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

Benzylserine inhibits breast cancer cell growth by disrupting intracellular amino acid homeostasis and triggering amino acid response pathways

(2018) Michelle van Geldermalsen et al.   BMC CANCER

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

(2018) Michael L Schulte et al.   NATURE MEDICINE

Cryo-EM structure of the human neutral amino acid transporter ASCT2

(2018) Alisa A. Garaeva et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Structural characterisation reveals insights into substrate recognition by the glutamine transporter ASCT2/SLC1A5

(2018) Amanda J Scopelliti et al.   Nature Communications

Cryo-EM structure of the human neutral amino acid transporter ASCT2

(2018) Alisa A. Garaeva et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Homology Modeling Informs Ligand Discovery for the Glutamine Transporter ASCT2

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

Structure and allosteric inhibition of excitatory amino acid transporter 1

(2017) Juan C. Canul-Tec et al.   NATURE

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

β-Sulfonamido Functionalized Aspartate Analogues as Excitatory Amino Acid Transporter Inhibitors: Distinct Subtype Selectivity Profiles Arising from Subtle Structural Differences

(2016) Jacob C. Hansen et al.   JOURNAL OF MEDICINAL CHEMISTRY

2-Substituted Nγ-glutamylanilides as novel probes of ASCT2 with improved potency

(2015) Michael L. Schulte et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Cysteine is not a substrate but a specific modulator of human ASCT2 (SLC1A5) transporter

(2015) Mariafrancesca Scalise et al.   FEBS LETTERS

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

(2015) Qian Wang et al.   JOURNAL OF PATHOLOGY

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

(2015) M van Geldermalsen et al.   ONCOGENE

Ligand Discovery for the Alanine-Serine-Cysteine Transporter (ASCT2, SLC1A5) from Homology Modeling and Virtual Screening

(2015) Claire Colas et al.   PLoS Computational Biology

Targeting glutamine transport to suppress melanoma cell growth

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

Voltage-dependent processes in the electroneutral amino acid exchanger ASCT2

(2013) Catherine B. Zander et al.   JOURNAL OF GENERAL PHYSIOLOGY

The expression of glutamine-metabolism-related proteins in breast phyllodes tumors

(2013) Sewha Kim et al.   TUMOR BIOLOGY

How cancer metabolism is tuned for proliferation and vulnerable to disruption

(2012) Almut Schulze et al.   NATURE

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