{"id":1074,"date":"2022-08-21T20:49:32","date_gmt":"2022-08-21T17:49:32","guid":{"rendered":"https:\/\/sites.uef.fi\/drug-targeting\/?page_id=1074"},"modified":"2026-07-03T15:41:05","modified_gmt":"2026-07-03T12:41:05","slug":"lat1","status":"publish","type":"page","link":"https:\/\/sites.uef.fi\/drug-targeting\/transporters\/lat1\/","title":{"rendered":"LAT1"},"content":{"rendered":"\n<p><strong>L-Type Amino Acid Transporter 1 (LAT1)<\/strong> is a sodium- and pH-independent transporter responsible for the uptake of large neutral amino acids and several clinically used drugs, including L-DOPA, gabapentin, baclofen, and melphalan. LAT1 functions as a heterodimer consisting of a light chain (SLC7A5) and a heavy chain (CD98\/4F2hc; SLC3A2), which is required for proper localization and activity of the transporter.<\/p>\n\n\n\n<p>LAT1 is highly expressed in tissues with high amino acid demand, such as the brain and placenta, and is frequently upregulated in cancer cells and activated immune cells. Its expression at the blood\u2013brain barrier and in several disease-relevant tissues makes LAT1 an attractive target for transporter-mediated drug delivery and therapeutic intervention.<\/p>\n\n\n\n<figure class=\"wp-block-image size-large is-resized\"><img loading=\"lazy\" decoding=\"async\" width=\"1024\" height=\"566\" src=\"https:\/\/sites.uef.fi\/drug-targeting\/wp-content\/uploads\/sites\/59\/2022\/12\/Graphical-Abstract-1024x566.png\" alt=\"\" class=\"wp-image-1296\" style=\"width:617px;height:auto\" srcset=\"https:\/\/sites.uef.fi\/drug-targeting\/wp-content\/uploads\/sites\/59\/2022\/12\/Graphical-Abstract-1024x566.png 1024w, https:\/\/sites.uef.fi\/drug-targeting\/wp-content\/uploads\/sites\/59\/2022\/12\/Graphical-Abstract-300x166.png 300w, https:\/\/sites.uef.fi\/drug-targeting\/wp-content\/uploads\/sites\/59\/2022\/12\/Graphical-Abstract-768x425.png 768w, https:\/\/sites.uef.fi\/drug-targeting\/wp-content\/uploads\/sites\/59\/2022\/12\/Graphical-Abstract-1536x849.png 1536w, https:\/\/sites.uef.fi\/drug-targeting\/wp-content\/uploads\/sites\/59\/2022\/12\/Graphical-Abstract-2048x1132.png 2048w\" sizes=\"auto, (max-width: 1024px) 100vw, 1024px\" \/><\/figure>\n\n\n\n<p><strong>LAT1 is one of the primary transporter platforms in our research.<\/strong> We investigate LAT1 as both a carrier and a therapeutic target, with applications ranging from brain- and cell-selective drug delivery to cancer-, pancreatic-, placental-, and mitochondrial-targeted therapies.<\/p>\n\n\n\n<figure class=\"wp-block-image size-full is-resized\"><img loading=\"lazy\" decoding=\"async\" width=\"608\" height=\"430\" src=\"https:\/\/sites.uef.fi\/drug-targeting\/wp-content\/uploads\/sites\/59\/2023\/12\/Graphical-abstract.jpg\" alt=\"\" class=\"wp-image-2093\" style=\"width:565px;height:auto\" srcset=\"https:\/\/sites.uef.fi\/drug-targeting\/wp-content\/uploads\/sites\/59\/2023\/12\/Graphical-abstract.jpg 