L-type amino acid transporter LAT1 inhibitor
CAS：20448-79-7
分子式：C8H13NO2
分子量：155.2
纯度：98%
存储：Store at -20°C

Background:

The L-type amino acid transporters (LATs) are Na+-dependent neutral amino acid transporters.[1] They include four members in two sub-families, with LAT1 and LAT2 belonging to solute carrier (SLC) family 7 and LAT3 and LAT4 being members of SLC43.1 LAT1 is overexpressed in many tumors and contributes to ribosome biogenesis and cell growth by supporting mTOR complex 1 (mTORC1) signaling.[2] BCH is an inhibitor of LAT1 that blocks the uptake of L-leucine with an IC50 value of 131.5 μM.[3],[4] It can inhibit all members of the LAT family at a concentration of 10 mM.[1] In addition to eliminating the uptake of neutral amino acids, BCH suppresses mTORC1 signaling that drives DNA synthesis and cell proliferation.[1],[2] LAT1 is also essential for the uptake of amino acid-related compounds, like L-DOPA, through the blood-brain barrier, and this can be inhibited by BCH.[4],[5]

Reference:
[1]. Wang, Q., and Holst, J. L-type amino acid transport and cancer: Targeting the mTORC1 pathway to inhibit neoplasia. Am.J.Cancer Res. 5(4), 1281-1294 (2015).
[2]. Dann, S.G., Selvaraj, A., and Thomas, G. mTOR Complex1-S6K1 signaling: At the crossroads of obesity, diabetes and cancer. Trends Mol. Med. 13(6), 252-259 (2007).
[3]. Fraga, S., Serrao, M.P., and Soares-Da-Silva, P. L-type amino acid transporters in two intestinal epithelial cell lines function as exchangers with neutral amino acids. Journal of Nutrition 132(4), 733-738 (2002).
[4]. Kim, D.K., Kanai, Y., Choi, H.W., et al. Characterization of the system L amino acid transporter in T24 human bladder carcinoma cells. Biochim Biophys.Acta. 1565(1), 112-121 (2002).
[5]. Kageyama, T., Nakamura, M., Matsuo, A., et al. The 4F2hc/LAT1 complex transports L-DOPA across the blood-brain barrier. Brain Research 879(1-2), 115-121 (2000).