Discovery of an Aurora kinase inhibitor through site-specific dynamic combinatorial chemistry.

Discovery of an Aurora kinase inhibitor through site-specific dynamic combinatorial chemistry. Research Abstract Details 

Research Abstract Table of Contents

Jump to the:

Discovery of an Aurora kinase inhibitor through site-specific dynamic combinatorial chemistry. Abstract Text:

We demonstrate a fragment-based lead discovery method that combines site-directed ligand discovery with dynamic combinatorial chemistry. Our technique targets dynamic combinatorial screening to a specified region of a protein by using reversible disulfide chemistry. We have used this technology to rapidly identify inhibitors of the drug target Aurora A that span the purine-binding site and the adaptive pocket of the kinase. The binding mode of a noncovalent inhibitor has been further characterized through crystallography.

Discovery of an Aurora kinase inhibitor through site-specific dynamic combinatorial chemistry. Publishing Authors By Initials

For similar abstracts research abstracts see: abstracts research

PUBMED ID PMID:

MEDLINE DATE:

Discovery of an Aurora kinase inhibitor through site-specific dynamic combinatorial chemistry. Journal Published:

PUBLICATION TYPE: Journal Article

Journal: Bioorganic & medicinal chemistry letters

VOLUME: 18

Page Numbers: 3978-81

Journal Abbreviation: Bioorg. Med. Chem. Lett.

ISSN: 1464-3405

DAY: 10

MONTH: 06

YEAR: 2008

Discovery of an Aurora kinase inhibitor through site-specific dynamic combinatorial chemistry. Information

Number of References:

LANGUAGE: eng

NlmUniqueID: 9107377

Discovery of an Aurora kinase inhibitor through site-specific dynamic combinatorial chemistry. Keywords Mesh Terms:

KEYWORDS:

MESH TERMS:

Chemical & Substance for Abstract: Discovery of an Aurora kinase inhibitor through site-specific dynamic combinatorial chemistry. Information

Substance Name:

Registry Number:

Grant and Affiliation Information for Discovery of an Aurora kinase inhibitor through site-specific dynamic combinatorial chemistry.

AFFILIATION: Sunesis Pharmaceuticals, Inc., 395 Oyster Point Boulevard, Suite 400, South San Francisco, CA 94080, USA.

Country: England

AGENCY:

GRANT:

ACRONYM:

MEDLINETA: Bioorg Med Chem Lett

REFSOURCE:

DATABASENAME:

ACCESSION NUMBER:

Number Hits: 0

Discovery of an Aurora kinase inhibitor through site-specific dynamic combinatorial chemistry Related Publications

• Determination of the sensitivity in vitro of bacteria to chemotherapeutic agents.
• Discovery of an Aurora kinase inhibitor through site-specific dynamic combinatorial chemistry.
• Effect of chemotherapy and evaluation of sensitivity test in vitro in surgical urinary infections.
• Fragment-based ligand discovery meets phage display.
• Thermal integration of electric power and life support systems for manned space stations. NASA CR-543.