2g9x: Difference between revisions

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[[Image:2g9x.~~gif~~|left|200px]]

[[Image:2g9x.png|left|200px]]

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~~'''~~Structure of Thr 160 phosphorylated CDK2/cyclin A in complex with the inhibitor NU6271~~'''~~

===Structure of Thr 160 phosphorylated CDK2/cyclin A in complex with the inhibitor NU6271===

~~==Overview==~~

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~~beta~~-~~Piperidinoethylsulfides are oxidized by m~~-~~chloroperbenzoic acid~~ to ~~intermediates containing both N-oxide and sulfone functions~~. ~~These undergo a Cope-type elimination to a vinylsulfone that can be captured by amines to afford beta-aminoethylsulfones~~. ~~When a beta-aminoethylsulfone group~~ is ~~linked to~~ the ~~4-position of a phenyl group attached at N-2 of O6-cyclohexylmethylguanine, the resulting derivatives are inhibitors of the cyclin-dependent kinase CDK2~~. ~~One of the most potent inhibitors (IC50 = 45 nM) contained a N~~-3-hydroxypropyl group on the aminoethylsulfonyl substituent. The crystal structure of this inhibitor bound to CDK2/cyclin A was determined and shows an unusual network of hydrogen bonds. The synthetic methodology developed can be utilized in multiple-parallel format and has numerous potential applications in medicinal chemistry.

The line below this paragraph, {{ABSTRACT_PUBMED_16669651}}, adds the Publication Abstract to the page

(as it appears on PubMed at http://www.pubmed.gov), where 16669651 is the PubMed ID number.

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==About this Structure==

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[[Category: Serine/threonine protein kinase]]

[[Category: Transferase]]

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun ~~May 4 04~~:52:03 2008''

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 15:01:00 2008''

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-[[Image:2g9x.gif|left|200px]]
+{{Seed}}
+[[Image:2g9x.png|left|200px]]
 <!--
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 {{STRUCTURE_2g9x|  PDB=2g9x  |  SCENE=  }}
-'''Structure of Thr 160 phosphorylated CDK2/cyclin A in complex with the inhibitor NU6271'''
+===Structure of Thr 160 phosphorylated CDK2/cyclin A in complex with the inhibitor NU6271===
-==Overview==
+<!--
-beta-Piperidinoethylsulfides are oxidized by m-chloroperbenzoic acid to intermediates containing both N-oxide and sulfone functions. These undergo a Cope-type elimination to a vinylsulfone that can be captured by amines to afford beta-aminoethylsulfones. When a beta-aminoethylsulfone group is linked to the 4-position of a phenyl group attached at N-2 of O6-cyclohexylmethylguanine, the resulting derivatives are inhibitors of the cyclin-dependent kinase CDK2. One of the most potent inhibitors (IC50 = 45 nM) contained a N-3-hydroxypropyl group on the aminoethylsulfonyl substituent. The crystal structure of this inhibitor bound to CDK2/cyclin A was determined and shows an unusual network of hydrogen bonds. The synthetic methodology developed can be utilized in multiple-parallel format and has numerous potential applications in medicinal chemistry.
+The line below this paragraph, {{ABSTRACT_PUBMED_16669651}}, adds the Publication Abstract to the page
+(as it appears on PubMed at http://www.pubmed.gov), where 16669651 is the PubMed ID number.
+-->
+{{ABSTRACT_PUBMED_16669651}}
 ==About this Structure==
@@ Line 32: / Line 36: @@
 [[Category: Serine/threonine protein kinase]]
 [[Category: Transferase]]
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May  4 04:52:03 2008''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 15:01:00 2008''