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- SLC16 family of monocarboxylate transporters
SLC16 family of monocarboxylate transporters C
Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).
Overview
Members of the SLC16 family may be divided into subfamilies on the basis of substrate selectivities, particularly lactate (e.g. L-lactic acid), pyruvic acid and ketone bodies, as well as aromatic amino acids. Topology modelling suggests 12 TM domains, with intracellular termini and an extended loop at TM 6/7.
The proton-coupled monocarboxylate transporters (monocarboxylate transporters 1, 4, 2 and 3) allow transport of the products of cellular metabolism, principally lactate (e.g. L-lactic acid) and pyruvic acid.
Transporters
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MCT1 (Monocarboxylate transporter 1 / SLC16A1) C Show summary »« Hide summary
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MCT2 (Monocarboxylate transporter 2 / SLC16A7) C Show summary »« Hide summary
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MCT3 (Monocarboxylate transporter 3 / SLC16A8) C Show summary »« Hide summary
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MCT4 (Monocarboxylate transporter 4 / SLC16A3) C Show summary »« Hide summary
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MCT5 (Monocarboxylate transporter 5 / SLC16A4) Show summary »« Hide summary
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MCT6 (Monocarboxylate transporter 6 / SLC16A5) C Show summary »« Hide summary
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MCT7 (Monocarboxylate transporter 7 / SLC16A6) Show summary »« Hide summary
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MCT8 (Monocarboxylate transporter 8 / SLC16A2) C Show summary »« Hide summary
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MCT9 (Monocarboxylate transporter 9 / SLC16A9) Show summary »« Hide summary
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TAT1 (Monocarboxylate transporter 10 / SLC16A10) C Show summary »« Hide summary
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MCT11 (Monocarboxylate transporter 11 / SLC16A11) Show summary »« Hide summary
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MCT12 (Monocarboxylate transporter 12 / SLC16A12) Show summary »« Hide summary
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MCT13 (Monocarboxylate transporter 13 / SLC16A13) Show summary »« Hide summary
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MCT14 (Monocarboxylate transporter 14 / SLC16A14) Show summary »« Hide summary
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Further reading
* Key recommended reading is highlighted with an asterisk
Anderson CM, Thwaites DT. (2010) Hijacking solute carriers for proton-coupled drug transport. Physiology (Bethesda), 25 (6): 364-77. [PMID:21186281]
* Bernal J, Guadaño-Ferraz A, Morte B. (2015) Thyroid hormone transporters-functions and clinical implications. Nat Rev Endocrinol, 11 (7): 406-417. [PMID:25942657]
Braun D, Wirth EK, Schweizer U. (2010) Thyroid hormone transporters in the brain. Rev Neurosci, 21 (3): 173-86. [PMID:20879691]
Friesema EC, Visser WE, Visser TJ. (2010) Genetics and phenomics of thyroid hormone transport by MCT8. Mol. Cell. Endocrinol., 322 (1-2): 107-13. [PMID:20083155]
* Halestrap AP. (2013) The SLC16 gene family - structure, role and regulation in health and disease. Mol. Aspects Med., 34 (2-3): 337-49. [PMID:23506875]
Halestrap AP, Meredith D. (2004) The SLC16 gene family-from monocarboxylate transporters (MCTs) to aromatic amino acid transporters and beyond. Pflugers Arch., 447 (5): 619-28. [PMID:12739169]
Heuer H, Visser TJ. (2009) Minireview: Pathophysiological importance of thyroid hormone transporters. Endocrinology, 150 (3): 1078-83. [PMID:19179441]
