Biochemical and Biophysical Research Communications
Regular ArticleInhibition of CMP-Sialic Acid Transport in Human Liver and Colorectal Cancer Cell Lines by a Sialic Acid Nucleoside Conjugate (KI-8110)
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A three-pocket model for substrate coordination and selectivity by the nucleotide sugar transporters SLC35A1 and SLC35A2
2021, Journal of Biological ChemistryCitation Excerpt :Cell surface hypersialylation benefits tumor cell growth and metastasis (12), making SLC35A1 an attractive target for drug design. Indeed, a small-molecule inhibitor of SLC35A1 has been shown to reduce cell surface sialylation and inhibit the metastasis of human colorectal cancer cells within a mouse model (45). Our findings may aid the development of new and specific SLC35A1 inhibitors for chemotherapeutic use.
Synthetic study of 3-fluorinated sialic acid derivatives
2015, Carbohydrate ResearchCitation Excerpt :In fact, the analogs and derivatives of sialic acid have been shown to be potent inhibitors of influenza virus sialidase, and they are commercially available.1,2 Moreover, sialic acid derivatives exhibiting immunoregulatory activity have been reported.3 Given the important functions of a glycan-bearing sialic acid, its derivatives and analogs are expected to become valuable tools for investigating the biological roles of glycoconjugates.
Expression, solubilisation, and purification of a functional CMP-sialic acid transporter in Pichia pastoris
2014, Protein Expression and PurificationCitation Excerpt :The CST is a Golgi-resident type III trans-membrane protein with 8–10 predicted trans-membrane domains (TMDs) that is essential for the transport of CMP-sialic acid into the Golgi apparatus of eukaryotic cells [7–9]. The CST is considered to be an attractive target for drug discovery given that its inhibition reduces cancer cell sialylation and decreases the metastatic potential of cancer cells [10]. However, the further development of more potent inhibitors has been hindered by the lack of 2D- or 3D- crystal structure data for any NST including the CST.
Membrane topology of the mammalian CMP-sialic acid transporter
1999, Journal of Biological Chemistry