osteoporosis/protease

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Iatrogenic Cushing's syndrome with osteoporosis and secondary adrenal failure in human immunodeficiency virus-infected patients receiving inhaled corticosteroids and ritonavir-boosted protease inhibitors: six cases.

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Ritonavir, a protease inhibitor (PI), is a potent inhibitor of cytochrome P450 3A4. This pharmacological effect, even at low doses (

Regulation of insulin-like growth factor-binding protein-4 protease activity by estrogen and parathyroid hormone in SaOS-2 cells: implications for the pathogenesis of postmenopausal osteoporosis.

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The cellular mechanisms involved in the accelerated bone loss occurring in association with estrogen deprivation as seen following the menopause are not fully understood. Insulin-like growth factor-I (IGF-I) is the local regulator of osteoblasts and one of its binding proteins, insulin-like growth

Pharmacological inhibition of cathepsin K: A promising novel approach for postmenopausal osteoporosis therapy.

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Osteoporosis is a metabolic bone disease that is characterized by heightened state of bone resorption accompanied by diminished bone formation, leading to a reduction of bone mineral density (BMD) and deterioration of bone quality, thus increasing the risk of developing fractures. Molecular insight

Development of Potent, Protease-Resistant Agonists of the Parathyroid Hormone Receptor with Broad β Residue Distribution.

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The parathyroid hormone receptor 1 (PTHR1) is a member of the B-family of GPCRs; these receptors are activated by long polypeptide hormones and constitute targets of drug development efforts. Parathyroid hormone (PTH, 84 residues) and PTH-related protein (PTHrP, 141 residues) are natural agonists of

Iatrogenic Cushing's syndrome and osteoporosis due to an interaction between fluticasone and ritonavir.

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The advent of highly active antiretroviral therapy for HIV infection dramatically changed the landscape of the disease. Ritonavir, a protease inhibitor (PI) frequently used in low doses to 'boost' the concentrations of other PIs, inhibits the cytochrome P450 3A4 isoenzyme, a common metabolic pathway

Cathepsin K inhibitors: a novel target but promising approach in the treatment of osteoporosis.

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Osteoporosis is a pathologic process characterized by low bone mass with skeletal fragility and an increased risk of fracture. It occurs due to an imbalance between bone resorption and formation. Although current antiresorptive therapy halts bone loss, it does not cure the condition as it also

Cathepsin K inhibitor-polymer conjugates: potential drugs for the treatment of osteoporosis and rheumatoid arthritis.

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The role of the newly discovered cysteine protease, cathepsin K, in osteoporosis and rheumatoid arthritis is reviewed. The current development of cathepsin K inhibitors and their targeted delivery using synthetic polymer carriers are discussed. Future challenges and possible strategies to improve

Ketoamide-based inhibitors of cysteine protease, cathepsin K: P3 modifications.

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Osteoporosis is a disease characterized by skeletal fragility. Cathepsin K, a lysosomal cysteine protease, has been implicated in the osteoclast mediated bone resorption. Inhibitors of this protease could potentially treat this skeletal disease. The present work describes exploration of the spatial

Design of potent, selective, and orally bioavailable inhibitors of cysteine protease cathepsin k.

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Osteoclast-mediated bone matrix resorption has been attributed to cathepsin K, a cysteine protease of the papain family that is abundantly and selectively expressed in osteoclast. Inhibition of cathepsin K could potentially be an effective method to prevent osteoporosis. Structure-activity studies

Microbial inhibitors of cysteine proteases.

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Cysteine proteases are one of the major classes of proteolytic enzymes involved in a number of physiological and pathological processes in plants, animals and microorganisms. When their synthesis, activity and localization in mammalian cells are altered, they may contribute to the development of

Reduced serum corin levels in patients with osteoporosis.

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BACKGROUND Corin is a cardiac protease that activates the natriuretic peptides. Corin is also expressed in chondrocytes and bone marrow-derived mesenchymal stem cells that undergo osteogenic differentiation, suggesting a potential role of corin in bone formation and homeostasis. METHODS To test if

[Cathepsin K and matrix metalloproteases activity in the bone tissue of OXYS rats with developing osteoporosis].

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The comparative study of activity of cysteine protease cathepsin K and matrix metalloproteases (MMPs) in bone tissue of accelerated senescent OXYS rats with early ageing comparatively to Wistar rats of the same age was performed. Early development osteoporosis is a typical feature of OXYS rats. In

Discovery of a New Class of Cathepsin K Inhibitors in Rhizoma Drynariae as Potential Candidates for the Treatment of Osteoporosis.

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Rhizoma Drynariae (RD), as one of the most common clinically used folk medicines, has been reported to exert potent anti-osteoporotic activity. The bioactive ingredients and mechanisms that account for its bone protective effects are under active investigation. Here we adopt a novel in silico target

Immunohistochemical expression of caspase-3, caspase-5, caspase-7 and apoptotic protease-activating factor-1 (APAF-1) in the liver and kidney of rats exposed to zoledronic acid (ZOL) and basic fibroblast growth factor (bFGF).

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BACKGROUND Bisphosphonates (BPs) like zoledronic acid (ZOL) are widely used for the treatment of different diseases such as osteoporosis, metastatic bone diseases and hypercalcaemia. However, the effects of BPs on apoptosis of the liver and kidney after treatment are unclear. Furthermore, basic

Osteoporosis and multiple fractures in an antiretroviral-naive, HIV-positive child.

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As a result of the increased incidence of osteopenia and osteoporosis in HIV-infected patients, numerous publications have suggested that there may be a link between bone metabolism alterations and HIV infection. The early bone loss seen in these patients was initially attributed to the use of

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