Combinatorial Purine Libraries As Inhibitors Of Cyclin Dependent Kinases
- 技術應用
- Inhibitors for protein kinasesAnalysis of signal transduction pathwaysTherapeuticsLicenses are available in fields EXCEPT for neurodegenerative disease
- 詳細技術說明
- None
- *Abstract
-
Abstract:
Selective protein kinase inhibitors were developed on the basis of the unexpected binding mode of 2,6,9-trisubstituted purines to the adenosine triphosphate-binding site of the human cyclin-dependent kinase 2 (CDK2). By iterating chemical library synthesis and biological screening, potent inhibitors of the human CDK2-cyclin A kinase complex and of Saccharomyces cerevisiae Cdc28p were identified. "Exploiting Chemical Libraries, Structure, and Genomics in the Search for Kinase Inhibitors," Peter Schultz et. al., Science, vol. 281, July 24, 1998, 533-537
The invention relates to purine analogs that inhibit, inter alia, protein kinases, G-proteins and polymerases. In addition, the present invention relates to methods of using such purine analogs to inhibit protein kinases, G-proteins, polymerases and other cellular processes and to treat cellular proliferative diseases. The generation of selective inhibitors for specific protein kinases may provide new tools for analyzing signal transduction pathways and possibly new therapeutic agents.
Applications:
? Inhibitors for protein kinases Analysis of signal transduction pathways Therapeutics Licenses are available in fields EXCEPT for neurodegenerative disease
Features/Benefits:
? The most potent inhibitor, purvalanol B(IC50 = 6 nM), binds with a 30-fold greater affinity than the known CDK2 inhibitor, flavopiridol.
- *IP Issue Date
- Jul 3, 2001
- *Principal Investigation
-
Name: Nathanael Gray
Department:
Name: SUNG HOU KIM
Department:
Name: DAVID LOCKHART
Department:
Name: LAURENT MEIJER
Department:
Name: Peter Schultz
Department:
Name: LISA WODICKA
Department:
- 附加資料
- Patent Number: US6255485B1
Application Number: US1998130255A
Inventor: Gray, Nathanael S. | Schultz, Peter | Kim, Sung Hou | Meijer, Laurent
Priority Date: 7 Aug 1997
Priority Number: US6255485B1
Application Date: 6 Aug 1998
Publication Date: 3 Jul 2001
IPC Current: A61K003152 | A61P002528 | A61P003500 | C07D047316
US Class: 544277
Assignee Applicant: The Regents of the University of California | Centre National de la Recherche Scientifique,Paris
Title: Purine inhibitors of protein kinases, G proteins and polymerases
Usefulness: Purine inhibitors of protein kinases, G proteins and polymerases
Summary: USE (I) are used in the treatment of atherosclerosis, solid tumours and tumour metastasis, benign tumours, e.g. hemangiomas, acoustic neuromas, neurofibromas, trachomas, and pyogenic granulomas, vascular malfunctions, abnormal wound healing, immune and inflammatory disorders, Bechet's disease, gout, gouty or rheumatoid arthritis, psoriasis, diabetic or other retinopathy, macular degeneration, corneal graft rejection, neuroscular glaucoma, Oster-Webber syndrome, restenosis, or fungal, parasitic, and viral infections. Typical tumours inhibited are those of lung, breast, colon, ovary, prostate, and hepatic cells. They are also used in the treatment of neurodegenerative diseases such as Alzheimer's, Alper's, and Leigh's diseases, AIDS-related dementia, Lewy body disease, epilepsy, multiple system atrophy, Guillain-Barre syndrome, lipofuchsinosis, Down's syndrome, and vertigo. (I) are used to treat laboratory and farm animals and domestic pets, and even inhibition of undesirable growth of plants. (I) can also be used as molecular tools and probes in research. They can be used alone, or in combination therapy with other, known, drugs, particularly chemotherapeutic and antineoplastic compounds.
Novelty: New 6-Arylamino-2-hydroxyalkylaminopurine derivatives of olomoucine are cellular kinase, G protein, and polymerase inhibitors, for treating e.g. cancer, arthritis and psoriasis
- 主要類別
- 診斷/治療
- 細分類別
- 癌症/腫瘤
- 申請號碼
- 6255485
- 其他
-
Tech ID/UC Case
18502/1997-072-0
Related Cases
1997-072-0
- 國家/地區
- 美國
