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Showing 1 to 20 of 47 for “"bisphosphonates"”.
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Osteonecrosis of the jaw in association to bisphosphonates
… of the jaw. The inhibitory effects of bisphosphonates on osteoclasts and its antiangiogenic properties have been examined as possible mechanisms to induce osteonecrosis of the jaw. The incidence of ONJ in osteoporosis patients receiving bisphosphonate treatment is <1 in 100,000, and in …
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An Improved Understanding of Bisphosphonates Through Computational Techniques
A number of bisphosphonates are currently used to treat human bone resorption disorders. In recent years, these compounds have been shown to have additional biological properties, such as the ability to inhibit the growth of parasite cells and the ability to stimulate human gammadelta T cells. We …
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Bisphosphonates and Aryloxyethyl Thiocyanate Derivatives: New Drugs Against Trypanosomatid Parasites
All together, this work represents a new approach to chemotherapy of important and difficult to treat diseases with a group of safe and well understood compounds not previously thought to be useful in infectious diseases.
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Experimental and Computational Study of Bisphosphonates Targeting Isoprenoid Biosynthesis Pathway
Bisphosphonates are a class of drugs widely used to treat bone resorption diseases. Recently, bisphosphonates have been found to have anti-cancer, anti-parasitic, anti-bacterial and herbicidal activity. They also have the unexpected property of activating human gammadelta T cells to kill tumor …
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Isoprenoid Biosynthesis Pathway as a Drug Target for Bisphosphonates: Transcriptional Profile Investigation
Bisphosphonates are known as potent inhibitors of the enzyme farnesyl diphosphate synthase (FPPS) and are clinically used to treat bone related disorders such as osteoporosis and bone cancer. Here we describe the development, testing and study of the mechanism of action of novel bisphosphonates as …
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The Development and Characterisation of a Peptide Delivery Platform to Interrogate the Anticancer Effects of Bisphosphonates
… However, the in vivo therapeutic use of bisphosphonates is limited due to low bioavailability and adverse effects such as necrosis of the jaw. When administered intravenously, free bisphosphonates preferentially bind to the bone microenvironment with only negligible internalisation in …
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NMR, Crystallographic and Computational Investigations of Peptides, Proteins and Bisphosphonates: New Paradigms for Rational Drug Design
… This dissertation explores the potential use of bisphosphonates, a class of molecules currently used clinically in humans for treating bone resorption diseases like osteoporosis, Paget's disease etc, as anti-parasitic, anti-bacterial and anti-cancer agents. The focus of this work can be broadly …
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The Role of Bisphosphonates and Osteoblast Lineage Cells in Promoting Osteogenic and Angiogenic Processes Necessary for Bone Repair
… active anti-resorptive pharmaceuticals such as bisphosphonates have been linked to nonhealing stress fractures called Atypical Femoral Fractures (AFFS). Animal models of full fracture and stress fracture have demonstrated that angiogenesis is critically important for osteogenesis and subsequent …
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The Effects of Bisphosphonates on Bone Remodeling: Analysis of Microdamage Targeting by BMUs, BMU Velocity and Crack Surface Density
… the damage. Additionally it was believed that bisphosphonates would have a suppressive force on the BMU's ability to seek out and remove microdamage. This study explored a further hypothesis that bisphosphonates would decrease BMU velocity and osteonal area while increasing crack surface …
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Farnesyl Pyrophosphate/geranylgeranyl Pyrophosphate Synthase of Toxoplasma Gondii: Its Role in the Parasite Isoprenoid Pathway and as a Target for Bisphosphonates
… of TgFGGPS as the molecular target of bisphosphonates in this work provides a key tool for rational-based drug design. In addition, this work represents a new approach to chemotherapy of toxoplasmosis with a group of safe and easy to prepare compounds.
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New Chemotherapeutic Approaches for the Treatment of Parasitic Protozoan Diseases
… and screening (in vitro and in vivo) of bisphosphonates as a novel class of anti-parasitic agents. The infectious agents targeted in this study are Trypanosoma brucei, Trypanosoma cruzi, Toxoplasma gondii, Leishmania spp., and Plasmodium falciparum. These parasites are responsible for …
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Applications of Solid State Nuclear Magnetic Resonance Spectroscopy as a Tool for Structure Based Drug Design
… factor staphyloxanthin in Staphylococcus aureus. Bisphosphonates, currently used to treat osteoporosis, have also been found to inhibit the formation of farnesyl diphosphate by binding to the farnesyl diphosphate synthase enzyme. Bisphosphonates are also interesting in context of cancer …
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ASSOCIATION BETWEEN CONCOMITANT USE OF BISPHOSPHONATES AND SEROTONIN REUPTAKE INHIBITORS AND INCREASED RISK OF OSTEOPOROTIC-RELATED FRACTURES: AMONG COMMUNITY-DWELLING POSTMENOPAUSAL WOMEN
… older postmenopausal women 65 years or older. Bisphosphonates (BPs) and selective serotonin reuptake inhibitors (SSRIs) or serotonin norepinephrine reuptake inhibitors (SNRIs) are commonly used medications to treat these conditions. Inhibitory effects of BPs on osteoclasts are responsible for …
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Approaches to Improve the Structure and Function of the Skeleton in Chronic Kidney Disease
… following key questions: (1) to what degree do bisphosphonates, an approved pharmacological agent used in metabolic bone disease, accumulate in the skeleton of animals with CKD; (2) can smaller and more frequent doses of bisphosphonates alter skeletal accumulation and improve cortical …
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Influence of Mechanical Stimulation on the Quantity and Quality of Bone During Modeling
… bone diseases prior to fracture often involves bisphosphonates (current gold-standard in osteoporosis care and prevention). Although bisphosphonates decrease fracture incidence, they often improve bone mass without regard for bone quality. Thus, although bisphosphonates increase the amount of …
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Osteonecrosis. Prognosis and Prevention of the Consequences of Osteonecrosis
… of the knee (SPONK), who were treated with bisphosphonates and evaluated regarding secondary degenerative changes. These 17 treated patients were compared to a previously untreated control group (paper 2). In paper 2, an almost life long follow-up of 40 SPONK patients was conducted. The …
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Targeting isoprenoid and quinone biosynthesis for antimicrobial discovery
… inhibit the enzyme, which is also inhibited by bisphosphonates. The most active inhibitors (Ki ~ 200 nM) were N-alkyl analogs of zoledronate containing ~C6 alkyl side-chains. They were modestly active against S. aureus cell growth, and growth inhibition was partially “rescued” by addition of …
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Comparison of Pharmacologic Treatment on Bone Mineral Density in Patients with Osteopenia
… was carried out to compare effectiveness of bisphosphonates and calcium and vitamin D supplements on bone mineral density in patients with osteopenia. METHOD: We evaluated the data of 94 patients who were diagnosed as having osteopenia with bone mineral densitometry in the health promotion …
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ISPH fusion proteins, ISPH inhibition, and bisphosphonate mechanism of action
… part of this work, the mechanism of action of bisphosphonates against cancer cell lines were studied. There are two types of bisphosphonates described in the literature: nitrogen containing (NBPs) and non-nitrogen containing bisphosphonates (NNBPs). These drugs are a major class of drugs …
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Bone Mass Preservation and Fracture Risk Assessment with Bisphosphonate Therapy During Spaceflight
… success of the mission and postflight recovery. Bisphosphonates may be able to counteract this bone loss by altering the remodeling process. These drugs increase bone mass, thus reducing fracture risk, but also lead to increased levels of fatigue microdamage. Fracture risk can be lowered by …
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