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Natural inhibitors targeting osteoclast-mediated bone resorption. 2006

Guang-Zhi Zeng, and Ning-Hua Tan, and Xiao-Jiang Hao, and Quan-Zhang Mu, and Rong-Tao Li
State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650204, China; Graduate School of the Chinese Academy of Sciences, Beijing 100039, China.

Human cathepsin K, matrix metalloproteinase 9, and alpha(V)beta(3) integrin are the key regulators in osteoclast-mediated bone resorption. In this paper, we found natural inhibitors 1-10 for them by enzyme inhibition assays. Inhibitors 1-7, 8-9, and 10 are novel inhibitors of human cathepsin K, matrix metalloproteinase 9, and alpha(V)beta(3), respectively.

UI MeSH Term Description Entries
D010010 Osteoclasts A large multinuclear cell associated with the BONE RESORPTION. An odontoclast, also called cementoclast, is cytomorphologically the same as an osteoclast and is involved in CEMENTUM resorption. Odontoclasts,Cementoclast,Cementoclasts,Odontoclast,Osteoclast
D011480 Protease Inhibitors Compounds which inhibit or antagonize biosynthesis or actions of proteases (ENDOPEPTIDASES). Antiprotease,Endopeptidase Inhibitor,Endopeptidase Inhibitors,Peptidase Inhibitor,Peptidase Inhibitors,Peptide Hydrolase Inhibitor,Peptide Hydrolase Inhibitors,Peptide Peptidohydrolase Inhibitor,Peptide Peptidohydrolase Inhibitors,Protease Antagonist,Protease Antagonists,Antiproteases,Protease Inhibitor,Antagonist, Protease,Antagonists, Protease,Hydrolase Inhibitor, Peptide,Hydrolase Inhibitors, Peptide,Inhibitor, Endopeptidase,Inhibitor, Peptidase,Inhibitor, Peptide Hydrolase,Inhibitor, Peptide Peptidohydrolase,Inhibitor, Protease,Inhibitors, Endopeptidase,Inhibitors, Peptidase,Inhibitors, Peptide Hydrolase,Inhibitors, Peptide Peptidohydrolase,Inhibitors, Protease,Peptidohydrolase Inhibitor, Peptide,Peptidohydrolase Inhibitors, Peptide
D001862 Bone Resorption Bone loss due to osteoclastic activity. Bone Loss, Osteoclastic,Osteoclastic Bone Loss,Bone Losses, Osteoclastic,Bone Resorptions,Loss, Osteoclastic Bone,Losses, Osteoclastic Bone,Osteoclastic Bone Losses,Resorption, Bone,Resorptions, Bone
D002403 Cathepsins A group of lysosomal proteinases or endopeptidases found in aqueous extracts of a variety of animal tissues. They function optimally within an acidic pH range. The cathepsins occur as a variety of enzyme subtypes including SERINE PROTEASES; ASPARTIC PROTEINASES; and CYSTEINE PROTEASES. Cathepsin
D004791 Enzyme Inhibitors Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction. Enzyme Inhibitor,Inhibitor, Enzyme,Inhibitors, Enzyme
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D015195 Drug Design The molecular designing of drugs for specific purposes (such as DNA-binding, enzyme inhibition, anti-cancer efficacy, etc.) based on knowledge of molecular properties such as activity of functional groups, molecular geometry, and electronic structure, and also on information cataloged on analogous molecules. Drug design is generally computer-assisted molecular modeling and does not include PHARMACOKINETICS, dosage analysis, or drug administration analysis. Computer-Aided Drug Design,Computerized Drug Design,Drug Modeling,Pharmaceutical Design,Computer Aided Drug Design,Computer-Aided Drug Designs,Computerized Drug Designs,Design, Pharmaceutical,Drug Design, Computer-Aided,Drug Design, Computerized,Drug Designs,Drug Modelings,Pharmaceutical Designs
D056657 Cathepsin K A cysteine protease that is highly expressed in OSTEOCLASTS and plays an essential role in BONE RESORPTION as a potent EXTRACELLULAR MATRIX-degrading enzyme.
D061965 Matrix Metalloproteinase Inhibitors Compounds that inhibit the enzyme activity or activation of MATRIX METALLOPROTEINASES. Collagenase Inhibitor,Gelatinase Inhibitor,MMP Inhibitor,Matrix Metalloproteinase Inhibitor,Collagenase Inhibitors,Gelatinase Inhibitors,MMP Inhibitors,Stromelysin Inhibitors,Inhibitor, Collagenase,Inhibitor, Gelatinase,Inhibitor, MMP,Inhibitor, Matrix Metalloproteinase,Inhibitors, Collagenase,Inhibitors, Gelatinase,Inhibitors, MMP,Inhibitors, Matrix Metalloproteinase,Inhibitors, Stromelysin,Metalloproteinase Inhibitor, Matrix,Metalloproteinase Inhibitors, Matrix
D039302 Integrin alphaVbeta3 An integrin that binds to a variety of plasma and extracellular matrix proteins containing the conserved RGD amino acid sequence and modulates cell adhesion. Integrin alphavbeta3 is highly expressed in OSTEOCLASTS where it may play role in BONE RESORPTION. It is also abundant in vascular smooth muscle and endothelial cells, and in some tumor cells, where it is involved in angiogenesis and cell migration. Although often referred to as the vitronectin receptor there is more than one receptor for vitronectin (RECEPTORS, VITRONECTIN). Integrin alpha-v beta-3,Receptors, alpha-v beta-3 Integrin,Vitronectin Receptor,alpha-v beta-3 Integrin Receptors,Integrin alpha v beta 3,Receptor, Vitronectin,Receptors, alpha v beta 3 Integrin,alpha v beta 3 Integrin Receptors,alpha-v beta-3, Integrin,alphaVbeta3, Integrin,beta-3, Integrin alpha-v

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