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:
May. 20, 2014

Filed:

May. 12, 2010
Applicants:

Huib Ovaa, Amsterdam, NL;

Farid El Oualid, Amsterdam, NL;

Inventors:

Huib Ovaa, Amsterdam, NL;

Farid El Oualid, Amsterdam, NL;

Attorney:
Primary Examiner:
Assistant Examiner:
Int. Cl.
CPC ...
A61K 38/02 (2006.01); C07K 2/00 (2006.01); C07C 319/24 (2006.01); C12P 21/00 (2006.01); G01N 21/00 (2006.01); C07C 323/60 (2006.01); C07K 1/06 (2006.01);
U.S. Cl.
CPC ...
A61K 38/02 (2013.01);
Abstract

The present invention concerns new thiolysine and selenolysine compounds that can be used as building blocks for peptides and proteins, providing ligation handles for site- and chemoselective modification of said peptides and proteins. In particular, the invention provides. In particular, the invention provides (the use of) the compounds 5-thiolysine (also referred to as δ-thiolysine); 4-thiolysine (also referred to as γ-thiolysine); 5-selenolysine (also referred to as δ-selenolysine) and 4-selenolysine (also referred to as γ-selenolysine). The positioning of the thiol or selenol group at the respective carbon atom allows for a very efficient intramolecular transfer reaction to take place after conjugation with a selected ligand, and the thiol or selenol group may subsequently be removed using reported procedures, thereby restoring the native lysine structure, or be used as an additional conjugation handle. The methodology is fast and gives well-defined material.


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