IP Library Granted Patent US 10,814,008
Granted Patent B2
US 10,814,008 · App. 15/891,397 · Granted Oct 27, 2020

Chemical crosslinkers

Inventor: Hung Do (New Hope, PA)
Assignee: Amicus Therapeutics, Inc.
A61K47/64A61K38/30A61K38/47A61K47/60C07K14/65C12N9/16C12N9/20C12N9/2402C12N9/2408C12N9/2434C12N9/2465C12N9/2488C12N9/96C07K2319/00C12Y302/0102
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Quick Facts
Patent No.
US 10,814,008
App. No.
15/891,397
Granted
Oct 27, 2020
Kind
B2
Abstract

Disclosed herein are methods of chemical conjugation comprising contacting a lysosomal enzyme with a first crosslinking agent to introduce aldehyde groups; contacting a lysosomal targeting peptide with a second crosslinking agent to introduce a hydrazide group at the N-terminal residue; contacting the lysosomal enzyme with aldehyde groups of step a. with the lysosomal targeting peptide with a hydrazide group at the N-terminal residue of step b; and forming a lysosomal enzyme-lysosomal targeting peptide conjugate.

Claims (12)

1. A lysosomal targeting peptide, comprising a variant human IGF-2 having the sequence set forth in SEQ ID NO:1 with the following modifications:

deletion of amino acids 1-4,

substitution of arginine for glutamic acid at position 6,

substitution of leucine for tyrosine at position 27;

and optionally the following modifications:

substitution of arginine for lysine at position 65.

2. The lysosomal targeting peptide of claim 1 , comprising the amino acid sequence of SEQ ID NO:2.

3. The lysosomal targeting peptide of claim 1 or 2 , further comprising a linker.

4. The lysosomal targeting peptide of any of claim 1 , wherein the variant human IGF-2 comprises the amino acid sequence of SEQ ID NO:3.

5. The lysosomal targeting peptide of any of claim 1 , wherein the variant human IGF-2 comprises the amino acid sequence of SEQ ID NO:4.

6. The lysosomal targeting peptide of any of claim 3 , wherein the linker is at the N-terminal end of the variant human IGF-2.

7. The lysosomal targeting peptide of any of claim 3 , wherein the linker is at the C-terminal end of the variant human IGF-2.

Assignments (3)
SECURITY INTEREST Recorded Apr 27, 2026
From: BIOMARIN PHARMACEUTICAL INC.; AMICUS THERAPEUTICS, INC.
To: CITIBANK, N.A., AS COLLATERAL AGENT
Reel/Frame 075493/0968 →
RELEASE OF SECURITY INTEREST Recorded Apr 27, 2026
From: WILMINGTON TRUST, NATIONAL ASSOCIATION
To: AMICUS THERAPEUTICS, INC.
Reel/Frame 075494/0030 →
SECURITY INTEREST Recorded Oct 6, 2023
From: AMICUS THERAPEUTICS, INC.
To: WILMINGTON TRUST, NATIONAL ASSOCIATION
Reel/Frame 065177/0196 →