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:
Sep. 04, 2018

Filed:

May. 13, 2015
Applicant:

University of South Carolina, Columbia, SC (US);

Inventors:

Campbell McInnes, Irmo, SC (US);

Doaa Boshra Farag, Cairo, EG;

Assignee:

University of South Carolina, Columbia, SC (US);

Attorney:
Primary Examiner:
Assistant Examiner:
Int. Cl.
CPC ...
C12N 9/16 (2006.01); G01N 33/573 (2006.01); A61K 47/48 (2006.01); A61K 38/06 (2006.01); A61K 38/08 (2006.01); C12N 9/12 (2006.01); C07K 5/083 (2006.01); C07K 7/06 (2006.01); G06F 19/18 (2011.01);
U.S. Cl.
CPC ...
G01N 33/573 (2013.01); A61K 38/06 (2013.01); A61K 38/08 (2013.01); A61K 47/48023 (2013.01); A61K 47/48038 (2013.01); A61K 47/48061 (2013.01); C07K 5/081 (2013.01); C07K 7/06 (2013.01); C12N 9/12 (2013.01); C12N 9/16 (2013.01); C12Y 207/11021 (2013.01); G06F 19/18 (2013.01); C07K 2317/34 (2013.01); C12Y 301/03048 (2013.01); G01N 2333/912 (2013.01); G01N 2500/02 (2013.01);
Abstract

Methods for developing non-peptidic inhibitors that target the polo-box domain of PLK1 proteins are described. Methods include developing structure activity relationships for peptidic inhibitors followed by development of non-peptide fragment alternatives for portions of the peptide inhibitors. The non-peptide fragment can provide similar structure activity relationship as the replaced peptide. Fragment alternatives to key binding determinants are identified in an iterative computational and synthetic process facilitated through understanding of the peptide structure-activity relationships. The approach is informed by peptide structure-activity data obtained through synthesis and testing of truncated and mutated analogs of known PBD binding motifs.


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