CNT1
CNT1 (SLC28A1) is a high-affinity, pyrimidine-preferring concentrative nucleoside transporter that imports nucleosides through a sodium-dependent mechanism[1]. Mechanistically, CNT1 supports nucleoside salvage and cellular handling of pyrimidine nucleosides, while CNT2 preferentially transports purine nucleosides and CNT3 shows broader substrate selectivity with sodium- and proton-coupled transport[1][2]. In disease and experimental models, SLC28A1 disruption causes increased urinary uridine and cytidine excretion in humans, defining uridine-cytidineuria as a CNT1-related inborn error of metabolism[3]. Consistently, CNT1 knockout mice show increased renal elimination of endogenous pyrimidine nucleosides and the synthetic nucleoside analog gemcitabine, linking CNT1 function to renal reabsorption and nucleoside-analog pharmacology[4]. Compared with equilibrative nucleoside transporters, CNT proteins are inwardly directed sodium-dependent transporters, whereas ENTs mediate bidirectional nucleoside flux down concentration gradients[2]. For experimental applications, hCNT1 transports AZT and d4T with low affinity, does not translocate 3TC or ddC, and shows substrate selectivity strongly affected by small ribose-ring structural changes[5].
References:
- [1]. Pastor-Anglada M, et al. SLC28 genes and concentrative nucleoside transporter (CNT) proteins. Xenobiotica. 2008 Jul;38(7-8):972-94. [Content Brief]
- [2]. Young JD. The SLC28 (CNT) and SLC29 (ENT) nucleoside transporter families: a 30-year collaborative odyssey. Biochem Soc Trans. 2016 Jun 15;44(3):869-76. doi: 10.1042/BST20160038. PMID: 27284054. et al. The SLC28 (CNT) and SLC29 (ENT) nucleoside transporter families: a 30-year collaborative odyssey. Biochem Soc Trans. 2016 Jun 15;44(3):869-76. [Content Brief]
- [3]. Wevers RA, et al. Functional disruption of pyrimidine nucleoside transporter CNT1 results in a novel inborn error of metabolism with high excretion of uridine and cytidine. J Inherit Metab Dis. 2019 May;42(3):494-500. [Content Brief]
- [4]. Persaud AK, et al. Increased renal elimination of endogenous and synthetic pyrimidine nucleosides in concentrative nucleoside transporter 1 deficient mice. Nat Commun. 2023 Jun 1;14(1):3175. [Content Brief]
- [5]. Cano-Soldado P, et al. Interaction of nucleoside inhibitors of HIV-1 reverse transcriptase with the concentrative nucleoside transporter-1 (SLC28A1). Antivir Ther. 2004;9(6):993-1002.
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CNT1 Related Products (2)
Related Products (2)
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dMeThPmR
0 ImagesCat. No.: HY-177747CAS No.: 1262032-37-0dMeThPmR, a ribonucleoside derivative, is a potent and selective human nucleoside transporter 1 (hCNT1) inhibitor (Ki = 0.3-0.98 μM). dMeThPmR exhibit weak inhibitory activity on hCNT2 (IC50 = 133 μM) and hCNT3 (Ki = 32.7 μM). dMeThPmR can protect cells from the toxicity of nucleoside drugs. dMeThPmR can be used for the research of cancer.
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MeThPmR
0 ImagesCat. No.: HY-177746CAS No.: 1262032-38-1MeThPmR, a ribonucleoside derivative, is a potent and selective human nucleoside transporter 1 (hCNT1) inhibitor (Ki/sub> = 0.16-0.69 μM). MeThPmR exhibit weak inhibitory activity on hCNT2 (IC50 = 360 μM) and hCNT3 (Ki = 4.7 μM). MeThPmR can protect cells from the toxicity of nucleoside drugs. MeThPmR can be used for the research of cancer.
