Characterization of pre-incubation inhibitory effects of JPH203 on L-type amino acid transporter 1 function.
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- Okunushi Kentaro
- Dept. Pharm., Grad. Sch. Med., Chiba Univ. Dept. Pediatrics, Grad. Sch. of Med., Chiba Univ.
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- Furihata Tomomi
- Dept. Pharm., Grad. Sch. Med., Chiba Univ.
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- Higuchi Kosuke
- Dept. Pharm., Grad. Sch. Med., Chiba Univ.
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- Reien Yoshie
- Dept. Pharm., Grad. Sch. Med., Chiba Univ.
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- Nakagawa Kiyoshi
- Dept. Pharm., Grad. Sch. Med., Chiba Univ.
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- Simojo Naoki
- Dept. Pediatrics, Grad. Sch. of Med., Chiba Univ.
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- Anzai Naohiko
- Dept. Pharm., Grad. Sch. Med., Chiba Univ.
Bibliographic Information
- Other Title
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- JPH203はLAT1に対して前曝露阻害効果を有する
Abstract
<p>BACKGROUND/AIM: JPH203 is a novel anti-cancer drug targeting L-type amino acid transporter 1 (LAT1), which plays a key role in essential amino acid uptake in cancer cells. While the co-incubation inhibitory effect of JPH203 has been characterized in conventional uptake assay, its pre-incubation inhibitory effects remain undetermined. Therefore, we aimed to characterize pre-incubation inhibitory effects of JPH203 on LAT1 function. METHODS: Pre-incubation effects were examined by leucine uptake assay using LAT1-positive human colon cancer HT-29 cells. RESULTS: In time-dependency analysis, pre-incubation of HT-29 cells with 10 uM JPH203 for 30, 60, and 120 min resulted in a significant decrease of the leucine uptake activity (42%, 32%, and 28% of those obtained from the control cells, respectively). Similarly, in concentration-dependency analysis, pre-incubation of the cells with JPH203 (1, 10, and 30 uM for 120 min) decreased the activity level to 68%, 25%, and 3% of those of the control cells, respectively. CONCLUSION: We have identified potent pre-incubation inhibitory effects of JPH203 on LAT1 function. Combination effects of pre- and co-incubation inhibitory effects are currently under examination.</p>
Journal
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- Proceedings for Annual Meeting of The Japanese Pharmacological Society
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Proceedings for Annual Meeting of The Japanese Pharmacological Society 92 (0), 1-P-105-, 2019
Japanese Pharmacological Society
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Details 詳細情報について
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- CRID
- 1390846609814429440
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- NII Article ID
- 130007812709
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- ISSN
- 24354953
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- Text Lang
- ja
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- Data Source
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- JaLC
- Crossref
- CiNii Articles
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- Abstract License Flag
- Disallowed