It is generally acknowledged that histamine is an important regulator of a plethora of (patho) physiological conditions and exerts its actions through the interaction with four histamine receptor subtypes. All these receptors belong to the family of heptahelical GPCR's and are considered as a promising molecular targets for drug development.
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11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1, cortisone reductase, HSD11B1, 11beta-hydroxysteroid dehydrogenase type 1,11beta-HSD1) is an enzyme that is involved in glucocorticoid regulation by catalyzing the conversion of inactive cortisone to its active form cortisol. These hormones regulate several physiological processes, and modulation of glucocorticoid action has been implicated as a potential treatment for a variety of diseases.
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Several glycoprocessing enzymes and glycoreceptors have been recognized as important targets for therapeutic intervention. This concept has inspired the development of important classes of therapeutics, such as anti-influenza, anti-inflammatory, Gaucher’s disease, hepatitis and cancer drugs.
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CREB Binding Protein (CREBBP) is a coactivator of transcription factor CREB that activates genes in cAMP transcriptional pathway. The coactivator binds to transcription factor activation domains positions histone acetyltransferases near specific nucleosomes in target gene promoter regions, recognizing the acetylated lysine residue.
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Post-translational modifications, such as acetylation or phosphorylation, play a crucial role in the regulation of gene transcription in eukaryotes. Different subtypes of histone acetyltransferases (HATs) catalyze the acetylation of histones on specific lysine residues.
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