(12) Patent Application Publication (10) Pub. No.: US 2015/0119330 A1 Mcgee Et Al
US 2015O1 19330A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2015/0119330 A1 McGee et al. (43) Pub. Date: Apr. 30, 2015 (54) SUBSTRATES AND INHIBITORS OF PROLYL Publication Classification OLGOPEPTIDASE AND FIBROBLAST ACTIVATION PROTEIN AND METHODS OF (51) Int. Cl. USE C07K 7/06 (2006.01) (71) Applicant: The Board of Regents of the University C07K5/II (2006.01) of Oklahoma, Norman, OK (US) C07K5/09 (2006.01) (52) U.S. Cl. (72) Inventors: Patrick A. McGee, Oklahoma City, OK CPC ................. C07K 7/06 (2013.01); C07K5/0817 (US); Kenneth W. Jackson, Edmond, OK (US); Victoria J. Christiansen, (2013.01); C07K5/1019 (2013.01) Oklahoma City, OK (US) (21) Appl. No.: 14/398,886 (57) ABSTRACT (22) PCT Filed: May 3, 2013 Inhibitors of fibroblast activation protein alpha (FAP) and (86). PCT No.: PCT/US2013/0395.43 Prolyl Oligopeptidase (POP) are disclosed, along with their S371 (c)(1), use in various therapies related to conditions, diseases, and (2) Date: Nov. 4, 2014 disorders involving abnormal cell proliferation Such as malig nancies and angiogenesis, and in neural disorders such as Related U.S. Application Data Alzheimer's disease. Stalk portions of the inhibitor mol (60) Provisional application No. 61/643,001, filed on May ecules, and substrates of FAP and POP, are also disclosed and 4, 2012, provisional application No. 61/793,183, filed may be used, for example, in screening methods for identify on Mar. 15, 2013. ing Such inhibitors. US 201S/O119330 A1 Iaun3]+. ;0zzzzzzzzzzzzzzzzzzzzzzzzzzzzzzzzzzzzzzzzzz… Patent Application Publication Apr. 30, 2015 Sheet 2 of 11 US 201S/O119330 A1 §§§§§§§§§§§ §§§§§§§§§§§§)§§§§§3 §§§§§§§§§§¶¡¿$¢$$$$$$§§§§§ $$$ §28, $$¢£€$£§§§§§§§§ §§§§§§§§§§§§§§§§§§ ? §§?ae, § § §§§§§§§§§§§§§§§§§§§§§??$$§§§§§§§§§§§§ $ §§§§§§§§§§§§§§§ a.
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