PubMed · 13232632
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C E BERRY. 1955. Construction; pro's & con's.. https://pubmed.ncbi.nlm.nih.gov/13232632/
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Measurements of fluorescence resonance energy transfer efficiency (E), via fluorescence polarization, have been applied to distinguish between chronic lymphocytic leukemia (CLL) patients and healthy persons. Capping of Concanavalin-A receptors is more pronounced in normal lymphocytes than in those of CLL patients. Membrane capping decreases the distance between donor and acceptor molecules embedded in the membrane (r), and thus increases the monitored energy transfer efficiency (E approximately 1/r6). Blood samples of 10 healthy subjects and 16 CLL patients were examined. In the healthy subjects, the mean E value for capped lymphocytes was 19 +/- 3, whereas in the CLL patients it was significantly lower (8 +/- 5) (P < 0.01).
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Dendritic beta-cyclodextrin (betaCD) derivatives bearing multivalent mannosyl ligands have been prepared and assessed for their binding efficiency toward the tetrameric plant lectin concanavalin A (Con A) and a mammalian mannose/fucose specific cell surface receptor from macrophages. The synthetic strategy exploits the reactivity between isothiocyanate and amine functionalities for the high-yielding assembly via thioureido links of the various building blocks, including host, spacer, branching, and carbohydrate ligand elements. The methodology has been applied to the preparation of a series of betaCD-polymannoside scaffolds differing in the ligand valency and geometry. This series allowed us to explore: (i) The effects of the glycodendritic architecture on the binding efficiency; (ii) the mutual influence between the cyclodextrin core and the glycodendritic moieties on the molecular inclusion and lectin-binding properties; and (iii) the consequence of inclusion complex formation, using the anticancer drug docetaxel (Taxotère) as a target guest, on biological recognition. Our results confirm the high drug solubilization capability of this new type of betaCD-dendrimer construct and indicate that subtle changes in the architecture of the conjugate may have important consequences on receptor affinity. Interestingly, the host-guest interaction can be monitored to build up supramolecular dynamic glycoclusters with increased lectin affinity. Alternatively, the information obtained from the structure-lectin-binding avidity-inclusion capability studies has been put forward in the design of very efficient molecular transporters for docetaxel based on glycodendritic CD dimers.