Cargando…

Homology Modeling Informs Ligand Discovery for the Glutamine Transporter ASCT2

The Alanine-Serine-Cysteine transporter (SLC1A5, ASCT2), is a neutral amino acid exchanger involved in the intracellular homeostasis of amino acids in peripheral tissues. Given its role in supplying glutamine to rapidly proliferating cancer cells in several tumor types such as triple-negative breast...

Descripción completa

Detalles Bibliográficos
Autores principales:	Garibsingh, Rachel-Ann A., Otte, Nicholas J., Ndaru, Elias, Colas, Claire, Grewer, Christof, Holst, Jeff, Schlessinger, Avner
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	Frontiers Media S.A. 2018
Materias:	Chemistry
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6066518/ https://www.ncbi.nlm.nih.gov/pubmed/30137742 http://dx.doi.org/10.3389/fchem.2018.00279

Ejemplares similares

Ligand Discovery for the Alanine-Serine-Cysteine Transporter (ASCT2, SLC1A5) from Homology Modeling and Virtual Screening
por: Colas, Claire, et al.
Publicado: (2015)

Novel alanine serine cysteine transporter 2 (ASCT2) inhibitors based on sulfonamide and sulfonic acid ester scaffolds
por: Ndaru, Elias, et al.
Publicado: (2019)

Rational design of ASCT2 inhibitors using an integrated experimental-computational approach
por: Garibsingh, Rachel-Ann A., et al.
Publicado: (2021)

Functional and Kinetic Comparison of Alanine Cysteine Serine Transporters ASCT1 and ASCT2
por: Wang, Jiali, et al.
Publicado: (2022)

Conserved allosteric inhibition mechanism in SLC1 transporters
por: Dong, Yang, et al.
Publicado: (2023)

Pre-steady-state Kinetic Analysis of Amino Acid Transporter SLC6A14 Reveals Rapid Turnover Rate and Substrate Translocation
por: Shi, Yueyue, et al.
Publicado: (2021)

ASCT2 regulates glutamine uptake and cell growth in endometrial carcinoma
por: Marshall, A D, et al.
Publicado: (2017)

Voltage-dependent processes in the electroneutral amino acid exchanger ASCT2
por: Zander, Catherine B., et al.
Publicado: (2013)

Targeting of glutamine transporter ASCT2 and glutamine synthetase suppresses gastric cancer cell growth
por: Ye, Jianxin, et al.
Publicado: (2018)

Targeting ASCT2‐mediated glutamine uptake blocks prostate cancer growth and tumour development
por: Wang, Qian, et al.
Publicado: (2015)

Effects of Mutations and Ligands on the Thermostability of the l-Arginine/Agmatine Antiporter AdiC and Deduced Insights into Ligand-Binding of Human l-Type Amino Acid Transporters
por: Ilgü, Hüseyin, et al.
Publicado: (2018)

Pharmacological Blockade of ASCT2-dependent Glutamine Transport Leads To Anti-tumor Efficacy in Preclinical Models
por: Schulte, Michael L., et al.
Publicado: (2018)

Ligand Discovery from a Dopamine D(3) Receptor Homology Model and Crystal Structure
por: Carlsson, Jens, et al.
Publicado: (2011)

Structural characterisation reveals insights into substrate recognition by the glutamine transporter ASCT2/SLC1A5
por: Scopelliti, Amanda J, et al.
Publicado: (2018)

ASCT2 overexpression is associated with poor survival of OSCC patients and ASCT2 knockdown inhibited growth of glutamine‐addicted OSCC cells
por: Luo, Yijun, et al.
Publicado: (2020)

Cryo-EM structures of the human glutamine transporter SLC1A5 (ASCT2) in the outward-facing conformation
por: Yu, Xiaodi, et al.
Publicado: (2019)

Inhibition of glucose metabolism prevents glycosylation of the glutamine transporter ASCT2 and promotes compensatory LAT1 upregulation in leukemia cells
por: Polet, Florence, et al.
Publicado: (2016)

Ag120-Mediated Inhibition of ASCT2-Dependent Glutamine Transport has an Anti-Tumor Effect on Colorectal Cancer Cells
por: Yu, Wei, et al.
Publicado: (2022)

