Amino Acid Transporters as Targets for Cancer Therapy: Why, Where, When, and How

Down-regulation of IDH2 sensitizes cancer cells to erastin-induced ferroptosis

(2020) Hyunjin Kim et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Amino acids in cancer

(2020) Elizabeth L. Lieu et al.   EXPERIMENTAL AND MOLECULAR MEDICINE

Novel Chemical Scaffolds to Inhibit the Neutral Amino Acid Transporter B0AT1 (SLC6A19), a Potential Target to Treat Metabolic Diseases

(2020) Aditya Yadav et al.   Frontiers in Pharmacology

Cysteine depletion induces pancreatic tumor ferroptosis in mice

(2020) Michael A. Badgley et al.   SCIENCE

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

(2020) Seth J Parker et al.   Cancer Discovery

Nutritional Exchanges Within Tumor Microenvironment: Impact for Cancer Aggressiveness

(2020) Giuseppina Comito et al.   Frontiers in Oncology

Cysteine Depletion, a Key Action to Challenge Cancer Cells to Ferroptotic Cell Death

(2020) Boutaina Daher et al.   Frontiers in Oncology

Ablation of the ASCT2 (SLC1A5) gene encoding a neutral amino acid transporter reveals transporter plasticity and redundancy in cancer cells

(2019) Angelika Bröer et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

The coordinated action of VCP/p97 and GCN2 regulates cancer cell metabolism and proteostasis during nutrient limitation

(2019) Katarzyna Parzych et al.   ONCOGENE

γ-Glutamyltransferase enzyme activity of cancer cells modulates L-γ-glutamyl-p-nitroanilide (GPNA) cytotoxicity

(2019) Alessandro Corti et al.   Scientific Reports

Novel alanine serine cysteine transporter 2 (ASCT2) inhibitors based on sulfonamide and sulfonic acid ester scaffolds

(2019) Elias Ndaru et al.   JOURNAL OF GENERAL PHYSIOLOGY

Prioritization of cancer therapeutic targets using CRISPR–Cas9 screens

(2019) Fiona M. Behan et al.   NATURE

Cystine/glutamate antiporter xCT (SLC7A11) facilitates oncogenic RAS transformation by preserving intracellular redox balance

(2019) Jonathan K. M. Lim et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The Non-Essential Amino Acid Cysteine Becomes Essential for Tumor Proliferation and Survival

(2019) Joseph A. Combs et al.   Cancers

CDK7 is a component of the integrated stress response regulating SNAT2 (SLC38A2)/System A adaptation in response to cellular amino acid deprivation

(2019) Clare Stretton et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH

Genetic Ablation of the Cystine Transporter xCT in PDAC Cells Inhibits mTORC1, Growth, Survival, and Tumor Formation via Nutrient and Oxidative Stresses

(2019) Boutaina Daher et al.   CANCER RESEARCH

A Physiological Function for Ferroptosis in Tumor Suppression by the Immune System

(2019) Brent R. Stockwell et al.   Cell Metabolism

Molecular mechanisms of ferroptosis and its role in cancer therapy

(2019) Tao Xu et al.   JOURNAL OF CELLULAR AND MOLECULAR MEDICINE

New aspects of amino acid metabolism in cancer

(2019) Lisa Vettore et al.   BRITISH JOURNAL OF CANCER

A Variant of SLC1A5 Is a Mitochondrial Glutamine Transporter for Metabolic Reprogramming in Cancer Cells

(2019) Hee Chan Yoo et al.   Cell Metabolism

The role of ASCT2 in cancer: A review

(2018) Yang Liu et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Insights into the Structure, Function, and Ligand Discovery of the Large Neutral Amino Acid Transporter 1, LAT1

(2018) Natesh Singh et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Targeted Suppression and Knockout of ASCT2 or LAT1 in Epithelial and Mesenchymal Human Liver Cancer Cells Fail to Inhibit Growth

(2018) Paige Bothwell et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

The glutamine transporter ASCT2 (SLC1A5) promotes tumor growth independently of the amino acid transporter LAT1 (SLC7A5)

(2018) Yann Cormerais et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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

