US 8,148,321 B2Granted

Bioconjugates as therapeutic agent and synthesis thereof

AssigneeNational Institute of Immunology

InventorsRajendra Prasad Roy, Sharmishtha Samantaray

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Abstract

The present disclosure relates to a novel enzymatic approach according to the invention using an unprecedented sortase-catalyzed transpeptidation reaction between a substrate comprising LPXTG (SEQ ID NO: 11) peptide motif and biomolecules such as aminosugars, hydroxyamino acids, hydroxyamino acid esters, aminolipids, polyamines; nucleic acids or derivatives thereof; or any molecule having such moieties; or any compound having such moieties to obtain a bioconjugates useful for target delivery of a compound. The present disclosure provides bioconjugates obtained by the novel sortase catalysed transpeptidedation reaction.

Claims15

Dependent claims

A novel therapeutic and diagnostic bioconjugate useful for target delivery of a compound, wherein said bioconjugate comprising:

a. a substrate comprising LPXTG (SEQ ID NO:
11) peptide motif capable of recognizing sortase, wherein said substrate is selected from a group consisting of peptides, polypeptides, proteins, glycoprotein, lipoprotein, antibodies, radionucleotides, fluorophores, ligand chromophore and any compound comprising the LPXTG (SEQ ID NO:
11) peptide motif;
and
b. a biomolecule that is an aminoglycoside having a 6-Deoxy-6-amino-hexose moiety, wherein the glycine moiety of the LPXTG (SEQ ID NO:
11) motif is cleaved and the substrate is attached to the biomolecule via an amide bond between the resulting terminal threonyl carboxylate and the biomolecule to form the bioconjugate.

3 more elements

Dependencies are inferred from the claim text.

Facts

Application: 12/234,233Filed 19 Sep 2008 · continuation
Priority: IN 797/DEL/200622 Mar 2006
Published: US 2009/0088372 A12 Apr 2009
Granted: 3 Apr 2012
Term ends: Not estimatedThe source records don’t support an estimate.

Classification8 codes

A61K 47/67
The modifying agent being a pre-targeting system involving a peptide or protein for targeting specific cells: enzyme prodrug therapy, e.g. gene…
A61K 47/552
The modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug: one of the codrug's…
A61K 47/645
Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is…:…
A61P 31/12
Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics: antivirals

Family

PCT/IN2007/000115Parent of this continuation · filed 21 Mar 2007
US 2009/0088372 A1Pre-grant publication · published 2 Apr 2009
US 8,148,321 B2This patent

From the US filing history. Foreign family members aren’t listed.

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