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2bkz
From Proteopedia
(Difference between revisions)
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| - | [[ | + | ==STRUCTURE OF CDK2-CYCLIN A WITH PHA-404611== |
| + | <StructureSection load='2bkz' size='340' side='right' caption='[[2bkz]], [[Resolution|resolution]] 2.60Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[2bkz]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2BKZ OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2BKZ FirstGlance]. <br> | ||
| + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=SBC:1-[4-(AMINOSULFONYL)PHENYL]-1,6-DIHYDROPYRAZOLO[3,4-E]INDAZOLE-3-CARBOXAMIDE'>SBC</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr> | ||
| + | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[1aq1|1aq1]], [[1b38|1b38]], [[1b39|1b39]], [[1buh|1buh]], [[1ckp|1ckp]], [[1di8|1di8]], [[1dm2|1dm2]], [[1e1v|1e1v]], [[1e1x|1e1x]], [[1e9h|1e9h]], [[1f5q|1f5q]], [[1fin|1fin]], [[1fq1|1fq1]], [[1fvt|1fvt]], [[1fvv|1fvv]], [[1g5s|1g5s]], [[1gih|1gih]], [[1gii|1gii]], [[1gij|1gij]], [[1gy3|1gy3]], [[1gz8|1gz8]], [[1h00|1h00]], [[1h01|1h01]], [[1h07|1h07]], [[1h08|1h08]], [[1h0v|1h0v]], [[1h0w|1h0w]], [[1h1p|1h1p]], [[1h1q|1h1q]], [[1h1r|1h1r]], [[1h1s|1h1s]], [[1h24|1h24]], [[1h25|1h25]], [[1h26|1h26]], [[1h27|1h27]], [[1h28|1h28]], [[1hck|1hck]], [[1hcl|1hcl]], [[1jst|1jst]], [[1jsu|1jsu]], [[1jsv|1jsv]], [[1jvp|1jvp]], [[1ke5|1ke5]], [[1ke6|1ke6]], [[1ke7|1ke7]], [[1ke8|1ke8]], [[1ke9|1ke9]], [[1ogu|1ogu]], [[1oi9|1oi9]], [[1oiq|1oiq]], [[1oir|1oir]], [[1oit|1oit]], [[1oiu|1oiu]], [[1oiy|1oiy]], [[1oku|1oku]], [[1okv|1okv]], [[1okw|1okw]], [[1ol1|1ol1]], [[1ol2|1ol2]], [[1p2a|1p2a]], [[1p5e|1p5e]], [[1pf8|1pf8]], [[1pkd|1pkd]], [[1pw2|1pw2]], [[1pxi|1pxi]], [[1pxj|1pxj]], [[1pxk|1pxk]], [[1pxl|1pxl]], [[1pxm|1pxm]], [[1pxn|1pxn]], [[1pxo|1pxo]], [[1pxp|1pxp]], [[1pye|1pye]], [[1qmz|1qmz]], [[1r78|1r78]], [[1urc|1urc]], [[1urw|1urw]], [[1v1k|1v1k]], [[1vyw|1vyw]], [[1vyz|1vyz]], [[1w0x|1w0x]], [[1w8c|1w8c]], [[1w98|1w98]], [[1wcc|1wcc]], [[1y8y|1y8y]], [[1y91|1y91]], [[2bhe|2bhe]], [[2bhh|2bhh]]</td></tr> | ||
| + | <tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[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] </span></td></tr> | ||
| + | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2bkz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2bkz OCA], [http://www.rcsb.org/pdb/explore.do?structureId=2bkz RCSB], [http://www.ebi.ac.uk/pdbsum/2bkz PDBsum]</span></td></tr> | ||
| + | </table> | ||
| + | == Function == | ||
| + | [[http://www.uniprot.org/uniprot/CCNA2_HUMAN CCNA2_HUMAN]] Essential for the control of the cell cycle at the G1/S (start) and the G2/M (mitosis) transitions. | ||
| + | == Evolutionary Conservation == | ||
| + | [[Image:Consurf_key_small.gif|200px|right]] | ||
| + | Check<jmol> | ||
| + | <jmolCheckbox> | ||
| + | <scriptWhenChecked>select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/bk/2bkz_consurf.spt"</scriptWhenChecked> | ||
| + | <scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked> | ||
| + | <text>to colour the structure by Evolutionary Conservation</text> | ||
