AI Article Synopsis
- UD29 (4-thio-uridylate) inhibits the enzyme glyceraldehyde 3-phosphate dehydrogenase (GAPDH), likely by interfering with its active center’s essential -SH group.
- The inhibition of GAPDH led to an investigation of UD29's anti-HIV activity, showing it effectively inhibited the replication of HIV-1 strains in laboratory settings.
- UD29 demonstrated low toxicity, as it did not harm peripheral blood mononuclear cells (PBMCs) in vitro or cause adverse effects in mice during intravenous administration.
Article Abstract
In this short communication, it is shown that 4-thio-uridylate (s(4)UMP, designated as UD29) inhibits glyceraldehyde 3-phosphate dehydrogenase (GAPDH), suggesting that the enol-form of the thiolated nucleotide may interfere with the function of the essential -SH group in the active center of the enzyme. Since HIV entry requires thiol/disulfide exchange processes, this activity prompted us to study the anti-HIV activity of the nucleotide. Indeed, UD29 inhibited the replication of HIV-1(IIIB) in the MT-4 cell line and HIV-1(Ada-M) in peripheral blood mononuclear cells (PBMC). Furthermore, UD29 was not toxic in PBMCs in vitro or in mice when the compound was administered intravenously.
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| http://dx.doi.org/10.1016/s1734-1140(09)70042-8 | DOI Listing |
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