1fvv: Difference between revisions
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'''THE STRUCTURE OF CDK2/CYCLIN A IN COMPLEX WITH AN OXINDOLE INHIBITOR'''<br /> | '''THE STRUCTURE OF CDK2/CYCLIN A IN COMPLEX WITH AN OXINDOLE INHIBITOR'''<br /> | ||
==Overview== | ==Overview== | ||
Most traditional cytotoxic anticancer agents ablate the rapidly dividing | Most traditional cytotoxic anticancer agents ablate the rapidly dividing epithelium of the hair follicle and induce alopecia (hair loss). Inhibition of cyclin-dependent kinase 2 (CDK2), a positive regulator of eukaryotic cell cycle progression, may represent a therapeutic strategy for prevention of chemotherapy-induced alopecia (CIA) by arresting the cell cycle and reducing the sensitivity of the epithelium to many cell cycle-active antitumor agents. Potent small-molecule inhibitors of CDK2 were developed using structure-based methods. Topical application of these compounds in a neonatal rat model of CIA reduced hair loss at the site of application in 33 to 50% of the animals. Thus, inhibition of CDK2 represents a potentially useful approach for the prevention of CIA in cancer patients. | ||
==About this Structure== | ==About this Structure== | ||
1FVV is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with 107 as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/Non-specific_serine/threonine_protein_kinase Non-specific serine/threonine protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.1 2.7.11.1] Full crystallographic information is available from [http:// | 1FVV is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=107:'>107</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/Non-specific_serine/threonine_protein_kinase Non-specific serine/threonine protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.1 2.7.11.1] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1FVV OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: Non-specific serine/threonine protein kinase]] | [[Category: Non-specific serine/threonine protein kinase]] | ||
[[Category: Protein complex]] | [[Category: Protein complex]] | ||
[[Category: Benson, B | [[Category: Benson, B G.]] | ||
[[Category: Bramson, H | [[Category: Bramson, H N.]] | ||
[[Category: Chapman, D | [[Category: Chapman, D E.]] | ||
[[Category: Davis, S | [[Category: Davis, S T.]] | ||
[[Category: Dickerson, S | [[Category: Dickerson, S H.]] | ||
[[Category: Dold, K | [[Category: Dold, K M.]] | ||
[[Category: Eberwein, D | [[Category: Eberwein, D J.]] | ||
[[Category: Edelstein, M.]] | [[Category: Edelstein, M.]] | ||
[[Category: Frye, S | [[Category: Frye, S V.]] | ||
[[Category: Griffin, R | [[Category: Griffin, R J.]] | ||
[[Category: Harris, P | [[Category: Harris, P A.]] | ||
[[Category: Hassell, A | [[Category: Hassell, A M.]] | ||
[[Category: Holmes, W | [[Category: Holmes, W D.]] | ||
[[Category: Hunter, R | [[Category: Hunter, R N.]] | ||
[[Category: Jr., R | [[Category: Jr., R T.Gampe.]] | ||
[[Category: Knick, V | [[Category: Knick, V B.]] | ||
[[Category: Kuyper, L | [[Category: Kuyper, L K.]] | ||
[[Category: Lackey, K.]] | [[Category: Lackey, K.]] | ||
[[Category: Lovejoy, B.]] | [[Category: Lovejoy, B.]] | ||
[[Category: Luzzio, M | [[Category: Luzzio, M J.]] | ||
[[Category: Murray, D.]] | [[Category: Murray, D.]] | ||
[[Category: Parker, P.]] | [[Category: Parker, P.]] | ||
[[Category: Rocque, W | [[Category: Rocque, W J.]] | ||
[[Category: Shewchuk, L.]] | [[Category: Shewchuk, L.]] | ||
[[Category: Veal, J | [[Category: Veal, J M.]] | ||
[[Category: Walker, D | [[Category: Walker, D H.]] | ||
[[Category: 107]] | [[Category: 107]] | ||
[[Category: cyclin a]] | [[Category: cyclin a]] | ||
[[Category: cyclin-dependent kinase]] | [[Category: cyclin-dependent kinase]] | ||
''Page seeded by [http:// | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 12:43:13 2008'' | ||
Revision as of 13:43, 21 February 2008
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THE STRUCTURE OF CDK2/CYCLIN A IN COMPLEX WITH AN OXINDOLE INHIBITOR
OverviewOverview
Most traditional cytotoxic anticancer agents ablate the rapidly dividing epithelium of the hair follicle and induce alopecia (hair loss). Inhibition of cyclin-dependent kinase 2 (CDK2), a positive regulator of eukaryotic cell cycle progression, may represent a therapeutic strategy for prevention of chemotherapy-induced alopecia (CIA) by arresting the cell cycle and reducing the sensitivity of the epithelium to many cell cycle-active antitumor agents. Potent small-molecule inhibitors of CDK2 were developed using structure-based methods. Topical application of these compounds in a neonatal rat model of CIA reduced hair loss at the site of application in 33 to 50% of the animals. Thus, inhibition of CDK2 represents a potentially useful approach for the prevention of CIA in cancer patients.
About this StructureAbout this Structure
1FVV is a Protein complex structure of sequences from Homo sapiens with as ligand. Active as Non-specific serine/threonine protein kinase, with EC number 2.7.11.1 Full crystallographic information is available from OCA.
ReferenceReference
Prevention of chemotherapy-induced alopecia in rats by CDK inhibitors., Davis ST, Benson BG, Bramson HN, Chapman DE, Dickerson SH, Dold KM, Eberwein DJ, Edelstein M, Frye SV, Gampe Jr RT, Griffin RJ, Harris PA, Hassell AM, Holmes WD, Hunter RN, Knick VB, Lackey K, Lovejoy B, Luzzio MJ, Murray D, Parker P, Rocque WJ, Shewchuk L, Veal JM, Walker DH, Kuyper LF, Science. 2001 Jan 5;291(5501):134-7. PMID:11141566
Page seeded by OCA on Thu Feb 21 12:43:13 2008
Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)
OCA- Pages with broken file links
- Homo sapiens
- Non-specific serine/threonine protein kinase
- Protein complex
- Benson, B G.
- Bramson, H N.
- Chapman, D E.
- Davis, S T.
- Dickerson, S H.
- Dold, K M.
- Eberwein, D J.
- Edelstein, M.
- Frye, S V.
- Griffin, R J.
- Harris, P A.
- Hassell, A M.
- Holmes, W D.
- Hunter, R N.
- Jr., R T.Gampe.
- Knick, V B.
- Kuyper, L K.
- Lackey, K.
- Lovejoy, B.
- Luzzio, M J.
- Murray, D.
- Parker, P.
- Rocque, W J.
- Shewchuk, L.
- Veal, J M.
- Walker, D H.
- 107
- Cyclin a
- Cyclin-dependent kinase