Pre-steady-state Kinetic Analysis of Amino Acid Transporter SLC6A14 Reveals Rapid Turnover Rate and Substrate Translocation

Autor: Yueyue Shi, Jiali Wang, Elias Ndaru, Christof Grewer

Publikováno v: Frontiers in Physiology, Vol 12 (2021)

SLC6A14 (solute carrier family 6 member 14) is an amino acid transporter, driven by Na+ and Cl− co-transport, whose structure, function, and molecular and kinetic mechanism have not been well characterized. Its broad substrate selectivity, includin

Externí odkaz: https://doaj.org/article/ed931a4e9a9440dfb4383a7146aa37a1

Alanine serine cysteine transporter (ASCT) substrate binding site properties probed with hydroxyhomoserine esters

Autor: Elias Ndaru, Laura Zielewicz, Yueyue Shi, Keino Hutchinson, Rachel‐Ann A. Garibsingh, Avner Schlessinger, Christof Grewer

Publikováno v: Journal of physical organic chemistry. 35(11)

The glutamine transporter ASCT2 is highly overexpressed in cancer cells. Block of glutamine uptake by ASCT2 is a potential strategy to inhibit growth of cancer cells. However, pharmacology of the ASCT2 binding site is not well established. In this wo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::30717a2d47b741d21565dc2e6e029f8f
https://pubmed.ncbi.nlm.nih.gov/36568026

Rational design of ASCT2 inhibitors using an integrated experimental-computational approach

Autor: Massimiliano Bonomi, Cristina Paulino, Christof Grewer, Paul Zakrepine, Rachel Ann A. Garibsingh, Avner Schlessinger, Dirk Jan Slotboom, Elias Ndaru, Laura Zielewicz, Yueyue Shi, Alisa A. Garaeva

Publikováno v: Proceedings of the National Academy of Sciences of the United States of America
Proceedings of the National Academy of Sciences of the United States of America, 2021, 118 (37), pp.e2104093118. ⟨10.1073/pnas.2104093118⟩
Proceedings of the National Academy of Sciences of the United States of America, National Academy of Sciences, 2021, 118 (37), pp.e2104093118. ⟨10.1073/pnas.2104093118⟩
Proceedings of the National Academy of Sciences of the United States of America, 118(37):e2104093118. NATL ACAD SCIENCES

Significance The glutamine transporter ASCT2 is an emerging therapeutic target for various cancer types. Here, we use an integrated computational and experimental approach to develop unique ASCT2 inhibitors targeting a conformational state useful for

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::adcd7b1cfe4aa735aca7cff14f732ba3
https://hal.science/hal-03417486v2/document

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

Autor: Paul Zakrepine, Rachel-Ann A. Garibsingh, Jiali Wang, Christof Grewer, Avner Schlessinger, Evan Wallace, Yueyue Shi, Elias Ndaru

Publikováno v: The Journal of General Physiology

ASCT2 is a transporter that exchanges neutral amino acids such as glutamine across the cell membrane, an essential process for rapidly growing cells, including cancerous ones. Ndaru et al. report the synthesis and characterization of a novel class of

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::568679f0822338ead44f0f798229d3e1
https://doi.org/10.1085/jgp.201812276

Interaction of the neutral amino acid transporter ASCT2 with basic amino acids

Autor: Avner Schlessinger, Elias Ndaru, Christof Grewer, Rachel-Ann A. Garibsingh, Laura Zielewicz

Publikováno v: Biochem J

Glutamine transport across cell membranes is performed by a variety of transporters, including the alanine serine cysteine transporter 2 (ASCT2). The substrate-binding site of ASCT2 was proposed to be specific for small amino acids with neutral side

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::678b9ec442cafe0aff0604bf1a877454
https://pubmed.ncbi.nlm.nih.gov/32242892