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New page: left|200px<br /> <applet load="1fvt" size="450" color="white" frame="true" align="right" spinBox="true" caption="1fvt, resolution 2.2Å" /> '''THE STRUCTURE OF CYC...
 
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[[Image:1fvt.gif|left|200px]]<br />
[[Image:1fvt.gif|left|200px]]<br /><applet load="1fvt" size="350" color="white" frame="true" align="right" spinBox="true"  
<applet load="1fvt" size="450" color="white" frame="true" align="right" spinBox="true"  
caption="1fvt, resolution 2.2&Aring;" />
caption="1fvt, resolution 2.2&Aring;" />
'''THE STRUCTURE OF CYCLIN-DEPENDENT KINASE 2 (CDK2) IN COMPLEX WITH AN OXINDOLE INHIBITOR'''<br />
'''THE STRUCTURE OF CYCLIN-DEPENDENT KINASE 2 (CDK2) IN COMPLEX WITH AN OXINDOLE INHIBITOR'''<br />


==Overview==
==Overview==
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.
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==
1FVT is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with 106 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://ispc.weizmann.ac.il/oca-bin/ocashort?id=1FVT OCA].  
1FVT is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=106:'>106</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=1FVT OCA].  


==Reference==
==Reference==
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[[Category: Non-specific serine/threonine protein kinase]]
[[Category: Non-specific serine/threonine protein kinase]]
[[Category: Single protein]]
[[Category: Single protein]]
[[Category: Benson, B.G.]]
[[Category: Benson, B G.]]
[[Category: Bramson, H.N.]]
[[Category: Bramson, H N.]]
[[Category: Chapman, D.E.]]
[[Category: Chapman, D E.]]
[[Category: Davis, S.T.]]
[[Category: Davis, S T.]]
[[Category: Dickerson, S.H.]]
[[Category: Dickerson, S H.]]
[[Category: Dold, K.M.]]
[[Category: Dold, K M.]]
[[Category: Eberwein, D.J.]]
[[Category: Eberwein, D J.]]
[[Category: Edelstein, M.]]
[[Category: Edelstein, M.]]
[[Category: Frye, S.V.]]
[[Category: Frye, S V.]]
[[Category: Griffin, R.J.]]
[[Category: Griffin, R J.]]
[[Category: Harris, P.A.]]
[[Category: Harris, P A.]]
[[Category: Hassell, A.M.]]
[[Category: Hassell, A M.]]
[[Category: Holmes, W.D.]]
[[Category: Holmes, W D.]]
[[Category: Hunter, R.N.]]
[[Category: Hunter, R N.]]
[[Category: Jr., R.T.Gampe.]]
[[Category: Jr., R T.Gampe.]]
[[Category: Knick, V.B.]]
[[Category: Knick, V B.]]
[[Category: Kuyper, L.K.]]
[[Category: Kuyper, L K.]]
[[Category: Lackey, K.]]
[[Category: Lackey, K.]]
[[Category: Lovejoy, B.]]
[[Category: Lovejoy, B.]]
[[Category: Luzzio, M.J.]]
[[Category: Luzzio, M J.]]
[[Category: Murray, D.]]
[[Category: Murray, D.]]
[[Category: Parker, P.]]
[[Category: Parker, P.]]
[[Category: Rocque, W.J.]]
[[Category: Rocque, W J.]]
[[Category: Shewchuk, L.]]
[[Category: Shewchuk, L.]]
[[Category: Veal, J.M.]]
[[Category: Veal, J M.]]
[[Category: Walker, D.H.]]
[[Category: Walker, D H.]]
[[Category: 106]]
[[Category: 106]]
[[Category: cyclin-dependent kinase]]
[[Category: cyclin-dependent kinase]]
[[Category: oxindole]]
[[Category: oxindole]]


''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 12 16:57:49 2007''
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 12:43:10 2008''