Kyung Sook Lee, 53Schaumburg, IL

2011007, Mar 31, 2011

May 15, 2009

12/992887

Kyung S. Lee - Gaithersburg MD, US
Jung Eun Park - Bethesda MD, US

The U.S.A. as Represented by the Secretary , Dept.of Health and Human Services (the Gov.) - Bethesda MD

G01N 33/573
C07K 14/00
C07K 7/06
C07K 7/08
C12Q 1/48
G01N 33/53

435 74, 530325, 530350, 530328, 530326, 530324, 530327, 536 231, 435 15, 435 71

Isolated peptide substrates of Plk1 and nucleic acids encoding these peptides are disclosed. The peptides include two to ten repeats of the amino acid sequence set forth as XXAXXXPLHSTXXXXXXX(SEQ ID NO: 1), in which within each repeat X, X, X, X, X, X, X, X, and Xare each independently any amino acid or no amino acid, and Xand Xare each independently any amino acid. Methods of using these peptides to detect Plk1 activity in a sample are also disclosed. In some examples, the method includes contacting a sample with a disclosed peptide substrate of Plk1 in the presence of adenosine triphosphate, or an analog thereof, for a period of time sufficient for Plk1 to phosphorylate the PBIPtide. The presence and/or amount of the phosphorylated and/or the unphosphorylated peptide is detected, thereby detecting and/or quantitating Plk1 kinase activity in the sample.

2016003, Feb 11, 2016

Mar 14, 2014

14/776512

- Rockville MD, US
Jung Eun Park - Bethesda MD, US
Christopher C. Lai - Ellicott City MD, US
James A. Kelley - Silver Spring MD, US
Kyung S. Lee - Gaithersburg MD, US

C07K 7/06
C07F 9/40
C07K 1/06
C07F 9/141

The invention provides novel compounds that may serve as anticancer therapeutics. The compounds of the invention bind to polo-like kinases through the polo-box domain. In certain embodiments, the compounds of the invention are POM-protected peptide derivatives. The use of cationic bis-alkyl his residues in combination with a mono POM-protected pho-phoryl group results in a peptide possessing an overall neutral charge. The peptide derivatives of the invention have achieved both good efficacy and an enhanced bioavailability. The invention also provides methods of use, compositions, and kits thereof. Further, the invention provides a novel method of design and/or synthesis of phosphoryl-derived peptide derivatives useful as therapeutic agents.