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rdf:type |
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lifeskim:mentions |
umls-concept:C0022634,
umls-concept:C0030956,
umls-concept:C0185125,
umls-concept:C0205314,
umls-concept:C0220781,
umls-concept:C0243077,
umls-concept:C0284930,
umls-concept:C0332256,
umls-concept:C0449444,
umls-concept:C0679622,
umls-concept:C1883254
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pubmed:issue |
20
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|
pubmed:dateCreated |
2002-9-24
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|
pubmed:abstractText |
Cathepsin K is highly expressed in human osteoclasts, and is implicated in bone resorption. This makes it an attractive target for the treatment of osteoporosis. Peptides containing 2-amino-1'-hydroxymethyl ketones and 2-amino-1'-alkoxymethyl ketones were discovered as potent inhibitors of cathepsin K. A novel synthetic route was devised to facilitate rapid elucidation of the SAR of these inhibitors. The synthesis and SAR of hydroxymethyl ketones are presented.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
|
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pubmed:status |
MEDLINE
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pubmed:month |
Oct
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pubmed:issn |
0960-894X
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pubmed:author |
|
|
pubmed:issnType |
Print
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pubmed:day |
21
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pubmed:volume |
12
|
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2887-91
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pubmed:dateRevised |
2009-11-19
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pubmed:meshHeading |
pubmed-meshheading:12270170-Cathepsin K,
pubmed-meshheading:12270170-Cathepsins,
pubmed-meshheading:12270170-Drug Design,
pubmed-meshheading:12270170-Humans,
pubmed-meshheading:12270170-Indicators and Reagents,
pubmed-meshheading:12270170-Ketones,
pubmed-meshheading:12270170-Osteoclasts,
pubmed-meshheading:12270170-Osteoporosis,
pubmed-meshheading:12270170-Peptides,
pubmed-meshheading:12270170-Protease Inhibitors,
pubmed-meshheading:12270170-Stereoisomerism,
pubmed-meshheading:12270170-Structure-Activity Relationship
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|
pubmed:year |
2002
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|
pubmed:articleTitle |
Novel route to the synthesis of peptides containing 2-amino-1'-hydroxymethyl ketones and their application as cathepsin K inhibitors.
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|
pubmed:affiliation |
Celera, 180 Kimball Way, South San Francisco, CA 94080, USA. rohan.mendonca@celera.com
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pubmed:publicationType |
Journal Article
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