| + | </jmolCheckbox> | ||
| + | </jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/chain_selection.php?pdb_ID=2ata ConSurf]. | ||
| + | <div style="clear:both"></div> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | The synthesis and the preliminary expansion of this new class of CDK2 inhibitors are presented. The synthesis was accomplished using a solution-phase protocol amenable to rapid parallel expansion and suitable to be scaled-up in view of possible lead development. Following a medicinal chemistry program aimed at improving cell permeability and selectivity, a series of compounds with nanomolar activity in the biochemical assay and able to efficiently inhibit tumor cell proliferation has been obtained. | ||
| - | + | Benzodipyrazoles: a new class of potent CDK2 inhibitors.,D'Alessio R, Bargiotti A, Metz S, Brasca MG, Cameron A, Ermoli A, Marsiglio A, Polucci P, Roletto F, Tibolla M, Vazquez ML, Vulpetti A, Pevarello P Bioorg Med Chem Lett. 2005 Mar 1;15(5):1315-9. PMID:15713378<ref>PMID:15713378</ref> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| - | + | </div> | |
| - | + | ||
| - | + | ||
| - | + | ||
| - | + | ||
==See Also== | ==See Also== | ||
| - | *[[Cell | + | *[[Cell division protein kinase 2|Cell division protein kinase 2]] |
*[[Cyclin|Cyclin]] | *[[Cyclin|Cyclin]] | ||
| - | + | == References == | |
| - | == | + | <references/> |
| - | < | + | __TOC__ |
| + | </StructureSection> | ||
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Non-specific serine/threonine protein kinase]] | [[Category: Non-specific serine/threonine protein kinase]] | ||
| - | [[Category: Bargiottia, A | + | [[Category: Bargiottia, A]] |
| - | [[Category: Brasca, M G | + | [[Category: Brasca, M G]] |
| - | [[Category: Cameron, A | + | [[Category: Cameron, A]] |
| - | [[Category: Dalessio, R | + | [[Category: Dalessio, R]] |
| - | [[Category: Ermoli, A | + | [[Category: Ermoli, A]] |
| - | [[Category: Marsiglio, A | + | [[Category: Marsiglio, A]] |
| - | [[Category: Metz, S | + | [[Category: Metz, S]] |
| - | [[Category: Pevarello, P | + | [[Category: Pevarello, P]] |
| - | [[Category: Polucci, P | + | [[Category: Polucci, P]] |
| - | [[Category: Roletto, F | + | [[Category: Roletto, F]] |
| - | [[Category: Tibolla, M | + | [[Category: Tibolla, M]] |
| - | [[Category: Vazquez, M L | + | [[Category: Vazquez, M L]] |
| - | [[Category: Vulpetti, A | + | [[Category: Vulpetti, A]] |
[[Category: Atp-binding]] | [[Category: Atp-binding]] | ||
[[Category: Cell cycle]] | [[Category: Cell cycle]] | ||
Revision as of 16:57, 24 December 2014
STRUCTURE OF CDK2-CYCLIN A WITH PHA-404611
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Categories: Homo sapiens | Non-specific serine/threonine protein kinase | Bargiottia, A | Brasca, M G | Cameron, A | Dalessio, R | Ermoli, A | Marsiglio, A | Metz, S | Pevarello, P | Polucci, P | Roletto, F | Tibolla, M | Vazquez, M L | Vulpetti, A | Atp-binding | Cell cycle | Cell division | Cyclin | Mitosis | Phosphorylation | Protein kinase | Serine/threonine-protein kinase | Transferase | Transferase-complex