A Novel ASCT2 Inhibitor, C118P, Blocks Glutamine Transport and Exhibits Antitumour Efficacy in Breast Cancer
por: Lyu, Xiao-Dan, et al.
Publicado: (2023)

Epigenetic silencing of microRNA-137 enhances ASCT2 expression and tumor glutamine metabolism
por: Dong, J, et al.
Publicado: (2017)

ASCT2 is the primary serine transporter in cancer cells
por: Conger, Kelly O., et al.
Publicado: (2023)

Targeting ASCT2-mediated glutamine metabolism inhibits proliferation and promotes apoptosis of pancreatic cancer cells
por: Wang, Wenbin, et al.
Publicado: (2022)

ASCT2/SLC1A5 controls glutamine uptake and tumour growth in triple-negative basal-like breast cancer
por: van Geldermalsen, M, et al.
Publicado: (2016)

The glutamine transporter ASCT2 (SLC1A5) promotes tumor growth independently of the amino acid transporter LAT1 (SLC7A5)
por: Cormerais, Yann, et al.
Publicado: (2018)

NDRG2 ablation reprograms metastatic cancer cells towards glutamine dependence via the induction of ASCT2
por: Ding, Mingchao, et al.
Publicado: (2020)

Cys Site-Directed Mutagenesis of the Human SLC1A5 (ASCT2) Transporter: Structure/Function Relationships and Crucial Role of Cys467 for Redox Sensing and Glutamine Transport
por: Scalise, Mariafrancesca, et al.
Publicado: (2018)

Delta-Tocotrienol Modulates Glutamine Dependence by Inhibiting ASCT2 and LAT1 Transporters in Non-Small Cell Lung Cancer (NSCLC) Cells: A Metabolomic Approach
por: Rajasinghe, Lichchavi Dhananjaya, et al.
Publicado: (2019)

ASCT2 (SLC1A5)-dependent glutamine uptake is involved in the progression of head and neck squamous cell carcinoma
por: Zhang, Ze, et al.
Publicado: (2019)

Cooperation of the Conserved Aspartate 439 and Bound Amino Acid Substrate Is Important for High-Affinity Na(+) Binding to the Glutamate Transporter EAAC1
por: Tao, Zhen, et al.
Publicado: (2007)

Early Intermediates in the Transport Cycle of the Neuronal Excitatory Amino Acid Carrier Eaac1
por: Watzke, Natalie, et al.
Publicado: (2001)

Mechanism and potential sites of potassium interaction with glutamate transporters
por: Wang, Jiali, et al.
Publicado: (2020)

The Glutamate Transporter Subtypes EAAT4 and EAATs 1-3 Transport Glutamate with Dramatically Different Kinetics and Voltage Dependence but Share a Common Uptake Mechanism
por: Mim, Carsten, et al.
Publicado: (2005)

On the Mechanism of Proton Transport by the Neuronal Excitatory Amino Acid Carrier 1
por: Watzke, Natalie, et al.
Publicado: (2000)

DFGmodel: Predicting Protein Kinase Structures in Inactive States for Structure-Based Discovery of Type-II Inhibitors
por: Ung, Peter Man-Un, et al.
Publicado: (2014)

Observing spontaneous, accelerated substrate binding in molecular dynamics simulations of glutamate transporters
por: Wang, Jiali, et al.
Publicado: (2021)

D-Serine Is a Substrate for Neutral Amino Acid Transporters ASCT1/SLC1A4 and ASCT2/SLC1A5, and Is Transported by Both Subtypes in Rat Hippocampal Astrocyte Cultures
por: Foster, Alan C., et al.
Publicado: (2016)

A one-gate elevator mechanism for the human neutral amino acid transporter ASCT2
por: Garaeva, Alisa A., et al.
Publicado: (2019)

Cysteine 467 of the ASCT2 Amino Acid Transporter Is a Molecular Determinant of the Antiport Mechanism
por: Scalise, Mariafrancesca, et al.
Publicado: (2022)

The Treatment of Multiple Myeloma Patients Not Eligible for Asct
por: Richardson, Paul, et al.
Publicado: (2010)

Inhibition of glutamine uptake regulates mTORC1, glutamine metabolism and cell growth in prostate cancer
por: Wang, Qian, et al.
Publicado: (2014)

Cannot write session to /tmp/vufind_sessions/sess_j13hdsbfe4naq3i73ueughit75