scholarly journals Amino Acid Transporter SLC6A14 (ATB0,+) – A Target in Combined Anti-cancer Therapy

2020 ◽  
Vol 8 ◽  
Author(s):  
Katarzyna A. Nałęcz
Keyword(s):  
Amino Acid ◽  
Cancer Therapy ◽  
Amino Acid Transporter ◽  
Anti Cancer ◽  
Acid Transporter

scholarly journals JPH203, a newly developed anti-cancer drug, shows a preincubation inhibitory effect on L-type amino acid transporter 1 function

2020 ◽  
Vol 144 (1) ◽  
pp. 16-22 ◽  
Author(s):  
Kentaro Okunushi ◽  
Tomomi Furihata ◽  
Hanae Morio ◽  
Yasuhide Muto ◽  
Kosuke Higuchi ◽  
...  
Keyword(s):  
Amino Acid ◽  
Inhibitory Effect ◽  
Amino Acid Transporter ◽  
Cancer Drug ◽  
Anti Cancer ◽  
Acid Transporter

scholarly journals JPH203 as a potential L-Type Amino Acid Transporter 1 (LAT 1) inhibitor in the development of cancer theragnostic compounds

2020 ◽  
Vol 16 (2) ◽  
pp. 167-181
Author(s):  
Yolanda Pertiwi ◽  
Driyanti Rahayu ◽  
Maula Eka Sriyani ◽  
Raden Bayu Indradi ◽  
Holis Abdul Holik
Keyword(s):  
Amino Acid ◽  
Cancer Therapy ◽  
Cancer Cells ◽  
Amino Acid Transporter ◽  
Potential Candidate ◽  
Literature Study ◽  
Cancer Cell Growth ◽  
Specific Target ◽  
Target Molecules ◽  
Acid Transporter

Background: Cancer has become a major cause of global health problems. Latest research currently focuses on an approach to cancer therapy that involves specific target molecules and theragnostic (therapy and diagnostic) agents. Among the specific target molecules in cancer therapy is LAT1, which is over expressed in cancer cells but under expressed in normal cells. Therefore, LAT1 inhibition can become an alternative to cancer therapy. A number of studies have shown that JPH203 specifically inhibits LAT1, thus reducing amino acid absorption into cancer cells and inhibiting cancer cell growth. Objective: The main objective of this literature study was to determine the potential of JPH203 as a LAT1 inhibitor to be developed into a novel theragnostic agent for cancer. Methods: Various studies were summarized to outline the development of JPH203 as a therapy targeting LAT1 and potential candidate of theragnostic compounds. Results: The results of the literature study showed that JPH203 as a selective LAT1 inhibitor was able to efficiently suppress the growth of cancer cells with a low IC50 value. Conclusion: The activity of LAT1 as an amino acid transporter of cancer cells could be selectively inhibited by JPH203, thereby allowing JPH203 to be reconsidered as a potential therapy in the development of theragnostic compounds against cancer. Keywords: JPH203, theragnostic, LAT1 inhibitor

Increased expression of an amino acid transporter LAT1 in healing of acetic acid-induced chronic gastric ulcer in rats

2001 ◽  
Vol 120 (5) ◽  
pp. A153-A153
Author(s):  
S MIYAMOTO ◽  
K KATO ◽  
Y ISHII ◽  
S ASAI ◽  
T NAGAISHI ◽  
...  
Keyword(s):  
Acetic Acid ◽  
Gastric Ulcer ◽  
Amino Acid ◽  
Amino Acid Transporter ◽  
Chronic Gastric Ulcer ◽  
Acid Transporter

scholarly journals Identification and Characterization of Inhibitors of a Neutral Amino Acid Transporter, SLC6A19, Using Two Functional Cell-Based Assays

2018 ◽  
Vol 24 (2) ◽  
pp. 111-120 ◽  
Author(s):  
Sanjay J. Danthi ◽  
Beirong Liang ◽  
Oanh Smicker ◽  
Benjamin Coupland ◽  
Jill Gregory ◽  
...  
Keyword(s):  
Amino Acid ◽  
High Throughput Screening ◽  
Amino Acid Transporter ◽  
Neutral Amino Acid ◽  
Imaging Plate ◽  
Acid Uptake ◽  
Functional Assays ◽  
Neutral Amino Acid Transporter ◽  
Acid Transporter ◽  
Pharmacologically Active

SLC6A19 (B0AT1) is a neutral amino acid transporter, the loss of function of which results in Hartnup disease. SLC6A19 is also believed to have an important role in amino acid homeostasis, diabetes, and weight control. A small-molecule inhibitor of human SLC6A19 (hSLC6A19) was identified using two functional cell-based assays: a fluorescence imaging plate reader (FLIPR) membrane potential (FMP) assay and a stable isotope-labeled neutral amino acid uptake assay. A diverse collection of 3440 pharmacologically active compounds from the Microsource Spectrum and Tocriscreen collections were tested at 10 µM in both assays using MDCK cells stably expressing hSLC6A19 and its obligatory subunit, TMEM27. Compounds that inhibited SLC6A19 activity in both assays were further confirmed for activity and selectivity and characterized for potency in functional assays against hSLC6A19 and related transporters. A single compound, cinromide, was found to robustly, selectively, and reproducibly inhibit SLC6A19 in all functional assays. Structurally related analogs of cinromide were tested to demonstrate structure–activity relationship (SAR). The assays described here are suitable for carrying out high-throughput screening campaigns to identify modulators of SLC6A19.

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