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| - Screening for Galectin-3 Inhibitors from Synthetic Lacto-N-bioseLibraries Using Microscale Affinity Chromatography Coupled toMass Spectrometry
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| - The synthesis and screening of two β-d-Galp-(1-3)-β-d-GlcpN (lacto-N-biose) disaccharide libraries arereported. Solution-phase synthetic modifications at the HO-2‘ and NH positions were performed in aneffort to enhance the affinity toward galectin-3, a galactose-binding protein involved in tumor metastasis,apoptosis, and inflammation. The libraries were screened for galectin-3 binding by microscale frontalaffinity chromatography coupled to mass spectrometry (FAC/MS) allowing for rapid ranking of the differentinhibitors and the determination of the galectin-3 binding Kd's. Compounds bearing a hydrophobicsubstituent on the NH group showed the highest affinity for the lectin. The N-naphthoyl derivative (Kd= 10.6 μM) was the best inhibitor with a 7 times increased affinity as compared to the N-acetyl parentcompound (Kd = 73.3 μM).
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