Click here to close
Hello! We notice that you are using Internet Explorer, which is not supported by Xenbase and may cause the site to display incorrectly.
We suggest using a current version of Chrome,
FireFox, or Safari.
Pharm Res
2007 Mar 01;243:575-84. doi: 10.1007/s11095-006-9176-1.
Show Gene links
Show Anatomy links
Transport of nicotinate and structurally related compounds by human SMCT1 (SLC5A8) and its relevance to drug transport in the mammalian intestinal tract.
Gopal E
,
Miyauchi S
,
Martin PM
,
Ananth S
,
Roon P
,
Smith SB
,
Ganapathy V
.
???displayArticle.abstract???
PURPOSE. To examine the involvement of human SMCT1, a Na+-coupled transporter for short-chain fatty acids, in the transport of nicotinate/structural analogs and monocarboxylate drugs, and to analyze its expression in mouse intestinal tract. We expressed human SMCT1 in X. laevis oocytes and monitored its function by [14C]nicotinate uptake and substrate-induced inward currents. SMCT1 expression in mouse intestinal tract was examined by immunofluorescence. [14C]Nicotinate uptake was several-fold higher in SMCT1-expressing oocytes than in water-injected oocytes. The uptake was inhibited by short-chain/medium-chain fatty acids and various structural analogs of nicotinate. Exposure of SMCT1-expressing oocytes to nicotinate induced Na+-dependent inward currents. Measurements of nicotinate flux and associated charge transfer into oocytes suggest a Na+:nicotinate stoichiometry of 2:1. Monocarboxylate drugs benzoate, salicylate, and 5-aminosalicylate are also transported by human SMCTI. The transporter is expressed in the small intestine as well as colon, and the expression is restricted to the lumen-facing apical membrane of intestinal and colonic epithelial cells. Human SMCTI transports not only nicotinate and its structural analogs but also various monocarboxylate drugs. The transporter is expressed on the luminal membrane of the epithelial cells lining the intestinal tract. SMCT1 may participate in the intestinal absorption of monocarboxylate drugs.
Casteels,
Diabetic ketoacidosis.
2003,
Pubmed
Coady,
The human tumour suppressor gene SLC5A8 expresses a Na+-monocarboxylate cotransporter.
2004,
Pubmed
,
Xenbase
Enerson,
Molecular features, regulation, and function of monocarboxylate transporters: implications for drug delivery.
2003,
Pubmed
Eskandari,
Thyroid Na+/I- symporter. Mechanism, stoichiometry, and specificity.
1997,
Pubmed
,
Xenbase
Ganapathy,
Biological functions of SLC5A8, a candidate tumour suppressor.
2005,
Pubmed
Gisbert,
Role of 5-aminosalicylic acid (5-ASA) in treatment of inflammatory bowel disease: a systematic review.
2002,
Pubmed
Gopal,
Sodium-coupled and electrogenic transport of B-complex vitamin nicotinic acid by slc5a8, a member of the Na/glucose co-transporter gene family.
2005,
Pubmed
,
Xenbase
Gopal,
Expression of slc5a8 in kidney and its role in Na(+)-coupled transport of lactate.
2004,
Pubmed
,
Xenbase
Gupta,
SLC5A8 (SMCT1)-mediated transport of butyrate forms the basis for the tumor suppressive function of the transporter.
2006,
Pubmed
Inoue,
Human Na+ -coupled citrate transporter: primary structure, genomic organization, and transport function.
2002,
Pubmed
Inoue,
Human sodium-coupled citrate transporter, the orthologue of Drosophila Indy, as a novel target for lithium action.
2003,
Pubmed
Inoue,
Functional features and genomic organization of mouse NaCT, a sodium-coupled transporter for tricarboxylic acid cycle intermediates.
2004,
Pubmed
,
Xenbase
Inoue,
Structure, function, and expression pattern of a novel sodium-coupled citrate transporter (NaCT) cloned from mammalian brain.
2002,
Pubmed
Itagaki,
Interaction of ibuprofen and other structurally related NSAIDs with the sodium-coupled monocarboxylate transporter SMCT1 (SLC5A8).
2006,
Pubmed
,
Xenbase
Li,
SLC5A8, a sodium transporter, is a tumor suppressor gene silenced by methylation in human colon aberrant crypt foci and cancers.
2003,
Pubmed
MacDermott,
Progress in understanding the mechanisms of action of 5-aminosalicylic acid.
2000,
Pubmed
Martin,
Identity of SMCT1 (SLC5A8) as a neuron-specific Na+-coupled transporter for active uptake of L-lactate and ketone bodies in the brain.
2006,
Pubmed
,
Xenbase
Miyauchi,
Functional identification of SLC5A8, a tumor suppressor down-regulated in colon cancer, as a Na(+)-coupled transporter for short-chain fatty acids.
2004,
Pubmed
,
Xenbase
Panayotova-Heiermann,
Kinetics of steady-state currents and charge movements associated with the rat Na+/glucose cotransporter.
1995,
Pubmed
,
Xenbase
Paroder,
Na(+)/monocarboxylate transport (SMCT) protein expression correlates with survival in colon cancer: molecular characterization of SMCT.
2006,
Pubmed
,
Xenbase
Regueiro,
Diagnosis and treatment of ulcerative proctitis.
2004,
Pubmed
Rodriguez,
Identification and characterization of a putative human iodide transporter located at the apical membrane of thyrocytes.
2002,
Pubmed
Schuette,
Renal transport and metabolism of nicotinic acid.
1986,
Pubmed
Thangaraju,
c/ebpdelta Null mouse as a model for the double knock-out of slc5a8 and slc5a12 in kidney.
2006,
Pubmed
Veech,
Ketone bodies, potential therapeutic uses.
2001,
Pubmed
Wang,
Structure, function, and genomic organization of human Na(+)-dependent high-affinity dicarboxylate transporter.
2000,
Pubmed
,
Xenbase
Xu,
Drug therapy for ulcerative colitis.
2004,
Pubmed