(2018) Michael L Schulte et al.   NATURE MEDICINE

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

(2018) Angelika Bröer et al.   Frontiers in Pharmacology

The Human SLC7A5 (LAT1): The Intriguing Histidine/Large Neutral Amino Acid Transporter and Its Relevance to Human Health

(2018) Mariafrancesca Scalise et al.   Frontiers in Chemistry

The Development of the Concept of Ferroptosis

(2018) Tal Hirschhorn et al.   FREE RADICAL BIOLOGY AND MEDICINE

Inhibition of GCN2 sensitizes ASNS-low cancer cells to asparaginase by disrupting the amino acid response

(2018) Akito Nakamura et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Amino acid transporters revisited: New views in health and disease

(2018) Palanivel Kandasamy et al.   TRENDS IN BIOCHEMICAL SCIENCES

Homology Modeling Informs Ligand Discovery for the Glutamine Transporter ASCT2

(2018) Rachel-Ann A. Garibsingh et al.   Frontiers in Chemistry

Spotlight on Bortezomib: potential in the treatment of hepatocellular carcinoma

(2018) I-Tao Huang et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

A genome-wide Drosophila epithelial tumorigenesis screen identifies Tetraspanin 29Fb as an evolutionarily conserved suppressor of Ras-driven cancer

(2018) Tamara Zoranovic et al.   PLoS Genetics

Identification and Characterization of Inhibitors of a Neutral Amino Acid Transporter, SLC6A19, Using Two Functional Cell-Based Assays

(2018) Sanjay J. Danthi et al.   SLAS Discovery

The potential of inhibiting glutamine uptake as a therapeutic target for multiple myeloma

(2017) Nicola Giuliani et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

Clinical Role of ASCT2 (SLC1A5) in KRAS-Mutated Colorectal Cancer

(2017) Kosuke Toda et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Asparagine synthetase: Function, structure, and role in disease

(2017) Carrie L. Lomelino et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Pathways of cellular proteostasis in aging and disease

(2017) Courtney L. Klaips et al.   JOURNAL OF CELL BIOLOGY

Dynamin inhibitors block activation of mTORC1 by amino acids independently of dynamin

(2017) Avinash Persaud et al.   JOURNAL OF CELL SCIENCE

Hostile takeover: how tumours hijack pre-existing vascular environments to thrive

(2017) Frank Winkler   JOURNAL OF PATHOLOGY

Structure-activity relationship of a novel series of inhibitors for cancer type transporter L-type amino acid transporter 1 (LAT1)

(2017) Pornparn Kongpracha et al.   JOURNAL OF PHARMACOLOGICAL SCIENCES

Circulating and disseminated tumor cells: harbingers or initiators of metastasis?

(2017) Arko Dasgupta et al.   Molecular Oncology

Genome-wide in vivo screen identifies novel host regulators of metastatic colonization

(2017) Louise van der Weyden et al.   NATURE

Nutrient acquisition strategies of mammalian cells

(2017) Wilhelm Palm et al.   NATURE

Inhibiting the system xC−/glutathione axis selectively targets cancers with mutant-p53 accumulation

(2017) David S. Liu et al.   Nature Communications

Arginine auxotrophic gene signature in paediatric sarcomas and brain tumours provides a viable target for arginine depletion therapies

(2017) Ashley Vardon et al.   Oncotarget

Environmental cystine drives glutamine anaplerosis and sensitizes cancer cells to glutaminase inhibition

(2017) Alexander Muir et al.   eLife

Reconstitution of T Cell Proliferation under Arginine Limitation: Activated Human T Cells Take Up Citrulline via L-Type Amino Acid Transporter 1 and Use It to Regenerate Arginine after Induction of Argininosuccinate Synthase Expression

(2017) Anke Werner et al.   Frontiers in Immunology

Systematic high-content genome-wide RNAi screens of endothelial cell migration and morphology

(2017) Steven P. Williams et al.   Scientific Data

Genetic Disruption of the Multifunctional CD98/LAT1 Complex Demonstrates the Key Role of Essential Amino Acid Transport in the Control of mTORC1 and Tumor Growth

