1yt7

From Proteopedia

(Difference between revisions)
Jump to: navigation, search
m (Protected "1yt7" [edit=sysop:move=sysop])
Current revision (07:00, 23 August 2023) (edit) (undo)
 
(8 intermediate revisions not shown.)
Line 1: Line 1:
-
[[Image:1yt7.png|left|200px]]
 
-
<!--
+
==Cathepsin K complexed with a constrained ketoamide inhibitor==
-
The line below this paragraph, containing "STRUCTURE_1yt7", creates the "Structure Box" on the page.
+
<StructureSection load='1yt7' size='340' side='right'caption='[[1yt7]], [[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'>[[1yt7]] 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=1YT7 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1YT7 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=3FC:(1R)-2,2-DIMETHYL-1-({5-[4-(TRIFLUOROMETHYL)PHENYL]-1,3,4-OXADIAZOL-2-YL}METHYL)PROPYL+(1S)-1-{OXO[(2-OXO-1,3-OXAZOLIDIN-3-YL)AMINO]ACETYL}PENTYLCARBAMATE'>3FC</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>
-
{{STRUCTURE_1yt7| PDB=1yt7 | SCENE= }}
+
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=1yt7 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1yt7 OCA], [https://pdbe.org/1yt7 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1yt7 RCSB], [https://www.ebi.ac.uk/pdbsum/1yt7 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1yt7 ProSAT]</span></td></tr>
 +
</table>
 +
== Disease ==
 +
[https://www.uniprot.org/uniprot/CATK_HUMAN CATK_HUMAN] Defects in CTSK are the cause of pycnodysostosis (PKND) [MIM:[https://omim.org/entry/265800 265800]. PKND is an autosomal recessive osteochondrodysplasia characterized by osteosclerosis and short stature.<ref>PMID:8703060</ref> <ref>PMID:9529353</ref> <ref>PMID:10491211</ref> <ref>PMID:10878663</ref>
 +
== Function ==
 +
[https://www.uniprot.org/uniprot/CATK_HUMAN CATK_HUMAN] Closely involved in osteoclastic bone resorption and may participate partially in the disorder of bone remodeling. Displays potent endoprotease activity against fibrinogen at acid pH. May play an important role in extracellular matrix degradation.
 +
== 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/yt/1yt7_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=1yt7 ConSurf].
 +
<div style="clear:both"></div>
 +
<div style="background-color:#fffaf0;">
 +
== Publication Abstract from PubMed ==
 +
An orally bioavailable series of ketoamide-based cathepsin K inhibitors with good pharmacokinetic properties has been identified. Starting from a potent inhibitor endowed with poor drug properties, conformational constraint of the P(2)-P(3) linker and modifications to P(1') elements led to an enhancement in potency, solubility, clearance, and bioavailability. These optimized inhibitors attenuated bone resorption in a rat TPTX hypocalcemic bone resorption model.
-
===Cathepsin K complexed with a constrained ketoamide inhibitor===
+
P2-P3 conformationally constrained ketoamide-based inhibitors of cathepsin K.,Barrett DG, Boncek VM, Catalano JG, Deaton DN, Hassell AM, Jurgensen CH, Long ST, McFadyen RB, Miller AB, Miller LR, Payne JA, Ray JA, Samano V, Shewchuk LM, Tavares FX, Wells-Knecht KJ, Willard DH Jr, Wright LL, Zhou HQ Bioorg Med Chem Lett. 2005 Aug 1;15(15):3540-6. PMID:15982880<ref>PMID:15982880</ref>
-
 
+
From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
-
<!--
+
</div>
-
The line below this paragraph, {{ABSTRACT_PUBMED_15982880}}, adds the Publication Abstract to the page
+
<div class="pdbe-citations 1yt7" style="background-color:#fffaf0;"></div>
-
(as it appears on PubMed at http://www.pubmed.gov), where 15982880 is the PubMed ID number.
+
-
-->
+
-
{{ABSTRACT_PUBMED_15982880}}
+
-
 
+
-
==About this Structure==
+
-
[[1yt7]] is a 1 chain structure of [[Cathepsin]] 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=1YT7 OCA].
+
==See Also==
==See Also==
-
*[[Cathepsin]]
+
*[[Cathepsin 3D structures|Cathepsin 3D structures]]
-
 
+
== References ==
-
==Reference==
+
<references/>
-
<ref group="xtra">PMID:15982880</ref><references group="xtra"/>
+
__TOC__
-
[[Category: Cathepsin K]]
+
</StructureSection>
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
-
[[Category: Barrett, D G.]]
+
[[Category: Large Structures]]
-
[[Category: Boncek, V M.]]
+
[[Category: Barrett DG]]
-
[[Category: Catalano, J G.]]
+
[[Category: Boncek VM]]
-
[[Category: Deaton, D N.]]
+
[[Category: Catalano JG]]
-
[[Category: Hassell, A M.]]
+
[[Category: Deaton DN]]
-
[[Category: Jurgensen, C H.]]
+
[[Category: Hassell AM]]
-
[[Category: Long, S T.]]
+
[[Category: Jurgensen CH]]
-
[[Category: McFadyen, R B.]]
+
[[Category: Long ST]]
-
[[Category: Miller, A B.]]
+
[[Category: McFadyen RB]]
-
[[Category: Miller, L R.]]
+
[[Category: Miller AB]]
-
[[Category: Payne, J A.]]
+
[[Category: Miller LR]]
-
[[Category: Ray, J A.]]
+
[[Category: Payne JA]]
-
[[Category: Samano, V.]]
+
[[Category: Ray JA]]
-
[[Category: Shewchuk, L M.]]
+
[[Category: Samano V]]
-
[[Category: Tavares, F X.]]
+
[[Category: Shewchuk LM]]
-
[[Category: Wells-Knecht, K J.]]
+
[[Category: Tavares FX]]
-
[[Category: Willard, D H.]]
+
[[Category: Wells-Knecht KJ]]
-
[[Category: Wright, L L.]]
+
[[Category: Willard DH]]
-
[[Category: Zhou, H Q.]]
+
[[Category: Wright LL]]
-
[[Category: Cathepsin]]
+
[[Category: Zhou HQ]]
-
[[Category: Cysteine protease]]
+
-
[[Category: Hydrolase]]
+

Current revision

Cathepsin K complexed with a constrained ketoamide inhibitor

PDB ID 1yt7

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/1yt7"
Personal tools