1tu6: Difference between revisions
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|PDB= 1tu6 |SIZE=350|CAPTION= <scene name='initialview01'>1tu6</scene>, resolution 1.75Å | |PDB= 1tu6 |SIZE=350|CAPTION= <scene name='initialview01'>1tu6</scene>, resolution 1.75Å | ||
|SITE= | |SITE= | ||
|LIGAND= | |LIGAND= <scene name='pdbligand=FSP:[1-(4-FLUOROBENZYL)CYCLOBUTYL]METHYL+(1S)-1-[OXO(1H-PYRAZOL-5-YLAMINO)ACETYL]PENTYLCARBAMATE'>FSP</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene> | ||
|ACTIVITY= [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] | |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> | ||
|GENE= CTSK, CTSO, CTSO2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens]) | |GENE= CTSK, CTSO, CTSO2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens]) | ||
|DOMAIN= | |||
|RELATEDENTRY= | |||
|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1tu6 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1tu6 OCA], [http://www.ebi.ac.uk/pdbsum/1tu6 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1tu6 RCSB]</span> | |||
}} | }} | ||
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==Overview== | ==Overview== | ||
A series of ketoamides were synthesized and evaluated for inhibitory activity against cathepsin K. Exploration of the interactions between achiral P(2) substituents and the cysteine protease based on molecular modelling suggestions resulted in potent cathepsin K inhibitors that demonstrated high selectivity versus cathepsins B, H, and L. Subsequent modifications of the P(3), P(1), and P(1') moieties afforded orally bioavailable inhibitors. | A series of ketoamides were synthesized and evaluated for inhibitory activity against cathepsin K. Exploration of the interactions between achiral P(2) substituents and the cysteine protease based on molecular modelling suggestions resulted in potent cathepsin K inhibitors that demonstrated high selectivity versus cathepsins B, H, and L. Subsequent modifications of the P(3), P(1), and P(1') moieties afforded orally bioavailable inhibitors. | ||
==About this Structure== | ==About this Structure== | ||
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[[Category: Wells-Knecht, K J.]] | [[Category: Wells-Knecht, K J.]] | ||
[[Category: Wright, L L.]] | [[Category: Wright, L L.]] | ||
[[Category: catk]] | [[Category: catk]] | ||
[[Category: cysteine protease]] | [[Category: cysteine protease]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 00:01:06 2008'' | ||