(2016) Y. Cormerais et al.   CANCER RESEARCH

Deletion of Amino Acid Transporter ASCT2 (SLC1A5) Reveals an Essential Role for Transporters SNAT1 (SLC38A1) and SNAT2 (SLC38A2) to Sustain Glutaminolysis in Cancer Cells

(2016) Angelika Bröer et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

A Selective and Slowly Reversible Inhibitor of l-Type Amino Acid Transporter 1 (LAT1) Potentiates Antiproliferative Drug Efficacy in Cancer Cells

(2016) Kristiina M. Huttunen et al.   JOURNAL OF MEDICINAL CHEMISTRY

A novel Na+-Independent alanine-serine-cysteine transporter 1 inhibitor inhibits both influx and efflux of D-Serine

(2016) Katsuya Sakimura et al.   JOURNAL OF NEUROSCIENCE RESEARCH

Asparagine promotes cancer cell proliferation through use as an amino acid exchange factor

(2016) Abigail S. Krall et al.   Nature Communications

Temozolomide toxicity operates in a xCT/SLC7a11 dependent manner and is fostered by ferroptosis

(2016) Tina Sehm et al.   Oncotarget

Fundamentals of cancer metabolism

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

High-Resolution CRISPR Screens Reveal Fitness Genes and Genotype-Specific Cancer Liabilities

(2015) Traver Hart et al.   CELL

Autophagy in cellular metabolism and cancer

(2015) Xuejun Jiang et al.   JOURNAL OF CLINICAL INVESTIGATION

Targeting ASCT2-mediated glutamine uptake blocks prostate cancer growth and tumour development

(2015) Qian Wang et al.   JOURNAL OF PATHOLOGY

Glutaminolysis and Transferrin Regulate Ferroptosis

(2015) Minghui Gao et al.   MOLECULAR CELL

ASCT2/SLC1A5 controls glutamine uptake and tumour growth in triple-negative basal-like breast cancer

(2015) M van Geldermalsen et al.   ONCOGENE

Identification and characterization of essential genes in the human genome

(2015) T. Wang et al.   SCIENCE

Famine versus feast: understanding the metabolism of tumors in vivo

(2015) Jared R. Mayers et al.   TRENDS IN BIOCHEMICAL SCIENCES

Glutamate and asparagine cataplerosis underlie glutamine addiction in melanoma

(2015) Boris Ratnikov et al.   Oncotarget

Monoterpene Glycoside ESK246 from Pittosporum Targets LAT3 Amino Acid Transport and Prostate Cancer Cell Growth

(2014) Qian Wang et al.   ACS Chemical Biology

Nimesulide binding site in the B0AT1 (SLC6A19) amino acid transporter. Mechanism of inhibition revealed by proteoliposome transport assay and molecular modelling

(2014) Lorena Pochini et al.   BIOCHEMICAL PHARMACOLOGY

Novel inhibitors of the high-affinity l-proline transporter as potential therapeutic agents for the treatment of cognitive disorders

(2014) G. Greg Zipp et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Targeting glutamine transport to suppress melanoma cell growth

(2014) Qian Wang et al.   INTERNATIONAL JOURNAL OF CANCER

Asparagine Plays a Critical Role in Regulating Cellular Adaptation to Glutamine Depletion

(2014) Ji Zhang et al.   MOLECULAR CELL

Pharmacological inhibition of cystine–glutamate exchange induces endoplasmic reticulum stress and ferroptosis

(2014) Scott J Dixon et al.   eLife

Membrane transporters for the special amino acid glutamine: structure/function relationships and relevance to human health

(2014) Lorena Pochini et al.   Frontiers in Chemistry

Sertraline inhibits the transport of PAT1 substratesin vivoandin vitro

(2013) C U Nielsen et al.   BRITISH JOURNAL OF PHARMACOLOGY

In vitroCharacterization of a small molecule inhibitor of the alanine serine cysteine transporter -1 (SLC7A10)

(2013) Jeffrey M. Brown et al.   JOURNAL OF NEUROCHEMISTRY

Tryptophan Catabolism in Cancer: Beyond IDO and Tryptophan Depletion

(2012) M. Platten et al.   CANCER RESEARCH

SLC1A5 Mediates Glutamine Transport Required for Lung Cancer Cell Growth and Survival

