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Volume 9
Issue 7
10.3390/pr9071170
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Review

Highly Specific L-Type Amino Acid Transporter 1 Inhibition by JPH203 as a Potential Pan-Cancer Treatment

by
Arifudin Achmad
1,2,†,
Shinta Lestari
3,†,
Holis Abdul Holik
3,
Driyanti Rahayu
3,
Muhammad Hasan Bashari
2,4,
Ahmad Faried
5 and
Achmad Hussein Sundawa Kartamihardja
1,*
1
Department of Nuclear Medicine and Molecular Theranostics, Faculty of Medicine, Universitas Padjadjaran/Hasan Sadikin General Hospital, Bandung 40161, Indonesia
2
Oncology and Stem Cell Working Group, Faculty of Medicine, Universitas Padjadjaran, Bandung 40161, Indonesia
3
Department of Pharmaceutical Analysis and Medicinal Chemistry, Faculty of Pharmacy, Universitas Padjadjaran, Sumedang 45363, Indonesia
4
Division of Pharmacology and Therapy, Department of Basic Medical Sciences, Faculty of Medicine, Universitas Padjadjaran, Bandung 40161, Indonesia
5
Department of Neurosurgery, Faculty of Medicine, Universitas Padjadjaran/Hasan Sadikin General Hospital, Bandung 40161, Indonesia
*
Author to whom correspondence should be addressed.
†
Equal contributions.
Processes 2021, 9(7), 1170; https://doi.org/10.3390/pr9071170
Submission received: 1 May 2021 / Revised: 22 June 2021 / Accepted: 2 July 2021 / Published: 5 July 2021
(This article belongs to the Special Issue Advances in Anticancer Agents)
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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 lines and tumor xenograft models. A limited phase I clinical trial was performed on five different solid tumors and showed that JPH203 is well-tolerated and has a promising activity for the treatment of bile duct cancer. This review details the development and prospect of JPH203 as a LAT1-targeting cancer therapy.
Keywords: cancer; JPH203; LAT1; targeted drug; amino acid metabolism cancer; JPH203; LAT1; targeted drug; amino acid metabolism

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MDPI and ACS Style

Achmad, A.; Lestari, S.; Holik, H.A.; Rahayu, D.; Bashari, M.H.; Faried, A.; Kartamihardja, A.H.S. Highly Specific L-Type Amino Acid Transporter 1 Inhibition by JPH203 as a Potential Pan-Cancer Treatment. Processes 2021, 9, 1170. https://doi.org/10.3390/pr9071170

AMA Style

Achmad A, Lestari S, Holik HA, Rahayu D, Bashari MH, Faried A, Kartamihardja AHS. Highly Specific L-Type Amino Acid Transporter 1 Inhibition by JPH203 as a Potential Pan-Cancer Treatment. Processes. 2021; 9(7):1170. https://doi.org/10.3390/pr9071170

Chicago/Turabian Style

Achmad, Arifudin, Shinta Lestari, Holis Abdul Holik, Driyanti Rahayu, Muhammad Hasan Bashari, Ahmad Faried, and Achmad Hussein Sundawa Kartamihardja. 2021. "Highly Specific L-Type Amino Acid Transporter 1 Inhibition by JPH203 as a Potential Pan-Cancer Treatment" Processes 9, no. 7: 1170. https://doi.org/10.3390/pr9071170

APA Style

Achmad, A., Lestari, S., Holik, H. A., Rahayu, D., Bashari, M. H., Faried, A., & Kartamihardja, A. H. S. (2021). Highly Specific L-Type Amino Acid Transporter 1 Inhibition by JPH203 as a Potential Pan-Cancer Treatment. Processes, 9(7), 1170. https://doi.org/10.3390/pr9071170

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