ArticleThe Biochemical journal1993
Characterization of the inhibition by stilbene disulphonates and phloretin of lactate and pyruvate transport into rat and guinea-pig cardiac myocytes suggests the presence of two kinetically distinct carriers in heart cells.
Article in The Biochemical journal, 1993. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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13 citing papers in PubMed, 54 citations in OpenAlex.
- Functional and molecular mechanism of intracellular pH regulation in human inducible pluripotent stem cells.World journal of stem cells · 2018Article
- Essential Roles of Lactate in Müller Cell Survival and Function.Molecular neurobiology · 2018Article
- Global gene expression in pseudomyxoma peritonei, with parallel development of two immortalized cell lines.Oncotarget · 2015Article
- Regulation of oligodendrocyte development and myelination by glucose and lactate.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2011Article
- The proton-linked monocarboxylate transporter (MCT) family: structure, function and regulation.The Biochemical journal · 1999Review
- Identification and characterization of a monocarboxylate transporter (MCT1) in pig and human colon: its potential to transport L-lactate as well as butyrate.The Journal of physiology · 1998Article
- NO3--induced pH changes in mammalian cells. Evidence for an NO3--H+ cotransporter.The Journal of general physiology · 1997Article
- Effect of Hoe 694, a novel Na(+)-H+ exchange inhibitor, on intracellular pH regulation in the guinea-pig ventricular myocyte.British journal of pharmacology · 1996Article
- The mitochondrial inner membrane anion channel is inhibited by DIDS.Journal of bioenergetics and biomembranes · 1996Article
- Chronic muscle stimulation increases lactate transport in rat skeletal muscle.Molecular and cellular biochemistry · 1996Article
- The kinetics, substrate and inhibitor specificity of the lactate transporter of Ehrlich-Lettre tumour cells studied with the intracellular pH indicator BCECF.The Biochemical journal · 1994Article
- The Role of Monocarboxylate Transporters and Their Chaperone CD147 in Lactate Efflux Inhibition and the Anticancer Effects ofEuropean journal of medicinal plantsArticle
- The effects of lactic acid production on contraction and intracellular pH during hypoxia in cardiac muscle.Basic research in cardiologyArticle
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4 authors at 1 institution in 1 country.
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Abstract
1. The kinetics of transport of pyruvate (Km 0.20 mM), L-lactate (Km 2.2 mM) and D-lactate (Ki 10.2 mM) into rat cardiac myocytes were studied and compared with those for guinea-pig heart cells [Poole, Halestrap, Price and Levi (1989) Biochem. J. 264, 409-418] whose equivalent values were 0.07, 2.3 and 6.6 mM respectively. Maximal rates of transport were about 5-fold higher in the rat heart cells. 2. 4,4'-Dibenzamidostilbene-2,2'-disulphonate (DBDS), a powerful inhibitor of monocarboxylate transport into erythrocytes [Poole & Halestrap (1991) Biochem. J. 275, 307-312], was found to be a potent but apparently partial inhibitor of lactate and pyruvate transport, with an apparent Ki value at 0.5 mM L-lactate of about 16 microM in both species. Maximal inhibition was 50% and 80% in rat and guinea-pig cells respectively. 3. The maximal extent of inhibition and apparent Ki values were dependent on both the substrate transported and its concentration. Maximum inhibition was less and the Ki was greater at higher substrate concentrations. 4. A variety of other stilbene disulphonates were studied which showed different Ki values and maximal extents of inhibition. 5. Phloretin was a significantly less potent inhibitor of transport into both rat (Ki 25 microM) and guinea-pig (Ki 16 microM) heart cells than into rat erythrocytes (Ki 1.4 microM). In the rat but not the guinea-pig heart cells, inhibition appeared partial (maximal inhibition 84%). 6. We demonstrate that our results can be explained by the presence of two monocarboxylate carriers in heart cells, both with Km values for L-lactate of about 2 mM and inhibited by alpha-cyano-4-hydroxycinnamate, but with different affinities for other substrates and inhibitors. One carrier is sensitive to inhibition by stilbene disulphonates and has lower Km values for pyruvate (0.05-0.10 mM) and D-lactate (5 mM), whereas the other has higher Km values for pyruvate (0.30 mM) and D-lactate (25 mM), and is relatively insensitive to stilbene disulphonates. Rat heart cells possess more of the latter carrier and guinea-pig heart cells more of the former. 7. The significance of these results for the study of lactate transport in the perfused heart is discussed.
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