Monocarboxylate Transporter
Monocarboxylates such as pyruvate, lactate, and the ketone bodies (acetoacetate and b-hydroxybutyrate) play essential roles in carbohydrate, fat, and amino acid metabolism and must be rapidly transported across the plasma membrane of cells. Transport is mediated by proton-linked monocarboxylate transporters (MCTs), four of which (MCTs1–4) have been characterized in detail. They are part of a family of transporter proteins, known as the MCT or SLC16 solute carrier family, that share characteristic sequence motifs. All family members are predicted to have 12-transmembrane helices (TMs) with intracellular C- and N-termini and a large cytosolic loop between TMs 6 and 7. As in other major facilitator superfamily members, the TM regions are more conserved than the loops and C-terminus. The MCT family has a total of 14 members whose predicted phylogeny, only MCTs1–4 have been confirmed to function as proton-linked MCTs. MCT10 was identified as an aromatic amino acid transporter originally called T-type amino acid transporter 1 (TAT1) and MCT8 shown to be an important thyroid hormone transporter. Transport mediated by MCT8 and MCT10 is not proton linked. The function of the other eight MCTs is unknown. In addition to their normal metabolic roles, MCTs may also be important for the transport of some drugs across the plasma membrane. There are also two distinct sodium-linked monocarboxylate transporters that are members of the SLC5 solute carrier family. These play a key role in endothelial monocarboxylate transport in the gut and kidney.
References
1.Halestrap AP. IUBMB Life. 2012;64(1):1–9.
References
1.Halestrap AP. IUBMB Life. 2012;64(1):1–9.
Membrane Transporter/Ion Channel
AMPK(58)
ASBT Transporter(6)
BCRP(10)
Beta Amyloid(69)
Carbonic Anhydrase(40)
Chloride Channel(34)
CRAC Channel(0)
CRM1(5)
Exportin-1(5)
FABP(6)
GAT(63)
GLUT(5)
Glutamate Transporter(1)
GlyT(13)
HCN Channel(5)
iGluR(52)
Monoamine Transporter(26)
Monocarboxylate Transporter(12)
MTP(1)
nAChR(5)
NADPH(35)
Na-K-ATPase(2)
NKCC(4)
NMDAR(65)
OCT(4)
Other Targets(13)
P2X Receptor(23)
P-glycoprotein(14)
Proton Pump(38)
Sodium Channel(147)
TRP/TRPV Channel(115)
URAT1(1)
Monocarboxylate Transporter
-
Coumarin343
catalog no : M36948
cas no: 55804-65-4
Coumarin343 inhibits monocarboxylic acid transporter protein 4 with IC50 values in the range of 0.01-100 μM. -
MCT1-IN-3
catalog no : M35939
cas no: 2878360-80-4
MCT1-IN-3 is a monocarboxylate transporter 1 (MCT1) inhibitor, targeting solute carrier (SLC) monocarboxylate transporter 1 (MCT1; SLC16A1) for cancer treatment. -
AZD0095
catalog no : M35816
cas no: 2750001-23-9
AZD0095 is a selective inhibitor of MCT4?with an IC50 of 1.3 nM. -
VB124
catalog no : M35358
cas no: 2230186-18-0
VB124 is an orally active, potent and selective MCT4 inhibitor. VB124 blocked lactate import (IC50 value of 8.6 nM) and export (IC50 value of 19 nM) in MDA-MB-231 cells. -
MSC-4381
catalog no : M34984
cas no: 2445185-57-7
MSC-4381 (MCT4-IN-1) is an orally available and selectively modeled highly potent inhibitor of monocarboxylic acid transporter protein 4 (MCT4/SLC16A3) with potential anticancer and antitumor activity for the study of osteosarcoma.