburg Effect in Pancreatic Cancer Relies on an Absence of p53 Function

(2015) N. V. Rajeshkumar et al.   CANCER RESEARCH

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

(2015) Kıvanç Birsoy et al.   CELL

A Human Interactome in Three Quantitative Dimensions Organized by Stoichiometries and Abundances

(2015) Marco Y. Hein et al.   CELL

Screening and In Vitro Testing of Antifolate Inhibitors of Human Cytosolic Serine Hydroxymethyltransferase

(2015) Alessandro Paiardini et al.   ChemMedChem

New Strategies in Renal Cell Carcinoma: Targeting the Genetic and Metabolic Basis of Disease

(2015) R. Srinivasan et al.   CLINICAL CANCER RESEARCH

Targeted inhibition of tumor-specific glutaminase diminishes cell-autonomous tumorigenesis

(2015) Yan Xiang et al.   JOURNAL OF CLINICAL INVESTIGATION

X-ray structure of a mammalian stearoyl-CoA desaturase

(2015) Yonghong Bai et al.   NATURE

Crystal structure of human stearoyl–coenzyme A desaturase in complex with substrate

(2015) Hui Wang et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

MYC, Metabolism, and Cancer

(2015) Z. E. Stine et al.   Cancer Discovery

Crystal structure of human stearoyl–coenzyme A desaturase in complex with substrate

(2015) Hui Wang et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

NAMPT Is the Cellular Target of STF-31-Like Small-Molecule Probes

(2014) Drew J. Adams et al.   ACS Chemical Biology

Effects of metformin and other biguanides on oxidative phosphorylation in mitochondria

(2014) Hannah R. Bridges et al.   BIOCHEMICAL JOURNAL

Acetate Dependence of Tumors

(2014) Sarah A. Comerford et al.   CELL

Targeting Lactate Dehydrogenase-A Inhibits Tumorigenesis and Tumor Progression in Mouse Models of Lung Cancer and Impacts Tumor-Initiating Cells

(2014) Han Xie et al.   Cell Metabolism

A Phase I Study of the First-in-Class Antimitochondrial Metabolism Agent, CPI-613, in Patients with Advanced Hematologic Malignancies

(2014) T. S. Pardee et al.   CLINICAL CANCER RESEARCH

Antitumor Activity of the Glutaminase Inhibitor CB-839 in Triple-Negative Breast Cancer

(2014) M. I. Gross et al.   MOLECULAR CANCER THERAPEUTICS

A Role for the Mitochondrial Pyruvate Carrier as a Repressor of the Warburg Effect and Colon Cancer Cell Growth

(2014) John C. Schell et al.   MOLECULAR CELL

The gut microbiota, bacterial metabolites and colorectal cancer

(2014) Petra Louis et al.   NATURE REVIEWS MICROBIOLOGY

Hexokinase 2 Is Required for Tumor Initiation and Maintenance and Its Systemic Deletion Is Therapeutic in Mouse Models of Cancer

(2013) Krushna C. Patra et al.   CANCER CELL

Blocking Lactate Export by Inhibiting the Myc Target MCT1 Disables Glycolysis and Glutathione Synthesis

(2013) J. R. Doherty et al.   CANCER RESEARCH

PKM2 Isoform-Specific Deletion Reveals a Differential Requirement for Pyruvate Kinase in Tumor Cells

(2013) William J. Israelsen et al.   CELL

Opportunities and Challenges in Developing Stearoyl-Coenzyme A Desaturase-1 Inhibitors as Novel Therapeutics for Human Disease

(2013) Zaihui Zhang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Carnitine-Acyltransferase System Inhibition, Cancer Cell Death, and Prevention of Myc-Induced Lymphomagenesis

(2013) Annalisa Pacilli et al.   JNCI-Journal of the National Cancer Institute

The Metabolic Profile of Tumors Depends on Both the Responsible Genetic Lesion and Tissue Type

(2012) Mariia O. Yuneva et al.   Cell Metabolism

Glucose-Independent Glutamine Metabolism via TCA Cycling for Proliferation and Survival in B Cells

(2012) Anne Le et al.   Cell Metabolism

AMP-activated protein kinase and ATP-citrate lyase are two distinct molecular targets for ETC-1002, a novel small molecule regulator of lipid and carbohydrate metabolism

(2012) Stephen L. Pinkosky et al.   JOURNAL OF LIPID RESEARCH

Passenger deletions generate therapeutic vulnerabilities in cancer

(2012) Florian L. Muller et al.   NATURE

Serine starvation induces stress and p53-dependent metabolic remodelling in cancer cells

(2012) Oliver D. K. Maddocks et al.   NATURE

Reprogramming of proline and glutamine metabolism contributes to the proliferative and metabolic responses regulated by oncogenic transcription factor c-MYC

(2012) W. Liu et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Structural basis for the allosteric inhibitory mechanism of human kidney-type glutaminase (KGA) and its regulation by Raf-Mek-Erk signaling in cancer cell metabolism

(2012) K. Thangavelu et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Targeted therapy with fatty acid synthase inhibitors in a human prostate carcinoma LNCaP/tk-luc-bearing animal model

(2012) H-W Chen et al.   PROSTATE CANCER AND PROSTATIC DISEASES

The cBio Cancer Genomics Portal: An Open Platform for Exploring Multidimensional Cancer Genomics Data: Figure 1.

(2012) Ethan Cerami et al.   Cancer Discovery

Targeting Mitochondrial Glutaminase Activity Inhibits Oncogenic Transformation

(2010) Jian-Bin Wang et al.   CANCER CELL

Inhibitors of Lactate Dehydrogenase Isoforms and their Therapeutic Potentials

(2010) C. Granchi et al.   CURRENT MEDICINAL CHEMISTRY

Recent Advances in Stearoyl-CoA Desaturase 1 Inhibitors for Dyslipidemia and Obesity

(2010) Gang Liu   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Glutaminase 2, a novel p53 target gene regulating energy metabolism and antioxidant function

(2010) W. Hu et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Inhibition of lactate dehydrogenase A induces oxidative stress and inhibits tumor progression

(2010) A. Le et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

l-Type amino acid transporter 1 inhibitors inhibit tumor cell growth

(2009) Koji Oda et al.   CANCER SCIENCE

c-Myc suppression of miR-23a/b enhances mitochondrial glutaminase expression and glutamine metabolism

(2009) Ping Gao et al.   NATURE

Understanding the Warburg Effect: The Metabolic Requirements of Cell Proliferation

(2009) M. G. Vander Heiden et al.   SCIENCE