INTRACELLULAR KINASE INHIBITORS

PROBLEM TO BE SOLVED: To provide intracellular kinase inhibitors and use of the same for patients having T cell malignant diseases, B cell malignant diseases, autoimmune disorders, and transplanted organs.SOLUTION: Provided is a protein kinase inhibitor that binds to a DKC triad kinase active site,...

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Main Authors FLYNN GARY A, MARY FARIS, LEE SANDRA AEYOUNG, BRANDT DAVID WILLIAM, SUBRATA CHAKRAVARTY
Format Patent
LanguageEnglish
Published 29.05.2014
Subjects
BEER
BIOCHEMISTRY
CHEMISTRY
COMPOSITIONS THEREOF
CULTURE MEDIA
ENZYMOLOGY
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
MICROBIOLOGY
MICROORGANISMS OR ENZYMES
MUTATION OR GENETIC ENGINEERING
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
PROPAGATING, PRESERVING OR MAINTAINING MICROORGANISMS
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
SPIRITS
VINEGAR
WINE
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Summary:PROBLEM TO BE SOLVED: To provide intracellular kinase inhibitors and use of the same for patients having T cell malignant diseases, B cell malignant diseases, autoimmune disorders, and transplanted organs.SOLUTION: Provided is a protein kinase inhibitor that binds to a DKC triad kinase active site, comprising (a) a proton acceptor arranged at a kinase active site within the distance of hydrogen bond in relation to amino group of lysines of tuple catalysts at the kinase active site, (b) an abstractable proton in hydrogen bond adjacent to aspartic acids of tuple catalysts at the kinase active site, (c) a leaving group produced by elimination due to further electron transposition, thereby forming Michael acceptor in the inhibitor, and (d) a kinase binding portion having affinity to a part of ATP binding site selected from the group consisting of a kinase hinge region, some hydrophobic residues, hydrophilic residues, and their combinations.
Bibliography:Application Number: JP20140010925