Lectin-directed prodrug delivery system
OwnerBenjamin Guy Davisinventor
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Abstract
The invention provides a kit for lectin-directed prodrug delivery comprising a prodrug and a lectin-directed glycoconjugate, wherein the glycoconjugate is adapted to cleave the prodrug and thereby release the drug. The glycoconjugate generally comprises an enzyme conjugated to a carbohydrate moiety which binds to a lectin. The invention also provides novel gylcoconjugates and novel methods of synthesizing prodrugs.
Claims39
A kit for lectin-directed prodrug delivery, comprising a prodrug and a lectin-directed glycoconjugate, wherein the glycoconjugate is adapted to cleave the prodrug and thereby release the drug.
A kit according to any one of the preceding claims, wherein the glycoconjugate comprises from 1 to 20 sugar residues per site at from 1 to 20 sites.
A kit according to any one of the preceding claims wherein the glycoconjugate comprises an enzyme of the class of rhamnopyranosidases.
A kit according to any one of the preceding claims wherein the enzyme is naringinase.
A kit according to any one of the preceding claims wherein the prodrug is a rhamnoside of an amine, alcohol or thiol.
A kit according to any one of the preceding claims for use in a method of therapy practised on the human or animal body.
A conjugate comprising a rhamnopyranosidase enzyme glycosylated with mannose, galactose, glucose, fucose, N-acetylglucosamine, rhamnose or a combination thereof.
A conjugate selected from:
- wild type naringinase modified by IME-thiogalactoside reagent;
- wild type naringinase modified by IME-thiomannoside reagent;
- wild type naringinase modified by IME-dendrithiogalactoside reagent;
- deglycosylated naringinase, reglycosylated using IME-thiomannoside reagent;
- wild type naringinase modified by IME-thioglycoside reagent;
- wild type naringinase modified by IME-dendrithioglycoside reagent;
- deglycosylated naringinase, reglycosylated using IME-thioglycoside reagent;
- and
- deglycosylated naringinase reglycosylated using IME-dendrithioglycoside reagent;
- wherein IME is 2-imino-2-methoxyethyl.
A method for synthesizing a prodrug comprising a drug moiety and a carbohydrate cap, which comprises contacting the drug in reactive form with a carbohydrate cap donor in the presence of an enzyme.
Use of a rhamnopyranosidase enzyme for the production of a prodrug comprising a drug moiety and an α-rhamnopyranoside cap.
A pure rhamnopyranosidase enzyme.
Dependencies are inferred from the claim text.