Acidity-sensitive spacer molecule to control the release of phar

Chemistry: natural resins or derivatives; peptides or proteins; – Proteins – i.e. – more than 100 amino acid residues – Blood proteins or globulins – e.g. – proteoglycans – platelet...

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530345, 5303919, 530404, 530405, 530406, 530408, 530409, 530410, 424 858, 424 8591, 435 71, 435174, 435188, 525 511, 549 60, 549 62, 562512, 210635, C07K 1706, A61K 3944, A61K 4748

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051440113

ABSTRACT:
A method for controlling the release of durgs or other passenger molecules form carrier conjugates, and a class of conjugates that releases drugs when ingested by a cell or subjected to acidic conditions, are disclosed. These conjugates contain a passenger molecule which is attached to a spacer molecule through an acidic bonding group, such as carboxyl, that is in a "cis" configuration with another acidic group, and a carrier molecule that is bonded to the spacer molecule at another site. When subjected to a mild increase in acidity, such as occurs within a lysosome of a cell, the drug or other passenger molecule is hydrolyzed from the the conjugate and released in unmodified, active form.

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