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* Residue conservation analysis
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Enzyme class:
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E.C.3.4.22.38
- Cathepsin K.
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Reaction:
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Broad proteolytic activity. With small-molecule substrates and inhibitors, the major determinant of specificity is P2, which is preferably Leu, Met > Phe, and not Arg.
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Gene Ontology (GO) functional annotation
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Biological process
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proteolysis
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1 term
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Biochemical function
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cysteine-type peptidase activity
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2 terms
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DOI no:
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J Med Chem
41:3563-3567
(1998)
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PubMed id:
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Conformationally constrained 1,3-diamino ketones: a series of potent inhibitors of the cysteine protease cathepsin K.
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R.W.Marquis,
D.S.Yamashita,
Y.Ru,
S.M.LoCastro,
H.J.Oh,
K.F.Erhard,
R.L.DesJarlais,
M.S.Head,
W.W.Smith,
B.Zhao,
C.A.Janson,
S.S.Abdel-Meguid,
T.A.Tomaszek,
M.A.Levy,
D.F.Veber.
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ABSTRACT
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Literature references that cite this PDB file's key reference
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PubMed id
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Reference
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M.Ravikumar,
S.Pavan,
S.Bairy,
A.B.Pramod,
M.Sumakanth,
M.Kishore,
and
T.Sumithra
(2008).
Virtual screening of cathepsin k inhibitors using docking and pharmacophore models.
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Chem Biol Drug Des, 72,
79-90.
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A.F.Schilling,
C.Mülhausen,
W.Lehmann,
R.Santer,
T.Schinke,
J.M.Rueger,
and
M.Amling
(2007).
High bone mineral density in pycnodysostotic patients with a novel mutation in the propeptide of cathepsin K.
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Osteoporos Int, 18,
659-669.
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D.S.Yamashita,
R.Xie,
H.Lin,
B.Wang,
S.D.Shi,
C.J.Quinn,
M.E.Hemling,
C.Hissong,
T.A.Tomaszek,
and
D.F.Veber
(2004).
Benzodioxocin-3-ones and N-acyl-3-amino-3-buten-2-ones: novel classes of cathepsin K cysteine protease inhibitors.
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J Pept Res, 63,
265-269.
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F.S.Giraudeau,
R.E.McGinnis,
I.C.Gray,
E.J.O'Brien,
K.E.Doncaster,
N.K.Spurr,
S.H.Ralston,
D.M.Reid,
and
J.Wood
(2004).
Characterization of common genetic variants in cathepsin K and testing for association with bone mineral density in a large cohort of perimenopausal women from Scotland.
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J Bone Miner Res, 19,
31-41.
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M.E.McGrath,
P.A.Sprengeler,
C.M.Hill,
V.Martichonok,
H.Cheung,
J.R.Somoza,
J.T.Palmer,
and
J.W.Janc
(2003).
Peptide ketobenzoxazole inhibitors bound to cathepsin K.
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Biochemistry, 42,
15018-15028.
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A.E.Fenwick,
B.Garnier,
A.D.Gribble,
R.J.Ife,
A.D.Rawlings,
and
J.Witherington
(2001).
Solid-phase synthesis of cyclic alkoxyketones, inhibitors of the cysteine protease cathepsin K.
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Bioorg Med Chem Lett, 11,
195-198.
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G.B.Stroup,
M.W.Lark,
D.F.Veber,
A.Bhattacharyya,
S.Blake,
L.C.Dare,
K.F.Erhard,
S.J.Hoffman,
I.E.James,
R.W.Marquis,
Y.Ru,
J.A.Vasko-Moser,
B.R.Smith,
T.Tomaszek,
and
M.Gowen
(2001).
Potent and selective inhibition of human cathepsin K leads to inhibition of bone resorption in vivo in a nonhuman primate.
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J Bone Miner Res, 16,
1739-1746.
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O.Ishibashi,
T.Inui,
Y.Mori,
T.Kurokawa,
T.Kokubo,
and
M.Kumegawa
(2001).
Quantification of the expression levels of lysosomal cysteine proteinases in purified human osteoclastic cells by competitive RT-PCR.
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Calcif Tissue Int, 68,
109-116.
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The most recent references are shown first.
Citation data come partly from CiteXplore and partly
from an automated harvesting procedure. Note that this is likely to be
only a partial list as not all journals are covered by
either method. However, we are continually building up the citation data
so more and more references will be included with time.
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Links
