1udt

From Proteopedia

(Difference between revisions)
Jump to: navigation, search
Current revision (23:51, 27 December 2023) (edit) (undo)
 
(10 intermediate revisions not shown.)
Line 1: Line 1:
-
{{Seed}}
 
-
[[Image:1udt.png|left|200px]]
 
-
<!--
+
==Crystal structure of Human Phosphodiesterase 5 complexed with Sildenafil(Viagra)==
-
The line below this paragraph, containing "STRUCTURE_1udt", creates the "Structure Box" on the page.
+
<StructureSection load='1udt' size='340' side='right'caption='[[1udt]], [[Resolution|resolution]] 2.30&Aring;' scene=''>
-
You may change the PDB parameter (which sets the PDB file loaded into the applet)
+
== Structural highlights ==
-
or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
+
<table><tr><td colspan='2'>[[1udt]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1UDT OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1UDT FirstGlance]. <br>
-
or leave the SCENE parameter empty for the default display.
+
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.3&#8491;</td></tr>
-
-->
+
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=VIA:5-{2-ETHOXY-5-[(4-METHYLPIPERAZIN-1-YL)SULFONYL]PHENYL}-1-METHYL-3-PROPYL-1H,6H,7H-PYRAZOLO[4,3-D]PYRIMIDIN-7-ONE'>VIA</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
-
{{STRUCTURE_1udt| PDB=1udt | SCENE= }}
+
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=1udt FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1udt OCA], [https://pdbe.org/1udt PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1udt RCSB], [https://www.ebi.ac.uk/pdbsum/1udt PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1udt ProSAT]</span></td></tr>
 +
</table>
 +
== Function ==
 +
[https://www.uniprot.org/uniprot/PDE5A_HUMAN PDE5A_HUMAN] Plays a role in signal transduction by regulating the intracellular concentration of cyclic nucleotides. This phosphodiesterase catalyzes the specific hydrolysis of cGMP to 5'-GMP.
 +
== 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/ud/1udt_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/main_output.php?pdb_ID=1udt ConSurf].
 +
<div style="clear:both"></div>
 +
<div style="background-color:#fffaf0;">
 +
== Publication Abstract from PubMed ==
 +
Phosphodiesterases (PDEs) are a superfamily of enzymes that degrade the intracellular second messengers cyclic AMP and cyclic GMP. As essential regulators of cyclic nucleotide signalling with diverse physiological functions, PDEs are drug targets for the treatment of various diseases, including heart failure, depression, asthma, inflammation and erectile dysfunction. Of the 12 PDE gene families, cGMP-specific PDE5 carries out the principal cGMP-hydrolysing activity in human corpus cavernosum tissue. It is well known as the target of sildenafil citrate (Viagra) and other similar drugs for the treatment of erectile dysfunction. Despite the pressing need to develop selective PDE inhibitors as therapeutic drugs, only the cAMP-specific PDE4 structures are currently available. Here we present the three-dimensional structures of the catalytic domain (residues 537-860) of human PDE5 complexed with the three drug molecules sildenafil, tadalafil (Cialis) and vardenafil (Levitra). These structures will provide opportunities to design potent and selective PDE inhibitors with improved pharmacological profiles.
-
===Crystal structure of Human Phosphodiesterase 5 complexed with Sildenafil(Viagra)===
+
Structure of the catalytic domain of human phosphodiesterase 5 with bound drug molecules.,Sung BJ, Hwang KY, Jeon YH, Lee JI, Heo YS, Kim JH, Moon J, Yoon JM, Hyun YL, Kim E, Eum SJ, Park SY, Lee JO, Lee TG, Ro S, Cho JM Nature. 2003 Sep 4;425(6953):98-102. PMID:12955149<ref>PMID:12955149</ref>
 +
From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
 +
</div>
 +
<div class="pdbe-citations 1udt" style="background-color:#fffaf0;"></div>
-
<!--
+
==See Also==
-
The line below this paragraph, {{ABSTRACT_PUBMED_12955149}}, adds the Publication Abstract to the page
+
*[[Phosphodiesterase 3D structures|Phosphodiesterase 3D structures]]
-
(as it appears on PubMed at http://www.pubmed.gov), where 12955149 is the PubMed ID number.
+
== References ==
-
-->
+
<references/>
-
{{ABSTRACT_PUBMED_12955149}}
+
__TOC__
-
 
+
</StructureSection>
-
==About this Structure==
+
-
1UDT is a 1 chain structure of 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=1UDT OCA].
+
-
 
+
-
==Reference==
+
-
<ref group="xtra">PMID:12955149</ref><references group="xtra"/>
+
-
[[Category: 3',5'-cyclic-nucleotide phosphodiesterase]]
+
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
-
[[Category: Cho, J M.]]
+
[[Category: Large Structures]]
-
[[Category: Eum, S J.]]
+
[[Category: Cho JM]]
-
[[Category: Heo, Y S.]]
+
[[Category: Eum SJ]]
-
[[Category: Hwang, K Y.]]
+
[[Category: Heo Y-S]]
-
[[Category: Hyun, Y L.]]
+
[[Category: Hwang KY]]
-
[[Category: Jeon, Y H.]]
+
[[Category: Hyun Y-L]]
-
[[Category: Kim, E.]]
+
[[Category: Jeon YH]]
-
[[Category: Kim, J H.]]
+
[[Category: Kim E]]
-
[[Category: Lee, J I.]]
+
[[Category: Kim JH]]
-
[[Category: Lee, J O.]]
+
[[Category: Lee J-O]]
-
[[Category: Lee, T G.]]
+
[[Category: Lee JI]]
-
[[Category: Moon, J.]]
+
[[Category: Lee TG]]
-
[[Category: Park, S Y.]]
+
[[Category: Moon J]]
-
[[Category: Ro, S.]]
+
[[Category: Park S-Y]]
-
[[Category: Sung, B J.]]
+
[[Category: Ro S]]
-
[[Category: Yoon, J M.]]
+
[[Category: Sung B-J]]
-
[[Category: Cgmp-specific phosphodiesterase 5]]
+
[[Category: Yoon JM]]
-
[[Category: Selective inhibitor]]
+
-
[[Category: Sildenafil]]
+
-
 
+
-
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Feb 17 07:57:41 2009''
+

Current revision

Crystal structure of Human Phosphodiesterase 5 complexed with Sildenafil(Viagra)

PDB ID 1udt

Drag the structure with the mouse to rotate

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/1udt"
Personal tools