Results 261 to 270 of about 94,685 (278)

Design of Cathepsin K Inhibitors for Osteoporosis

Current Topics in Medicinal Chemistry, 2005
Osteoporosis is a progressive, debilitating bone disease resulting in increased cost and morbidity to the elderly. This review summarizes the therapeutic approaches taken in the treatment of osteoporosis with particular emphasis on cathepsin K inhibitors.
David N, Deaton, Francis X, Tavares
openaire   +2 more sources

Acyclic cyanamide-based inhibitors of cathepsin K

Bioorganic & Medicinal Chemistry Letters, 2005
Conversion of the proline-derived cyanamide lead to an acyclic cyanamide capable of forming an additional hydrogen bond with cathepsin K resulted in a large increase in inhibitory activity. An X-ray structure of a co-crystal of a cyanamide with cathepsin K confirmed the enzyme interaction.
David G, Barrett, David N, Deaton, Anne M, Hassell, Robert B, McFadyen, Aaron B, Miller, Larry R, Miller, J Alan, Payne, Lisa M, Shewchuk, Derril H, Willard, Lois L, Wright   +9 more
openaire   +2 more sources

Cathepsin K Preferentially Solubilizes Matured Bone Matrix

Calcified Tissue International, 2012
Bone collagen undergoes a series of enzymatic and nonenzymatic posttranslational modifications with maturation. The aim of this study was to analyze the collagenolytic efficiency of cathepsin K in relation to the extent of bone collagen age. Bone collagen posttranslational maturation was induced in vitro by preincubating bovine fetal cortical bone ...
Olivier, Borel, Evelyne, Gineyts, Cindy, Bertholon, Patrick, Garnero   +3 more
openaire   +2 more sources

Cathepsin K expression in basal cell carcinoma

Journal of the European Academy of Dermatology and Venereology, 2012
AbstractBackground  Cathepsin K is a cysteine protease with strong collagenolytic and elastolytic properties. Recently, cathepsin K expression in tumour cells of malignant melanoma and in the stromal cells of squamous cell carcinoma of the skin has been reported to play an important role in tumour progression.
M, Ishida, F, Kojima, H, Okabe
openaire   +2 more sources

Cathepsin K – a marker of macrophage differentiation?

The Journal of Pathology, 2001
Abstract Cathepsin K is a cysteine protease with high matrix‐degrading activity. Initially, cathepsin K was described as being expressed exclusively by osteoclasts. It was suggested that cathepsin K expression is a specific feature of cells involved in bone remodelling. The aim of this study was to investigate the
F, Bühling, A, Reisenauer, A, Gerber, S, Krüger, E, Weber, D, Brömme, A, Roessner, S, Ansorge, T, Welte, C, Röcken   +9 more
openaire   +2 more sources

Cathepsin K: a unique collagenolytic cysteine peptidase

bchm, 2013
Abstract Cathepsin K has emerged as a promising target for the treatment of osteoporosis in recent years. Initially identified as a papain-like cysteine peptidase expressed in high levels in osteoclasts, the important role of this enzyme in bone metabolism was highlighted by the finding that mutations in the CTSK gene cause the rare ...
Marko, Novinec, Brigita, Lenarčič
openaire   +2 more sources

Distinct Roles of Cathepsin K and Cathepsin L IN Osteoclastic Bone Resorption

Endocrine Research, 2000
The role of cathepsin K (CAK), cloned as a novel collagenolytic cysteine protease (CCP), cathepsin L (CAL) and cathepsin B (CAB) in bone resorption was investigated. In mouse calvarial organ culture medium, CAL, detected in trace amounts in control conditions, and CCP activity were increased by stimulants of bone resorption: 1alpha,25-(OH)2D3 ...
N, Furuyama, Y, Fujisawa
openaire   +2 more sources

Chapter 8 Cathepsin K Inhibitors

2007
Publisher Summary Cathepsin K (Cat K) is a member of the CA1 family of lysosomal cysteine proteases. This family is comprised of 11 human members (cathepsins B, C, F, H, K, L, O, S, V, W, Z) which share a common papain-like structural fold and a conserved active site Cys-Asn-His triad of residues. Cat K plays a key role in bone resorption.
W. Cameron Black, M. David Percival
openaire   +1 more source

The Toll of Cathepsin K Deficiency

Science, 2008
An enzyme that is important to bone metabolism also acts in immune cell responses to pathogen DNA.
Arthur M. Krieg, Grayson B. Lipford
openaire   +1 more source

The Regulation of Cathepsin K Gene Expression

Annals of the New York Academy of Sciences, 2006
Abstract: Cathepsin K is essential for normal bone resorption. Osteoclasts synthesize and secrete cathepsin Kinto the extracellular compartment at the attachment site between osteoclasts and the bone surface, wherein the organic matrix is subsequently degraded by cathepsin K.
openaire   +2 more sources