2r6n: Difference between revisions

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==Overview==
==Overview==
Pyrrolopyrimidine, a novel scaffold, allows to adjust interactions within, the S3 subsite of cathepsin K. The core intermediate 10 facilitated the P3, optimization and identified highly potent and selective cathepsin K, inhibitors 11-20.
Pyrrolopyrimidine, a novel scaffold, allows to adjust interactions within the S3 subsite of cathepsin K. The core intermediate 10 facilitated the P3 optimization and identified highly potent and selective cathepsin K inhibitors 11-20.
 
==Disease==
Known disease associated with this structure: Pycnodysostosis OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=601105 601105]]


==About this Structure==
==About this Structure==
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[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Single protein]]
[[Category: Single protein]]
[[Category: Cowan-Jacob, S.W.]]
[[Category: Cowan-Jacob, S W.]]
[[Category: Geisse, S.]]
[[Category: Geisse, S.]]
[[Category: Mathis, B.]]
[[Category: Mathis, B.]]
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[[Category: zymogen]]
[[Category: zymogen]]


''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jan 23 12:24:21 2008''
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 18:45:05 2008''

Revision as of 19:45, 21 February 2008

File:2r6n.jpg


2r6n, resolution 1.950Å

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Crystal structure of a pyrrolopyrimidine inhibitor in complex with human Cathepsin K

OverviewOverview

Pyrrolopyrimidine, a novel scaffold, allows to adjust interactions within the S3 subsite of cathepsin K. The core intermediate 10 facilitated the P3 optimization and identified highly potent and selective cathepsin K inhibitors 11-20.

DiseaseDisease

Known disease associated with this structure: Pycnodysostosis OMIM:[601105]

About this StructureAbout this Structure

2R6N is a Single protein structure of sequence from Homo sapiens with as ligand. Active as Cathepsin K, with EC number 3.4.22.38 Full crystallographic information is available from OCA.

ReferenceReference

Novel scaffold for cathepsin K inhibitors., Teno N, Miyake T, Ehara T, Irie O, Sakaki J, Ohmori O, Gunji H, Matsuura N, Masuya K, Hitomi Y, Nonomura K, Horiuchi M, Gohda K, Iwasaki A, Umemura I, Tada S, Kometani M, Iwasaki G, Cowan-Jacob SW, Missbach M, Lattmann R, Betschart C, Bioorg Med Chem Lett. 2007 Nov 15;17(22):6096-100. Epub 2007 Sep 15. PMID:17911019

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