Jansen J, Friesema EC, Milici C, Visser TJ. (2005) Thyroid hormone transporters in health and disease. Thyroid, 15 (8): 757-68. [PMID:16131319]
* Jones RS, Morris ME. (2016) Monocarboxylate Transporters: Therapeutic Targets and Prognostic Factors in Disease. Clin. Pharmacol. Ther., 100 (5): 454-463. [PMID:27351344]
Meredith D, Christian HC. (2008) The SLC16 monocaboxylate transporter family. Xenobiotica, 38 (7-8): 1072-106. [PMID:18668440]
Morris ME, Felmlee MA. (2008) Overview of the proton-coupled MCT (SLC16A) family of transporters: characterization, function and role in the transport of the drug of abuse gamma-hydroxybutyric acid. AAPS J, 10 (2): 311-21. [PMID:18523892]
van der Deure WM, Peeters RP, Visser TJ. (2010) Molecular aspects of thyroid hormone transporters, including MCT8, MCT10, and OATPs, and the effects of genetic variation in these transporters. J. Mol. Endocrinol., 44 (1): 1-11. [PMID:19541799]
Visser TJ. (2007) Thyroid hormone transporters. Horm. Res., 68 Suppl 5: 28-30. [PMID:18174701]
Visser WE, Friesema EC, Jansen J, Visser TJ. (2008) Thyroid hormone transport in and out of cells. Trends Endocrinol. Metab., 19 (2): 50-6. [PMID:18291666]
References
1. Curtis NJ, Mooney L, Hopcroft L, Michopoulos F, Whalley N, Zhong H, Murray C, Logie A, Revill M, Byth KF et al.. (2017) Pre-clinical pharmacology of AZD3965, a selective inhibitor of MCT1: DLBCL, NHL and Burkitt's lymphoma anti-tumor activity. Oncotarget, 8 (41): 69219-69236. [PMID:29050199]
2. Draoui N, Schicke O, Fernandes A, Drozak X, Nahra F, Dumont A, Douxfils J, Hermans E, Dogné JM, Corbau R et al.. (2013) Synthesis and pharmacological evaluation of carboxycoumarins as a new antitumor treatment targeting lactate transport in cancer cells. Bioorg. Med. Chem., 21 (22): 7107-17. [PMID:24095010]
3. Friesema EC, Kuiper GG, Jansen J, Visser TJ, Kester MH. (2006) Thyroid hormone transport by the human monocarboxylate transporter 8 and its rate-limiting role in intracellular metabolism. Mol. Endocrinol., 20 (11): 2761-72. [PMID:16887882]
4. Guile SD, Bantick JR, Cheshire DR, Cooper ME, Davis AM, Donald DK, Evans R, Eyssade C, Ferguson DD, Hill S et al.. (2006) Potent blockers of the monocarboxylate transporter MCT1: novel immunomodulatory compounds. Bioorg. Med. Chem. Lett., 16 (8): 2260-5. [PMID:16455256]
5. Murakami Y, Kohyama N, Kobayashi Y, Ohbayashi M, Ohtani H, Sawada Y, Yamamoto T. (2005) Functional characterization of human monocarboxylate transporter 6 (SLC16A5). Drug Metab. Dispos., 33 (12): 1845-51. [PMID:16174808]
6. Quanz M, Bender E, Kopitz C, Grünewald S, Schlicker A, Schwede W, Eheim A, Toschi L, Neuhaus R, Richter C et al.. (2018) Preclinical Efficacy of the Novel Monocarboxylate Transporter 1 Inhibitor BAY-8002 and Associated Markers of Resistance. Mol. Cancer Ther., 17 (11): 2285-2296. [PMID:30115664]
7. Wang Q, Darling IM, Morris ME. (2006) Transport of gamma-hydroxybutyrate in rat kidney membrane vesicles: Role of monocarboxylate transporters. J. Pharmacol. Exp. Ther., 318 (2): 751-61. [PMID:16707723]
How to cite this family page
Database page citation:
SLC16 family of monocarboxylate transporters. Accessed on 06/07/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=188.
Concise Guide to PHARMACOLOGY citation:
Alexander SPH, Kelly E, Mathie A, Peters JA, Veale EL, Armstrong JF, Faccenda E, Harding SD, Pawson AJ, Sharman JL, Southan C, Davies JA; CGTP Collaborators. (2019) The Concise Guide to PHARMACOLOGY 2019/20: Transporters. Br J Pharmacol. 176 Issue S1: S397-S493.
This work is licensed under a Creative Commons Attribution-ShareAlike 4.0 International License
MCT1 and MCT2, but not MCT3 and MCT4, are inhibited by CHC, which also inhibits members of the mitochondrial transporter family, SLC25.
MCT5-MCT7, MCT9 and MCT11-14 are regarded as orphan transporters.