3fw3

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{{Seed}}
 
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[[Image:3fw3.png|left|200px]]
 
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==Crystal Structure of soluble domain of CA4 in complex with Dorzolamide==
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The line below this paragraph, containing "STRUCTURE_3fw3", creates the "Structure Box" on the page.
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<StructureSection load='3fw3' size='340' side='right'caption='[[3fw3]], [[Resolution|resolution]] 1.72&Aring;' scene=''>
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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== Structural highlights ==
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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<table><tr><td colspan='2'>[[3fw3]] is a 2 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=3FW3 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3FW3 FirstGlance]. <br>
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or leave the SCENE parameter empty for the default display.
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.72&#8491;</td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=ETS:(4S-TRANS)-4-(ETHYLAMINO)-5,6-DIHYDRO-6-METHYL-4H-THIENO(2,3-B)THIOPYRAN-2-SULFONAMIDE-7,7-DIOXIDE'>ETS</scene>, <scene name='pdbligand=GLC:ALPHA-D-GLUCOSE'>GLC</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
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{{STRUCTURE_3fw3| PDB=3fw3 | SCENE= }}
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=3fw3 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3fw3 OCA], [https://pdbe.org/3fw3 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3fw3 RCSB], [https://www.ebi.ac.uk/pdbsum/3fw3 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3fw3 ProSAT]</span></td></tr>
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</table>
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== Disease ==
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[https://www.uniprot.org/uniprot/CAH4_HUMAN CAH4_HUMAN] Defects in CA4 are the cause of retinitis pigmentosa type 17 (RP17) [MIM:[https://omim.org/entry/600852 600852]. RP leads to degeneration of retinal photoreceptor cells. Patients typically have night vision blindness and loss of midperipheral visual field. As their condition progresses, they lose their far peripheral visual field and eventually central vision as well. RP17 inheritance is autosomal dominant. Note=Defective acid overload removal from retina and retinal epithelium, due to mutant CA4, is responsible for photoreceptor degeneration, indicating that impaired pH homeostasis is the most likely cause underlying the RP17 phenotype.<ref>PMID:15563508</ref>
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== Function ==
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[https://www.uniprot.org/uniprot/CAH4_HUMAN CAH4_HUMAN] Reversible hydration of carbon dioxide. May stimulate the sodium/bicarbonate transporter activity of SLC4A4 that acts in pH homeostasis. It is essential for acid overload removal from the retina and retina epithelium, and acid release in the choriocapillaris in the choroid.<ref>PMID:15563508</ref>
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== Evolutionary Conservation ==
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[[Image:Consurf_key_small.gif|200px|right]]
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Check<jmol>
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<jmolCheckbox>
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<scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/fw/3fw3_consurf.spt"</scriptWhenChecked>
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<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview03.spt</scriptWhenUnchecked>
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<text>to colour the structure by Evolutionary Conservation</text>
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</jmolCheckbox>
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</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=3fw3 ConSurf].
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<div style="clear:both"></div>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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A novel series of potent thioether benzenesulfonamide inhibitors of carbonic anhydrases II and IV was discovered using structure-based drug design. Synthesis, structure-activity relationship, and optimization of physicochemical properties are described. Low nanomolar potency was achieved, and selected compounds with improved thermodynamic solubility showed promising in vitro inhibition of carbonic anhydrase activity in rabbit iris ciliary body homogenate.
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===Crystal Structure of soluble domain of CA4 in complex with Dorzolamide===
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Thioether benzenesulfonamide inhibitors of carbonic anhydrases II and IV: structure-based drug design, synthesis, and biological evaluation.,Vernier W, Chong W, Rewolinski D, Greasley S, Pauly T, Shaw M, Dinh D, Ferre RA, Nukui S, Ornelas M, Reyner E Bioorg Med Chem. 2010 May 1;18(9):3307-19. Epub 2010 Mar 11. PMID:20363633<ref>PMID:20363633</ref>
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
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<div class="pdbe-citations 3fw3" style="background-color:#fffaf0;"></div>
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==See Also==
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The line below this paragraph, {{ABSTRACT_PUBMED_20363633}}, adds the Publication Abstract to the page
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*[[Carbonic anhydrase 3D structures|Carbonic anhydrase 3D structures]]
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(as it appears on PubMed at http://www.pubmed.gov), where 20363633 is the PubMed ID number.
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== References ==
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<references/>
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{{ABSTRACT_PUBMED_20363633}}
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__TOC__
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</StructureSection>
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==Disease==
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Known disease associated with this structure: Retinitis pigmentosa-17 OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=114760 114760]]
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==About this Structure==
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3FW3 is a 2 chains structure with sequences 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=3FW3 OCA].
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==Reference==
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<ref group="xtra">PMID:20363633</ref><references group="xtra"/>
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[[Category: Carbonate dehydratase]]
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[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Ferre, R A.A.]]
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[[Category: Large Structures]]
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[[Category: Greasley, S E.]]
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[[Category: Ferre RAA]]
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[[Category: Paz, R.]]
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[[Category: Greasley SE]]
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[[Category: Wickersham, J.]]
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[[Category: Paz R]]
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[[Category: Cell membrane]]
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[[Category: Wickersham J]]
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[[Category: Disease mutation]]
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[[Category: Glycoprotein]]
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[[Category: Gpi-anchor]]
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[[Category: Lipoprotein]]
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[[Category: Lyase]]
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[[Category: Membrane]]
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[[Category: Metal-binding]]
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[[Category: Polymorphism]]
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[[Category: Retinitis pigmentosa]]
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[[Category: Sensory transduction]]
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[[Category: Structure-based drug design. small molecule complex. co-crystal]]
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[[Category: Vision]]
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[[Category: Zinc]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed May 12 10:35:22 2010''
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Current revision

Crystal Structure of soluble domain of CA4 in complex with Dorzolamide

PDB ID 3fw3

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