The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Oct. 11, 2022

Filed:

Sep. 09, 2019
Applicant:

The Board of Trustees of the Leland Stanford Junior University, Stanford, CA (US);

Inventors:

Jennifer R. Cochran, Stanford, CA (US);

Jun Woo Kim, Mountain View, CA (US);

Frank V. Cochran, Stanford, CA (US);

Attorneys:
Primary Examiner:
Int. Cl.
CPC ...
A61K 38/00 (2006.01); A61K 47/64 (2017.01); A61P 35/00 (2006.01); C07K 14/47 (2006.01); C07K 14/81 (2006.01);
U.S. Cl.
CPC ...
C07K 14/4702 (2013.01); A61K 47/64 (2017.08); C07K 14/811 (2013.01); A61K 38/00 (2013.01); C07K 2319/00 (2013.01); C07K 2319/33 (2013.01);
Abstract

Disclosed are knottin peptides containing non-natural amino acids so that they can be formed by chemical conjugation into two or more knottin monomers. The knottin monomers comprise a non-natural amino acid such as an aminooxy residue within the polypeptide sequence. The exemplified dimers were produced by oxime formation between two aldehyde groups present on a polyether linker and an aminooxy functional group that was site-specifically incorporated the knottin. Knottins variants based on EETI (trypsin inhibitor) and AgRP (Agouti-related protein) were engineered to contain integrin-binding loops. These dimers were shown to have increased binding strength to integrins on U87MG tumor cells, achieving significant increases in inhibition of cell adhesion and proliferation. Also disclosed are knottin monomers comprising an aminooxy residue; these may be conjugated to molecules such as doxorubicin.


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