608w, https:\/\/sites.uef.fi\/drug-targeting\/wp-content\/uploads\/sites\/59\/2023\/12\/Graphical-abstract-300x212.jpg 300w\" sizes=\"auto, (max-width: 608px) 100vw, 608px\" \/><\/figure>\n\n\n\n<h2 class=\"wp-block-heading\">Selected Publications<\/h2>\n\n\n\n<p>Bahrami, K.; J\u00e4rvinen, J.; Laitinen, T.; Reinisalo, M.; Honkakoski, P.; Poso, A.; Huttunen, K. M.; Rautio, J. Structural features affecting selectivity of LAT1-targeted phenylalanine drug conjugates. <strong><em>Molecular Pharmaceutics<\/em><\/strong>, <strong>2022<\/strong>, <em>20<\/em>(1):206-218. <a href=\"https:\/\/doi.org\/10.1021\/acs.molpharmaceut.2c00594\" target=\"_blank\" rel=\"noreferrer noopener\">https:\/\/doi.org\/10.1021\/acs.molpharmaceut.2c00594<\/a><\/p>\n\n\n\n<p>Huttunen, J.; Agami, M.; Tampio, J.; Montaser, A. B.; Huttunen, K. M. Comparison of Experimental Strategies to Study L-Type Amino Acid Transporter 1 (LAT1) Utilization by Ligands. <strong><em>Molecules<\/em><\/strong>, <strong>2021<\/strong>, <em>27<\/em>(1), 37, 37-57. <a href=\"https:\/\/doi.org\/10.3390\/molecules27010037\" target=\"_blank\" rel=\"noreferrer noopener\">https:\/\/doi.org\/10.3390\/molecules27010037<\/a><\/p>\n\n\n\n<p>Jalkanen, A.; Ihalainen, J.; Lehtonen, M.; Forsberg, M. M.; Rautio, J.; Huttunen, K. M.; Gynther, M. Species differences between mice and rats in the pharmacology of a LAT1-utilizing compound. <em><strong>International Journal of Pharmaceutics<\/strong><\/em>, <strong>2021<\/strong>, <em>596<\/em>: 120300.&nbsp;<a href=\"https:\/\/doi.org\/10.1016\/j.ijpharm.2021.120300\" target=\"_blank\" rel=\"noreferrer noopener\">https:\/\/doi.org\/10.1016\/j.ijpharm.2021.120300<\/a><\/p>\n\n\n\n<p>K\u00e4rkk\u00e4inen, J.; Laitinen, T.; Markowicz-Piasecka, M.; Montaser, A.; Lehtonen, M.; Rautio, J.; Gynther, M.; Poso, A.; Huttunen, K.M. Molecular characteristics supporting l-Type amino acid transporter 1 (LAT1)-mediated translocation. <em><strong>Bioorganic Chemistry<\/strong><\/em>, <strong>2021<\/strong>, 112: 104921. <a href=\"https:\/\/doi.org\/10.1016\/j.bioorg.2021.104921\" target=\"_blank\" rel=\"noreferrer noopener\">https:\/\/doi.org\/10.1016\/j.bioorg.2021.104921<\/a><\/p>\n\n\n\n<p>Huttunen J.; Gynther, M.; Vellonen, K.-S.; Huttunen, K. M. L-Type Amino Acid Transporter 1 (LAT1)-Utilizing Prodrugs Are Carrier-Selective Despite Having Low Affinity for Organic Anion Transporting Polypeptides (OATPs). <strong><em>International Journal of Pharmaceutics<\/em><\/strong>, <strong>2019<\/strong>, <em>571<\/em>, 11871410. <a href=\"http:\/\/doi.org\/10.1016\/j.ijpharm.2019.118714\" target=\"_blank\" rel=\"noreferrer noopener\">http:\/\/doi.org\/10.1016\/j.ijpharm.2019.118714<\/a><\/p>\n\n\n\n<p>K\u00e4rkk\u00e4inen, J.; Gynther, M.; Kokkola, T.; Petsalo, A.; Auriola, S.; Lahtela-Kakkonen, M.; Laine, K.; Rautio, J.; Huttunen, K. M. Structural Properties for Selective and Efficient L-Type Amino Acid Transporter 1 (LAT1)- Mediated Cellular Uptake. <strong><em>International Journal of