1yt7

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[[Image:1yt7.gif|left|200px]]
[[Image:1yt7.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 1yt7 |SIZE=350|CAPTION= <scene name='initialview01'>1yt7</scene>, resolution 2.3&Aring;
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The line below this paragraph, containing "STRUCTURE_1yt7", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <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>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/Cathepsin_K Cathepsin K], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.22.38 3.4.22.38] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE= CTSK, CTSO, CTSO2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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-->
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|DOMAIN=
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{{STRUCTURE_1yt7| PDB=1yt7 | SCENE= }}
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|RELATEDENTRY=[[1tu6|1TU6]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1yt7 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1yt7 OCA], [http://www.ebi.ac.uk/pdbsum/1yt7 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1yt7 RCSB]</span>
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}}
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'''Cathepsin K complexed with a constrained ketoamide inhibitor'''
'''Cathepsin K complexed with a constrained ketoamide inhibitor'''
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[[Category: Wright, L L.]]
[[Category: Wright, L L.]]
[[Category: Zhou, H Q.]]
[[Category: Zhou, H Q.]]
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[[Category: cathepsin]]
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[[Category: Cathepsin]]
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[[Category: cysteine protease]]
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[[Category: Cysteine protease]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 16:45:26 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 01:21:18 2008''
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Revision as of 13:45, 3 May 2008

Image:1yt7.gif

Template:STRUCTURE 1yt7

Cathepsin K complexed with a constrained ketoamide inhibitor


Overview

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.

About this Structure

1YT7 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

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 Page seeded by OCA on Sat May 3 16:45:26 2008

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OCA

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