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[[Image:3tc5.png|left|200px]]
==Selective targeting of disease-relevant protein binding domains by O-phosphorylated natural product derivatives==
<StructureSection load='3tc5' size='340' side='right' caption='[[3tc5]], [[Resolution|resolution]] 1.40&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[3tc5]] is a 1 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=3TC5 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3TC5 FirstGlance]. <br>
</td></tr><tr><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=3T5:(11ALPHA,16ALPHA)-9-FLUORO-11,17-DIHYDROXY-16-METHYL-3,20-DIOXOPREGNA-1,4-DIEN-21-YL+DIHYDROGEN+PHOSPHATE'>3T5</scene>, <scene name='pdbligand=P6G:HEXAETHYLENE+GLYCOL'>P6G</scene><br>
<tr><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[1pin|1pin]], [[2zr6|2zr6]], [[2itk|2itk]], [[2q5a|2q5a]]</td></tr>
<tr><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">PIN1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])</td></tr>
<tr><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Peptidylprolyl_isomerase Peptidylprolyl isomerase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=5.2.1.8 5.2.1.8] </span></td></tr>
<tr><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3tc5 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3tc5 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3tc5 RCSB], [http://www.ebi.ac.uk/pdbsum/3tc5 PDBsum]</span></td></tr>
<table>
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
Phosphorylation-dependent protein binding domains are crucially important for intracellular signaling pathways and thus highly relevant targets in chemical biology. By screening of chemical libraries against 12 structurally diverse phosphorylation-dependent protein binding domains, we have identified fosfosal and dexamethasone-21-phosphate as selective inhibitors of two antitumor targets: the SH2 domain of the transcription factor STAT5b and the substrate-binding domain of the peptidyl-prolyl isomerase Pin1, respectively. Both compounds are phosphate prodrugs with documented clinical use as anti-inflammatory agents in humans and were discovered with a high hit rate from a small subgroup within the screening library. Our study indicates O-phosphorylation of appropriately preselected natural products or natural product derivatives as a generally applicable strategy for the identification of non-reactive and non-peptidic ligands of phosphorylation-dependent protein binding domains. Moreover, our data indicate that it would be advisable to monitor the bioactivities of clinically used prodrugs in their uncleaved state against phosphorylation-dependent protein binding domains.


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Selective Targeting of Disease-Relevant Protein Binding Domains by O-Phosphorylated Natural Product Derivatives.,Graber M, Janczyk W, Sperl B, Elumalai N, Kozany C, Hausch F, Holak TA, Berg T ACS Chem Biol. 2011 Aug 10. PMID:21797253<ref>PMID:21797253</ref>
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{{STRUCTURE_3tc5|  PDB=3tc5  |  SCENE=  }}


===Selective targeting of disease-relevant protein binding domains by O-phosphorylated natural product derivatives===
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
 
</div>
 
== References ==
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<references/>
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{{ABSTRACT_PUBMED_21797253}}
 
==About this Structure==
[[3tc5]] is a 1 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=3TC5 OCA].
 
==Reference==
<ref group="xtra">PMID:021797253</ref><references group="xtra"/>
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Peptidylprolyl isomerase]]
[[Category: Peptidylprolyl isomerase]]

Revision as of 05:41, 5 June 2014

Selective targeting of disease-relevant protein binding domains by O-phosphorylated natural product derivatives

3tc5, resolution 1.40Å

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