A new approach to the chemical synthesis of keto-proteins |
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Authors: | Tumelty David Carnevali Maia Miranda Les P |
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Affiliation: | Gryphon Therapeutics, 600 Gateway Boulevard, South San Francisco, CA 94080, USA. |
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Abstract: | To increase the versatility of protein-conjugation, an orthogonal protection strategy is described, which enables the efficient synthesis of keto-proteins bearing a reactive ketone functionality using Boc, Fmoc, and chemical ligation methodologies. A 1,3-dithiolane group was used to protect the ketone function of levulinate- and pyruvate-derivatized peptides during solid-phase synthesis, acidolytic cleavage, and purification. When required, the 1,3-dithiolane group could be cleanly removed using aqueous silver or mercuric solutions to regenerate the reactive keto-protein at ambient temperature. The liberated keto-protein was chemoselectively conjugated in situ to an aminooxy-derivatized monodisperse polymer. |
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