Pharmaceutics<\/em><\/strong>, <strong>2018<\/strong>, <em>544<\/em> (1), 91-99. <a href=\"http:\/\/doi.org\/10.1016\/j.ijpharm.2018.04.025\" target=\"_blank\" rel=\"noreferrer noopener\">http:\/\/doi.org\/10.1016\/j.ijpharm.2018.04.025<\/a><\/p>\n\n\n\n<p>Huttunen, K. M.; Huttunen, J.; Aufderhaar, I.; Gynther, M.; Denny, W. A.; Spicer, J. A. L-Type Amino Acid Transporter 1 (LAT1)- Mediated Targeted Delivery of Perforin Inhibitors. <strong><em>International Journal of Pharmaceutics<\/em><\/strong>, <strong>2015<\/strong>, <em>498<\/em> (1-2), 205-216. <a href=\"http:\/\/dx.doi.org\/10.1016\/j.ijpharm.2015.12.034\" target=\"_blank\" rel=\"noreferrer noopener\">http:\/\/dx.doi.org\/10.1016\/j.ijpharm.2015.12.034<\/a><\/p>\n\n\n\n<p>Ylikangas, H.; Malmioja, K.; Peura, L.; Gynther, M.; Nwachukwu, E. O.; Lepp\u00e4nen, J.; Laine, K.; Rautio, J.; Lahtela-Kakkonen, M.; Huttunen, K. M.; Poso, A. Quantitative Insights for the Design of Compounds Recognized by L-Type Amino Acid Transporter 1 (LAT1). <strong><em>ChemMedChem<\/em><\/strong>, <strong>2014<\/strong>,<em> 9<\/em> (12), 2699-2707. <a href=\"http:\/\/dx.doi.org\/10.1002\/cmdc.201402281\" target=\"_blank\" rel=\"noreferrer noopener\">http:\/\/dx.doi.org\/10.1002\/cmdc.201402281<\/a><\/p>\n","protected":false},"excerpt":{"rendered":"<p>L-Type Amino Acid Transporter 1 (LAT1) is a sodium- and pH-independent transporter responsible for the uptake of large neutral amino acids and several clinically used drugs, including L-DOPA, gabapentin, baclofen, and melphalan. LAT1 functions as a heterodimer consisting of a light chain (SLC7A5) and a heavy chain (CD98\/4F2hc; SLC3A2), which is required for proper localization [&hellip;]<\/p>\n","protected":false},"author":140,"featured_media":0,"parent":1047,"menu_order":1,"comment_status":"closed","ping_status":"closed","template":"","meta":{"_acf_changed":false,"_monsterinsights_skip_tracking":false,"_monsterinsights_sitenote_active":false,"_monsterinsights_sitenote_note":"","_monsterinsights_sitenote_category":0,"footnotes":""},"class_list":["post-1074","page","type-page","status-publish","hentry"],"acf":[],"yoast_head":"<!-- This site is optimized with the Yoast SEO plugin v27.7 - https:\/\/yoast.com\/product\/yoast-seo-wordpress\/ -->\n<title>LAT1 - Transporter Targeted Drug Delivery<\/title>\n<meta name=\"robots\" content=\"index, follow, max-snippet:-1, max-image-preview:large, max-video-preview:-1\" \/>\n<link rel=\"canonical\" href=\"https:\/\/sites.uef.fi\/drug-targeting\/transporters\/lat1\/\" \/>\n<meta property=\"og:locale\" content=\"en_US\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"LAT1 - Transporter Targeted Drug Delivery\" \/>\n<meta property=\"og:description\" content=\"L-Type Amino Acid Transporter 1 (LAT1) is a sodium- and pH-independent transporter responsible for the uptake of large neutral amino acids and several clinically used drugs, including L-DOPA, gabapentin, baclofen, and melphalan. 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