Invention Grant
- Patent Title: Peptide and peptide mimetic binding antagonists of polo-like kinase 1 polo box domain and methods of use
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Application No.: US15977768Application Date: 2018-05-11
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Publication No.: US10905769B2Publication Date: 2021-02-02
- Inventor: Terrence R. Burke, Jr. , David T. Hymel , Kohei Tsuji
- Applicant: The United States of America, as represented by the Secretary, Department of Health & Human Services
- Applicant Address: US MD Rockville
- Assignee: The United States of America, as represented by the Secretary, Department of Health & Human Services
- Current Assignee: The United States of America, as represented by the Secretary, Department of Health & Human Services
- Current Assignee Address: US MD Rockville
- Agency: Locke Lord LLP
- Agent Nicholas J. DiCeglie, Jr.
- Main IPC: A61K38/00
- IPC: A61K38/00 ; A61K47/64 ; C07K7/06 ; A61K31/519 ; A61K31/585 ; C07K7/56 ; C07K7/64

Abstract:
The description provides novel compounds that may serve as anticancer therapeutics. The compounds of the description bind to polo-like kinases through the polo-box domain. The peptide derivatives of the description have achieved improved efficacy in biochemical assays against Plk1. Exemplary compounds of the description include macrocyclic peptidomimetics with high affinity and selectivity for polo-like kinases, which may provide the basis for a new genre of anticancer therapeutics. Other exemplary compounds of the description include bi-valent compounds with that bind to polo-like kinases through both kinase domain and polo-box domain simultaneously by incorporating additional moieties that target Plk1 kinase domain, which significantly enhances affinitity relative and may provide the basis for a new genre of anticancer therapeutics. The description also provides methods of use, methods of preparation, compositions, and kits thereof. Further, the description provides a novel method of design and/or synthesis of phosphoryl-derived peptide derivatives useful as therapeutic agents.
Public/Granted literature
- US20180296686A1 PEPTIDE AND PEPTIDE MIMETIC BINDING ANTAGONISTS OF POLO-LIKE KINASE 1 POLO BOX DOMAIN AND METHODS OF USE Public/Granted day:2018-10-18
Information query
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