The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K.
Publication
, Journal Article
Gauthier, JY; Chauret, N; Cromlish, W; Desmarais, S; Duong, LT; Falgueyret, J-P; Kimmel, DB; Lamontagne, S; Léger, S; LeRiche, T; Li, CS ...
Published in: Bioorganic & medicinal chemistry letters
February 2008
Odanacatib is a potent, selective, and neutral cathepsin K inhibitor which was developed to address the metabolic liabilities of the Cat K inhibitor L-873724. Substituting P1 and modifying the P2 side chain led to a metabolically robust inhibitor with a long half-life in preclinical species. Odanacatib was more selective in whole cell assays than the published Cat K inhibitors balicatib and relacatib. Evaluation in dermal fibroblast culture showed minimal intracellular collagen accumulation relative to less selective Cat K inhibitors.
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Published In
Bioorganic & medicinal chemistry letters
DOI
EISSN
1464-3405
ISSN
0960-894X
Publication Date
February 2008
Volume
18
Issue
3
Start / End Page
923 / 928
Related Subject Headings
- Sulfones
- Structure-Activity Relationship
- Skin
- Osteoporosis, Postmenopausal
- Molecular Structure
- Models, Biological
- Medicinal & Biomolecular Chemistry
- Humans
- Fibroblasts
- Dogs
Citation
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NLM
Gauthier, J. Y., Chauret, N., Cromlish, W., Desmarais, S., Duong, L. T., Falgueyret, J.-P., … Black, W. C. (2008). The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K. Bioorganic & Medicinal Chemistry Letters, 18(3), 923–928. https://doi.org/10.1016/j.bmcl.2007.12.047
Gauthier, Jacques Yves, Nathalie Chauret, Wanda Cromlish, Sylvie Desmarais, Le T. Duong, Jean-Pierre Falgueyret, Donald B. Kimmel, et al. “The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K.” Bioorganic & Medicinal Chemistry Letters 18, no. 3 (February 2008): 923–28. https://doi.org/10.1016/j.bmcl.2007.12.047.
Gauthier JY, Chauret N, Cromlish W, Desmarais S, Duong LT, Falgueyret J-P, et al. The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K. Bioorganic & medicinal chemistry letters. 2008 Feb;18(3):923–8.
Gauthier, Jacques Yves, et al. “The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K.” Bioorganic & Medicinal Chemistry Letters, vol. 18, no. 3, Feb. 2008, pp. 923–28. Epmc, doi:10.1016/j.bmcl.2007.12.047.
Gauthier JY, Chauret N, Cromlish W, Desmarais S, Duong LT, Falgueyret J-P, Kimmel DB, Lamontagne S, Léger S, LeRiche T, Li CS, Massé F, McKay DJ, Nicoll-Griffith DA, Oballa RM, Palmer JT, Percival MD, Riendeau D, Robichaud J, Rodan GA, Rodan SB, Seto C, Thérien M, Truong V-L, Venuti MC, Wesolowski G, Young RN, Zamboni R, Black WC. The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K. Bioorganic & medicinal chemistry letters. 2008 Feb;18(3):923–928.
Published In
Bioorganic & medicinal chemistry letters
DOI
EISSN
1464-3405
ISSN
0960-894X
Publication Date
February 2008
Volume
18
Issue
3
Start / End Page
923 / 928
Related Subject Headings
- Sulfones
- Structure-Activity Relationship
- Skin
- Osteoporosis, Postmenopausal
- Molecular Structure
- Models, Biological
- Medicinal & Biomolecular Chemistry
- Humans
- Fibroblasts
- Dogs