2iw8: Difference between revisions

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[[Image:2iw8.~~gif~~|left|200px]]

[[Image:2iw8.png|left|200px]]

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~~'''~~STRUCTURE OF HUMAN THR160-PHOSPHO CDK2-CYCLIN A F82H-L83V-H84D MUTANT WITH AN O6-CYCLOHEXYLMETHYLGUANINE INHIBITOR~~'''~~

===STRUCTURE OF HUMAN THR160-PHOSPHO CDK2-CYCLIN A F82H-L83V-H84D MUTANT WITH AN O6-CYCLOHEXYLMETHYLGUANINE INHIBITOR===

~~==Overview==~~

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~~Cyclin dependent kinases are a key family of kinases involved in cell cycle regulation and are an attractive target for cancer chemotherapy.~~ The roles of four residues of the cyclin-dependent kinase active site in inhibitor selectivity were investigated by producing cyclin-dependent kinase 2 mutants bearing equivalent cyclin-dependent kinase 4 residues, ~~namely F82H~~, ~~L83V, H84D, and K89T. Assay of~~ the ~~mutants with a cyclin-dependent kinase 4-selective bisanilinopyrimidine shows that~~ the ~~K89T mutation is primarily responsible for the selectivity of this compound~~. ~~Use of the cyclin-dependent kinase 2-selective 6-cyclohexylmethoxy-2-(4'-sulfamoylanilino~~)~~purine (NU6102) shows that K89T has no role in the selectivity~~, ~~while~~ the ~~remaining three mutations have a cumulative influence~~. ~~The results indicate that certain residues that are not frequently considered in structure~~-~~aided kinase inhibitor design have an important role to play.~~

The line below this paragraph, {{ABSTRACT_PUBMED_16942020}}, adds the Publication Abstract to the page

(as it appears on PubMed at http://www.pubmed.gov), where 16942020 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 07~~:58:23 2008''

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 10:18:48 2008''

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-[[Image:2iw8.gif|left|200px]]
+{{Seed}}
+[[Image:2iw8.png|left|200px]]
 <!--
@@ Line 9: / Line 10: @@
 {{STRUCTURE_2iw8|  PDB=2iw8  |  SCENE=  }}
-'''STRUCTURE OF HUMAN THR160-PHOSPHO CDK2-CYCLIN A F82H-L83V-H84D MUTANT WITH AN O6-CYCLOHEXYLMETHYLGUANINE INHIBITOR'''
+===STRUCTURE OF HUMAN THR160-PHOSPHO CDK2-CYCLIN A F82H-L83V-H84D MUTANT WITH AN O6-CYCLOHEXYLMETHYLGUANINE INHIBITOR===
-==Overview==
+<!--
-Cyclin dependent kinases are a key family of kinases involved in cell cycle regulation and are an attractive target for cancer chemotherapy. The roles of four residues of the cyclin-dependent kinase active site in inhibitor selectivity were investigated by producing cyclin-dependent kinase 2 mutants bearing equivalent cyclin-dependent kinase 4 residues, namely F82H, L83V, H84D, and K89T. Assay of the mutants with a cyclin-dependent kinase 4-selective bisanilinopyrimidine shows that the K89T mutation is primarily responsible for the selectivity of this compound. Use of the cyclin-dependent kinase 2-selective 6-cyclohexylmethoxy-2-(4'-sulfamoylanilino)purine (NU6102) shows that K89T has no role in the selectivity, while the remaining three mutations have a cumulative influence. The results indicate that certain residues that are not frequently considered in structure-aided kinase inhibitor design have an important role to play.
+The line below this paragraph, {{ABSTRACT_PUBMED_16942020}}, adds the Publication Abstract to the page
+(as it appears on PubMed at http://www.pubmed.gov), where 16942020 is the PubMed ID number.
+-->
+{{ABSTRACT_PUBMED_16942020}}
 ==About this Structure==
@@ Line 42: / Line 46: @@
 [[Category: Serine/threonine-protein kinase]]
 [[Category: Transferase]]
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May  4 07:58:23 2008''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 10:18:48 2008''