Substrate-derived triazolo- and azapeptides as inhibitors of cathepsins K and S.

[1]  G. Brayer,et al.  Identification of mouse cathepsin K structural elements that regulate the potency of odanacatib. , 2017, The Biochemical journal.

[2]  A. Delmas,et al.  A synthetic kisspeptin analog that triggers ovulation and advances puberty , 2016, Scientific Reports.

[3]  D. Brömme,et al.  Cathepsin K osteoporosis trials, pycnodysostosis and mouse deficiency models: Commonalities and differences , 2016, Expert opinion on drug discovery.

[4]  J. Delaissé,et al.  A novel approach to inhibit bone resorption: exosite inhibitors against cathepsin K , 2016, British journal of pharmacology.

[5]  Neil D. Rawlings,et al.  Twenty years of the MEROPS database of proteolytic enzymes, their substrates and inhibitors , 2015, Nucleic Acids Res..

[6]  C. Scott,et al.  Cathepsin S: therapeutic, diagnostic, and prognostic potential , 2015, Biological chemistry.

[7]  K. Gevaert,et al.  Proteomic Identification of Cysteine Cathepsin Substrates Shed from the Surface of Cancer Cells* , 2015, Molecular & Cellular Proteomics.

[8]  A. Delmas,et al.  Combining triazole ligation and enzymatic glycosylation on solid phase simplifies the synthesis of very long glycoprotein analogues† †Electronic supplementary information (ESI) available: Detailed synthetic procedures, characterization and optimization. See DOI: 10.1039/c5sc00773a , 2015, Chemical science.

[9]  A. Delmas,et al.  Rational design of triazololipopeptides analogs of kisspeptin inducing a long-lasting increase of gonadotropins. , 2015, Journal of medicinal chemistry.

[10]  S. Marchand-Adam,et al.  Cysteine cathepsins and cystatins: from ancillary tasks to prominent status in lung diseases , 2015, Biological chemistry.

[11]  G. Brayer,et al.  Structural basis of collagen fiber degradation by cathepsin K , 2014, Proceedings of the National Academy of Sciences.

[12]  M. Fonović,et al.  Cysteine cathepsins and extracellular matrix degradation. , 2014, Biochimica et biophysica acta.

[13]  M. A. Walter,et al.  1,2,3-Triazoles as amide bond mimics: triazole scan yields protease-resistant peptidomimetics for tumor targeting. , 2013, Angewandte Chemie.

[14]  A. Delmas,et al.  Towards the simplification of protein synthesis: iterative solid-supported ligations with concomitant purifications. , 2012, Angewandte Chemie.

[15]  Takako Sasaki,et al.  Cleavage of Nidogen-1 by Cathepsin S Impairs Its Binding to Basement Membrane Partners , 2012, PloS one.

[16]  M. Cadene,et al.  A selective reversible azapeptide inhibitor of human neutrophil proteinase 3 derived from a high affinity FRET substrate , 2012, Biochemical pharmacology.

[17]  A. Delmas,et al.  Synthesis of a biologically active triazole-containing analogue of cystatin A through successive peptidomimetic alkyne-azide ligations. , 2012, Angewandte Chemie.

[18]  Olga Vasiljeva,et al.  Cysteine cathepsins: From structure, function and regulation to new frontiers☆ , 2011, Biochimica et Biophysica Acta (BBA) - Proteins and Proteomics.

[19]  Jochen Spiegel,et al.  Azapeptides and their therapeutic potential. , 2011, Future medicinal chemistry.

[20]  G. Lalmanach,et al.  Kininogens: More than cysteine protease inhibitors and kinin precursors. , 2010, Biochimie.

[21]  T. Reinheckel,et al.  Specialized roles for cysteine cathepsins in health and disease. , 2010, The Journal of clinical investigation.

[22]  L. Gentilucci,et al.  Chemical modifications designed to improve peptide stability: incorporation of non-natural amino acids, pseudo-peptide bonds, and cyclization. , 2010, Current pharmaceutical design.

