35 research outputs found

    Rational steering of insulin binding specificity by intra-chain chemical crosslinking

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    Insulin is a key hormone of human metabolism with major therapeutic importance for both types of diabetes. New insulin analogues with more physiological profiles and better glycemic control are needed, especially analogues that preferentially bind to the metabolic B-isoform of insulin receptor (IR-B). Here, we aimed to stabilize and modulate the receptor-compatible conformation of insulin by covalent intra-chain crosslinking within its B22-B30 segment, using the Cu I -catalyzed Huisgen 1,3-dipolar cycloaddition reaction of azides and alkynes. This approach resulted in 14 new, systematically crosslinked insulin analogues whose structures and functions were extensively characterized and correlated. One of the analogues, containing a B26-B29 triazole bridge, was highly active in binding to both IR isoforms, with a significant preference for IR-B. Our results demonstrate the potential of chemistry-driven modulation of insulin function, also shedding new light on the functional importance of hormones B-chain C-terminus for its IR-B specificity

    Lactose to Naturalize Textile Dyes

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    Many natural dyes, for example carminic acid, are soluble in water. We present a simple strategy to naturalize synthetic azadyes through their linkage with lactose to induce their water solubility. The dyeing process of textile fibres then becomes possible in water without additives such as surfactants and mordants, which result in products that are difficult to eliminate. Glyco-azadyes (GADs) we are presenting here are obtained through a diether linker to bond the azadye and the sugar. Tinctorial test were carried out with fabrics containing wool, polyester, cotton, nylon, and acetate. GADs were found to be multipurpose and capable of dyeing many fabrics efficiently under mild conditions

    Disperse dyes soluble in water

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    • The Application describes disperse dyes sol. in water of formula D-L-Sn wherein: D is a disperse dye insol. in water, L is a linker, S is a sugar, n is comprised between 2 and 4 that are able to dye in an homogeneous way natural fibers and textiles and also textile materials including different fibers, and have high biodegradability through digestion by micro organisms, that found in the mol. itself a useful nourishment for their survival and proliferation; processes for the prepn. of the above said dyes and their use are also describe

    Ethereal Glycoconjugated Azodyes (GADs): A New Group of Water-Soluble, Naturalised Dyes

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    This report deals with azodyes naturalised through glycoconjugation with a very common saccharide -lactose- and with its galactose and glucose components. The conjugation takes place through a bifunctional linker, here a terminal dibromoalkane, so the final products are very stable diether derivatives of the starting dyes. These transformations produce nat uralised dyes -indeed, water-soluble and multipurpose- that are able to dye different materials without addition of chemical additives such as surface agents
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