LGD-5552, an Antiinflammatory Glucocorticoid Receptor Ligand with Reduced Side Effects, in Vivo
نویسندگان
چکیده
منابع مشابه
Antiinflammatory glucocorticoid receptor ligand with reduced side effects exhibits an altered protein-protein interaction profile.
Glucocorticoids are commonly used antiinflammatory agents whose use is limited by side effects. We have developed a series of glucocorticoid receptor (GR) ligands that retain the strong antiinflammatory activity of conventional glucocorticoids with reduced side effects. We present a compound, LGD5552, that binds the receptor efficiently and strongly represses inflammatory gene expression. LGD55...
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Glucocorticoids (GCs) are widely used to treat inflammatory diseases. However, they cause debilitating side effects, which limit the use of these compounds. In the past decade, many researchers have attempted to find so-called dissociated GCs that have separate distinct transactivation and transrepression activities. Anti-inflammation of GCs is a result of glucocorticoid receptor (GR)-mediated ...
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Non-steroidal anti-inflammatory drugs (NSAIDs) are a widely prescribed group of drugs, known to be responsible for many cases of gastroduodenal ulcers by inhibiting cyclo-oxygenase (1). The incidence of side effects while taking NSAID therapy is high, and has been reported to approach 70% in patients receiving long-term therapy. The most frequent complications are those involving the gastroduod...
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OBJECTIVE To describe the main undesirable side effects of glucocorticoid therapy, mechanisms of action and the necessary measures to minimize side effects. SOURCES Author's experience, supplemented with papers published in MEDLINE. SUMMARY OF THE FINDINGS The principles for minimizing undesirable side effects of glucocorticoid therapy include: a) only use glucocorticoids if they are essent...
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Hormones are characteristically secreted in distinct pulses. Corticosterone (in rodents) and cortisol (in human) show profound circadian and ultradian rhythmicity which results in rapid changes in ligand concentration in the circulating blood. The pattern of ultradian glucocorticoid levels shows genetic modulation, can change according to the physiological and pathological status of the animal ...
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ژورنال
عنوان ژورنال: Endocrinology
سال: 2008
ISSN: 0013-7227,1945-7170
DOI: 10.1210/en.2007-1353