LY353381·HCl: An Improved Benzothiophene Analog with Bone Efficacy Complementary to Parathyroid Hormone-(1–34)
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چکیده
منابع مشابه
Dronedarone, an amiodarone analog with improved anti-Leishmania mexicana efficacy.
Dronedarone and amiodarone are cationic lipophilic benzofurans used to treat cardiac arrhythmias. They also have activity against the parasitic protozoan Trypanosoma cruzi, the causative agent of Chagas' disease. They function by disrupting intracellular Ca2+ homeostasis of the parasite and by inhibiting membrane sterol (ergosterol) biosynthesis. Amiodarone also has activity against Leishmania ...
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A two-phase system in vitro has been developed for studying the bone-mobilizing effects of parathyroid hormone. Phase I consists of the incubation of hormone with ascites cells, and Phase II is the incubation of Phase I supernatant with dead bone powder. The mobilization of labeled calcium from this powder is the index of hormonal activity. The response to hormone is apparent at lo-* M hormone,...
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Osteoporosis is a major public health problem despite widespread use of bisphosphonate therapy. PTH(1-34) is a more effective treatment; but its use has been limited by side effects (hypercalcemia, tumor risk) and inconvenient dosing (daily injection). Long-acting forms of PTH are also effective but cause severe hypercalcemia, presumably from effects in kidney. We hypothesized that targeted del...
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Transcription of the mouse parathyroid hormone (PTH)/PTH-related peptide (PTHrP) receptor (PTHR) gene is controlled by promoters P1 and P2. We performed transcript-specific in situ hybridization and found that P2 is the predominant promoter controlling PTHR gene expression in bone and cartilage. Treatment with 1alpha, 25-dihydroxyvitamin D3 (D3) in vivo specifically downregulated P2-specific tr...
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Metastasis of breast cancers is a common and serious clinical problem, with up to one third of women with earlystage breast cancer eventually dying of the disease. Of all patients with distant spread of the cancer, 70% have bone metastases (1,2), reflective of the observations of Paget (3) that breast cancers had a particular predilection to grow in bone. A special property required of cancer c...
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ژورنال
عنوان ژورنال: Endocrinology
سال: 1998
ISSN: 0013-7227,1945-7170
DOI: 10.1210/endo.139.11.6307