2021
DOI: 10.3390/pr9071170
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Highly Specific L-Type Amino Acid Transporter 1 Inhibition by JPH203 as a Potential Pan-Cancer Treatment

Abstract: Accelerated cancer cell growth requires a massive intake of amino acids. Overexpression of L-type (large) amino acid transporter 1 (LAT1) on the cancer cell membrane facilitates such a demand, which is limited in normal organs. Therefore, LAT1 overexpression is ideal as a molecular cancer therapeutic target. JPH203, a LAT1-selective non-transportable blocker, had demonstrated LAT1 inhibition in <10 µM IC50 values and effectively suppressed cancer cell growth in studies involving several types of cancer cell… Show more

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Cited by 10 publications
(11 citation statements)
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“…BCH and 4F2Hc that were contained in the selected microscopy structure of LAT-1 must be extracted from the LAT-1 structure and re-docked to verify that the molecular docking software can reproduce the agonist conformation of the native ligand (N3). The result is valid if the obtained Root Mean Square Deviation (RMSD) value is ≤2.0 Å [7]. The best-docked N3 conformation showed an RMSD of 1.827 Å compared to the previous pose (table 1).…”
Section: Discussionmentioning
confidence: 85%
See 1 more Smart Citation
“…BCH and 4F2Hc that were contained in the selected microscopy structure of LAT-1 must be extracted from the LAT-1 structure and re-docked to verify that the molecular docking software can reproduce the agonist conformation of the native ligand (N3). The result is valid if the obtained Root Mean Square Deviation (RMSD) value is ≤2.0 Å [7]. The best-docked N3 conformation showed an RMSD of 1.827 Å compared to the previous pose (table 1).…”
Section: Discussionmentioning
confidence: 85%
“…LAT-1 can distribute eight of the nine essential amino acids to certain body areas such as the placenta and blood-brain barrier so that LAT-1 is said to be one of the main proteins in cell growth and development [6]. In addition, LAT-1 has overexpression and is highly selective against cancer cells, but its distribution is limited to normal cells [7]. The overexpression of LAT-1 in cancer cells and its ability to deliver substrates makes LAT-1 become a promising target for therapy and diagnostic (theranostic) molecules (fig.…”
Section: Introductionmentioning
confidence: 99%
“…There are several dozen types of amino acids transporters, and one of the most important is the SLC family which includes SLC7A5 (LAT1), SLC7A8 (LAT2), SLC43A1 (LAT3), and SLC43A2 (LAT4). The abbreviation LATs means that their transport large neutral amino acids [2,3].…”
Section: Introductionmentioning
confidence: 99%
“…The large-type amino acid transporter (LAT-1) is an antiporter of ubiquitous Na+and H+involved in the uptake of essential amino acids of the cells. LAT-1 is over-expressed in human cancer cells due to its increased demand for amino acids, but its distribution is limited to normal cells [1][2][3][4]. LAT-1 can distribute eight of the nine essential amino acids at somebody areas, such as the blood-brain barrier and placenta [5].…”
Section: Introductionmentioning
confidence: 99%