What question did this study set out to answer?

To evaluate the efficacy and selectivity of the novel compound KYT-0353 in inhibiting L-type amino acid transporter 1 and suppressing tumor cell growth.

October 8, 2009Cancer ScienceOpen Access

l‐Type amino acid transporter 1 inhibitors inhibit tumor cell growth

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Authors

KOKoji OdaKawaguchi Junior College NHNoriko HosodaTanabe Research Laboratories HEHiroshi EndôUniversity of Shiga Prefecture

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Implication

Preclinical study demonstrates that selective LAT1 inhibitor KYT-0353 suppresses colon cancer growth in vitro and in vivo, indicating its potential as an anti-tumor agent.

Key Points

To evaluate the efficacy and selectivity of the novel compound KYT-0353 in inhibiting L-type amino acid transporter 1 and suppressing tumor cell growth.
Measured (14)C-leucine uptake and in vitro growth inhibition in human colon cancer HT-29 cells and mouse renal proximal tubule cells.
Assessed in vivo anti-tumor efficacy and safety by intravenously administering KYT-0353 at 12.5 mg/kg and 25.0 mg/kg to nude mice bearing HT-29 xenografts.
In HT-29 cells, KYT-0353 inhibited (14)C-leucine uptake with an IC50 of 0.06 µM and suppressed cell growth with an IC50 of 4.1 µM; in mouse renal proximal tubule cells, the IC50 values were 0.14 µM and 16.4 µM, respectively.
Intravenous KYT-0353 produced statistically significant tumor growth inhibition in mice, reaching maximal inhibition ratios of 65.9% at 12.5 mg/kg and 77.2% at 25.0 mg/kg, with minimal body weight loss (maximal depression of 3.7% and 6.3%, respectively).

Cite This Study

Oda et al. (2009) studied this question.

synapsesocial.com/papers/69fafa86ed76930a72df7c8f https://doi.org/10.1111/j.1349-7006.2009.01386.x

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Implication

Preclinical study demonstrates that selective LAT1 inhibitor KYT-0353 suppresses colon cancer growth in vitro and in vivo, indicating its potential as an anti-tumor agent.

l‐Type amino acid transporter 1 inhibitors inhibit tumor cell growth

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Implication

Key Points

Cite This Study

l‐Type amino acid transporter 1 inhibitors inhibit tumor cell growth

Discussion

Member takes

Implication

Key Points

Cite This Study

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