Transglutaminase-Catalyzed Transamidation: A Novel Mechanism for Rac1 Activation by 5-Hydroxytryptamine2A Receptor Stimulation
نویسندگان
چکیده
منابع مشابه
Transglutaminase-catalyzed transamidation: a novel mechanism for Rac1 activation by 5-hydroxytryptamine2A receptor stimulation.
Transglutaminase (TGase)-induced activation of small G proteins via 5-hydroxytryptamine (HT)(2A) receptor signaling leads to platelet aggregation (Cell 115:851-862, 2003). We hypothesize that stimulation of 5-HT(2A) receptors in neurons activates TGase, resulting in transamidation of serotonin to a small G protein, Rac1, thereby constitutively activating Rac1. Using immunoprecipitation and immu...
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We have used a cell-based functional assay to define the pharmacological profiles of a wide range of central nervous system active compounds as agonists, competitive antagonists, and inverse agonists at almost all known monoaminergic G-protein-coupled receptor (GPCR) subtypes. Detailed profiling of 40 antipsychotics confirmed that as expected, most of these agents are potent competitive antagon...
متن کاملTransamidation reactions catalyzed by cathepsin C.
Previous publications from this laboratory (l-3) have described the catalysis of transamidation reactions by the proteinases papain, ficin, and crystalline chymotrypsin. In addition, preliminary experiments were reported on replacement reactions catalyzed by beef spleen cathepsin C, an intracellular endopeptidase of animal tissues, which resembles pancreatic chymotrypsin in its specificity. The...
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The serotonin (5-HT)2A and 5-HT2C receptors share a high degree of sequence homology and have very similar pharmacological profiles. Although it is generally believed that the cellular signal transduction mechanisms activated by these receptors are indistinguishable, recent data suggest significant differences in their signaling cascades. In this study we explored differences in the characteris...
متن کاملSpecificity of papain-catalyzed transamidation reactions.
In the experiments reported in the present communication, these studies have been extended with special reference to the specificity of the enzyme toward the dipeptide used as replacement agent. It had been suggested (1) that the value of pKz’ of a dipeptide is a determining factor in the efficiency with which it can participate in a transamidation reaction at ‘a given pH. This suggestion has b...
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ژورنال
عنوان ژورنال: Journal of Pharmacology and Experimental Therapeutics
سال: 2008
ISSN: 0022-3565,1521-0103
DOI: 10.1124/jpet.107.135046