[23]  O. Melnyk,et al.  Selective cleavage of an azaGly peptide bond by copper(II). Long‐range effect of histidine residue , 2010, Journal of peptide science : an official publication of the European Peptide Society.

[24]  Nicolas Lützner,et al.  Quantifying Cathepsin S Activity in Antigen Presenting Cells Using a Novel Specific Substrate* , 2008, Journal of Biological Chemistry.

[25]  F. Veillard,et al.  Lung cysteine cathepsins: intruders or unorthodox contributors to the kallikrein-kinin system? , 2008, The international journal of biochemistry & cell biology.

[26]  J. Falgueyret,et al.  The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K. , 2008, Bioorganic & medicinal chemistry letters.

[27]  K. Brix,et al.  Cysteine cathepsins: cellular roadmap to different functions. , 2008, Biochimie.

[28]  D. Brömme,et al.  Biochemical properties and regulation of cathepsin K activity. , 2008, Biochimie.

[29]  D. Speijer,et al.  1,2,3-Triazoles as peptide bond isosteres: synthesis and biological evaluation of cyclotetrapeptide mimics. , 2007, Organic & biomolecular chemistry.

[30]  D. Brömme,et al.  Modulation of hypotensive effects of kinins by cathepsin K. , 2007, Archives of biochemistry and biophysics.

[31]  O. Vasiljeva,et al.  Emerging roles of cysteine cathepsins in disease and their potential as drug targets. , 2007, Current pharmaceutical design.

[32]  David S Goodsell,et al.  1,2,3‐Triazole as a Peptide Surrogate in the Rapid Synthesis of HIV‐1 Protease Inhibitors , 2005, Chembiochem : a European journal of chemical biology.

[33]  M. Ghadiri,et al.  Heterocyclic Peptide Backbone Modifications in an α-Helical Coiled Coil , 2004 .

[34]  P. Saftig,et al.  Cathepsin K: a cysteine protease with unique kinin-degrading properties. , 2004, The Biochemical journal.

[35]  Conrad C. Huang,et al.  UCSF Chimera—A visualization system for exploratory research and analysis , 2004, J. Comput. Chem..

[36]  V. Turk,et al.  Human brain cathepsin H as a neuropeptide and bradykinin metabolizing enzyme , 2003, Peptides.

[37]  M. Juliano,et al.  Probing cathepsin K activity with a selective substrate spanning its active site. , 2003, Biochemical Journal.

[38]  Luke G Green,et al.  A stepwise huisgen cycloaddition process: copper(I)-catalyzed regioselective "ligation" of azides and terminal alkynes. , 2002, Angewandte Chemie.

[39]  C. Craik,et al.  Selective inhibition of the collagenolytic activity of human cathepsin K by altering its S2 subsite specificity. , 2002, Biochemistry.

[40]  Morten Meldal,et al.  Peptidotriazoles on solid phase: [1,2,3]-triazoles by regiospecific copper(i)-catalyzed 1,3-dipolar cycloadditions of terminal alkynes to azides. , 2002, The Journal of organic chemistry.

[41]  L. Juliano,et al.  New, Sensitive Fluorogenic Substrates for Human Cathepsin G Based on the Sequence of Serpin-reactive Site Loops* , 1999, The Journal of Biological Chemistry.

[42]  G. Dranoff,et al.  Cathepsin S required for normal MHC class II peptide loading and germinal center development. , 1999, Immunity.

[43]  J G Gleason,et al.  Design of potent and selective human cathepsin K inhibitors that span the active site. , 1997, Proceedings of the National Academy of Sciences of the United States of America.

[44]  I. H. Segel.  Enzyme Kinetics: Behavior and Analysis of Rapid Equilibrium and Steady-State Enzyme Systems , 1975 .

[45]  A. Barrett,et al.  L-trans-Epoxysuccinyl-leucylamido(4-guanidino)butane (E-64) and its analogues as inhibitors of cysteine proteinases including cathepsins B, H and L. , 1982, The Biochemical journal.