(2012) M. Hassanein et al.   CLINICAL CANCER RESEARCH

Systematic identification of genomic markers of drug sensitivity in cancer cells

(2012) Mathew J. Garnett et al.   NATURE

The Cancer Cell Line Encyclopedia enables predictive modelling of anticancer drug sensitivity

(2012) Jordi Barretina et al.   NATURE

Inactivation of the glutamine/amino acid transporter ASCT2 by 1,2,3-dithiazoles: proteoliposomes as a tool to gain insights in the molecular mechanism of action and of antitumor activity

(2012) Francesca Oppedisano et al.   TOXICOLOGY AND APPLIED PHARMACOLOGY

Metabolism and Pharmacokinetic Studies of JPH203, an L-Amino Acid Transporter 1 (LAT1) Selective Compound

(2011) Michael F. Wempe et al.   Drug Metabolism and Pharmacokinetics

SLC6A14 (ATB0,+) Protein, a Highly Concentrative and Broad Specific Amino Acid Transporter, Is a Novel and Effective Drug Target for Treatment of Estrogen Receptor-positive Breast Cancer

(2011) Senthil Karunakaran et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Lipoprotein Lipase Links Dietary Fat to Solid Tumor Cell Proliferation

(2011) N. B. Kuemmerle et al.   MOLECULAR CANCER THERAPEUTICS

Essential Gene Profiles in Breast, Pancreatic, and Ovarian Cancer Cells

(2011) Richard Marcotte et al.   Cancer Discovery

The GCN2-ATF4 pathway is critical for tumour cell survival and proliferation in response to nutrient deprivation

(2010) Jiangbin Ye et al.   EMBO JOURNAL

Selective GlyT1 Inhibitors: Discovery of [4-(3-Fluoro-5-trifluoromethylpyridin-2-yl)piperazin-1-yl][5-methanesulfonyl-2-((S)-2,2,2-trifluoro-1-methylethoxy)phenyl]methanone (RG1678), a Promising Novel Medicine To Treat Schizophrenia

(2010) Emmanuel Pinard et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure−Activity Relationship Study of First Selective Inhibitor of Excitatory Amino Acid Transporter Subtype 1: 2-Amino-4-(4-methoxyphenyl)-7-(naphthalen-1-yl)-5-oxo-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile (UCPH-101)

(2010) Mette N. Erichsen et al.   JOURNAL OF MEDICINAL CHEMISTRY

Identification and evaluation of [11C]GSK931145 as a novel ligand for imaging the type 1 glycine transporter with positron emission tomography

(2010) J. Passchier et al.   SYNAPSE

Glutamine addiction: a new therapeutic target in cancer

(2010) David R. Wise et al.   TRENDS IN BIOCHEMICAL SCIENCES

Bidirectional Transport of Amino Acids Regulates mTOR and Autophagy

(2009) Paul Nicklin et al.   CELL

Discovery and characterization of potent small molecule inhibitors of the high affinity proline transporter

(2009) Xuan-Chuan Yu et al.   NEUROSCIENCE LETTERS

Interaction of tryptophan derivatives with SLC6A14 (ATB0,+) reveals the potential of the transporter as a drug target for cancer chemotherapy

(2008) Senthil Karunakaran et al.   BIOCHEMICAL JOURNAL

Neurochemical and behavioral profiling of the selective GlyT1 inhibitors ALX5407 and LY2365109 indicate a preferential action in caudal vs. cortical brain areas

(2008) Kenneth W. Perry et al.   NEUROPHARMACOLOGY

Disruption of xCT inhibits cancer cell metastasis via the caveolin-1/β-catenin pathway

(2008) R-S Chen et al.   ONCOGENE

Characterization of SSR103800, a selective inhibitor of the glycine transporter-1 in models predictive of therapeutic activity in schizophrenia☆

(2008) D BOULAY et al.   PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR

Highly parallel identification of essential genes in cancer cells

(2008) B. Luo et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA