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Showing 1-30 of 41 results for "G110" within Papers
B Holmes et al.
Drugs, 26(3), 212-229 (1983-09-01)
Guanabenz is an orally active central alpha 2-adrenoceptor agonist. Its antihypertensive action is thought to result from a decrease in sympathetic outflow from the brain to the peripheral circulatory system as a result of stimulation of central alpha 2-adrenoceptors. In
Jonghwa Won et al.
European journal of pharmacology, 854, 320-327 (2019-04-23)
Alpha 2 (α2-) adrenoceptor agonists, such as clonidine or dexmedetomidine, have been found to inhibit hyperpolarization-activated, cyclic nucleotide-modulated (HCN) channels, not only by reducing intracellular cyclic AMP levels but also by directly blocking HCN channels. In this study, we examined
Déborah Tribouillard-Tanvier et al.
PloS one, 3(4), e1981-e1981 (2008-04-24)
Prion-based diseases are incurable transmissible neurodegenerative disorders affecting animals and humans. Here we report the discovery of the in vivo antiprion activity of Guanabenz (GA), an agonist of alpha2-adrenergic receptors routinely used in human medicine as an antihypertensive drug. We
Melissa J Fullwood et al.
Progress in molecular biology and translational science, 106, 75-106 (2012-02-22)
The unfolded protein response, also known as endoplasmic reticulum (ER) stress, has been implicated in numerous human diseases, including atherosclerosis, cancer, diabetes, and neurodegenerative disorders. Protein misfolding activates one or more of the three ER transmembrane sensors to initiate a
Pavel Tsaytler et al.
The FEBS journal, 280(2), 766-770 (2012-02-22)
Selective and reversible phosphorylation is one of the most common post-translational modifications of proteins. Although kinase inhibitors are popular in drug development programmes, selective pharmacological manipulation of phosphatase activity has been challenging to achieve. We review recent advances in the
Suzana Dos Reis et al.
Biochimie, 93(6), 1047-1054 (2011-03-15)
The ribosome, the protein synthesis machinery of the cell, has also been implicated in protein folding. This activity resides within the domain V of the main RNA component of the large subunit of the ribosome. It has been shown that
Juliette Humeau et al.
Cell death & disease, 11(6), 433-433 (2020-06-10)
The integrated stress response is characterized by the phosphorylation of eukaryotic initiation factor-2α (eIF2α) on serine 51 by one out of four specific kinases (EIF2AK1 to 4). Here we provide three series of evidence suggesting that macroautophagy (to which we
Anwar Y Dunbar et al.
Drug metabolism and disposition: the biological fate of chemicals, 34(9), 1448-1456 (2006-06-02)
It is established that guanabenz inhibits neuronal nitric-oxide (NO) synthase (nNOS) and causes the enhanced proteasomal degradation of nNOS in vivo. Although the time- and NADPH-dependent inhibition of nNOS has been reported in studies where guanabenz was incubated with crude
Cécile Voisset et al.
Biotechnology journal, 6(6), 668-673 (2011-05-14)
In addition to its involvement in protein synthesis, the ribosome is implicated in protein folding. Some co-translational events, such as the rhythm of protein synthesis, the passage through the exit tunnel of the ribosome, or the interaction with ribosome-associated chaperones
Domenic A Sica
Journal of clinical hypertension (Greenwich, Conn.), 9(5), 399-405 (2007-05-09)
Centrally acting agents stimulate alpha(2) receptors and/or imadozoline receptors on adrenergic neurons situated within the rostral ventrolateral medulla and, in so doing, sympathetic outflow is reduced. Centrally acting agents also stimulate peripheral alpha(2) receptors, which, for the most part, is
Denis Fourches et al.
Chemical research in toxicology, 23(1), 171-183 (2009-12-18)
Drug-induced liver injury is one of the main causes of drug attrition. The ability to predict the liver effects of drug candidates from their chemical structures is critical to help guide experimental drug discovery projects toward safer medicines. In this
Haifeng Ye et al.
Proceedings of the National Academy of Sciences of the United States of America, 110(1), 141-146 (2012-12-19)
Synthetic biology has significantly advanced the design of genetic devices that can reprogram cellular activities and provide novel treatment strategies for future gene- and cell-based therapies. However, many metabolic disorders are functionally linked while developing distinct diseases that are difficult
Kuichang Yuan et al.
Peptides, 29(7), 1207-1215 (2008-04-02)
Sympathetic nervous system and atrial natriuretic peptide (ANP) system play fundamental roles in the regulation of cardiovascular functions. Overactivity of sympathetic nervous system can lead into cardiovascular diseases such as heart failure and hypertension. The present study aimed to define
Kuichang Yuan et al.
Regulatory peptides, 154(1-3), 112-120 (2009-03-04)
Cold exposure induces hypertension and cardiac hypertrophy via sympathetic activation. The sympathetic nervous system is fundamentally important for the regulation of cardiac atrial natriuretic peptide (ANP) secretion. The present study aimed to define changes in ANP level with renal functions
Yu Chen et al.
The Journal of clinical investigation, 123(12), 5119-5134 (2013-11-16)
A systems pharmacological approach that capitalizes on the characterization of intracellular signaling networks can transform our understanding of human diseases and lead to therapy development. Here, we applied this strategy to identify pharmacological targets for the treatment of Stargardt disease
Fernando G Vieira et al.
PloS one, 10(8), e0135570-e0135570 (2015-08-20)
Amyotrophic lateral sclerosis (ALS) is a progressive neurodegenerative disease characterized by loss of motor neurons. The mechanisms leading to motor neuron degeneration in ALS are unclear. However, there is evidence for involvement of endoplasmic reticulum (ER) stress and the unfolded
R D Wainford et al.
British journal of pharmacology, 166(1), 210-220 (2011-09-08)
Activation of brain α(2) -adrenoceptors in conscious rodents decreases heart rate (HR) and mean arterial blood pressure (MAP) and increases urine output and urinary sodium excretion. In vitro, α(2) -adrenoceptor stimulation activates Gα(i(1-3)) , Gα(o) and Gα(s) -subunit protein-gated signal
Caroline Norez et al.
European journal of pharmacology, 592(1-3), 33-40 (2008-07-22)
In cystic fibrosis respiratory epithelial cells, the absence or dysfunction of the chloride channel CFTR (Cystic Fibrosis Transmembrane conductance Regulator) results in reduced chloride ion transport. In contrast, Ca2+-stimulated Cl- secretion is intact in cystic fibrosis airway epithelia. One possible
Phedias Diamandis et al.
Nature chemical biology, 3(5), 268-273 (2007-04-10)
The identification of self-renewing and multipotent neural stem cells (NSCs) in the mammalian brain holds promise for the treatment of neurological diseases and has yielded new insight into brain cancer. However, the complete repertoire of signaling pathways that governs the
Gabriel Marcelín-Jiménez et al.
Bioanalysis, 1(1), 47-55 (2009-04-01)
The aim of the present work was to develop a chromatographic technique coupled with mass spectrometry for the measurement of lamotrigine in plasma. Lamotrigine and guanabenz (internal standard) were measured by selected reaction monitoring. The method was validated and applied
Nicolas Barbezier et al.
EMBO molecular medicine, 3(1), 35-49 (2011-01-05)
Oculopharyngeal muscular dystrophy (OPMD) is an adult-onset syndrome characterized by progressive degeneration of specific muscles. OPMD is caused by extension of a polyalanine tract in poly(A) binding protein nuclear 1 (PABPN1). Insoluble nuclear inclusions form in diseased muscles. We have
Bernd Clement et al.
Drug metabolism and disposition: the biological fate of chemicals, 33(11), 1740-1747 (2005-08-25)
In previous studies, it was shown that liver microsomes from rabbit, rat, pig, and human are involved in the reduction of N-hydroxylated amidines, guanidines, and amidinohydrazones of various drugs and model compounds (Drug Metab Rev 34: 565-579). One responsible enzyme
Fabienne Massé et al.
Behavioural brain research, 164(1), 17-28 (2005-08-06)
Selective serotonin reuptake inhibitors (SSRIs) and serotonin/noradrenaline reuptake inhibitors (SNRIs) has been reported to be efficient in anxiety disorders. Some animal models have demonstrated an anxiolytic-like effect following acute administration, however, it is not yet known how noradrenergic receptors are
Christian Konrad et al.
Antimicrobial agents and chemotherapy, 57(4), 1815-1822 (2013-02-06)
Toxoplasma gondii is an obligate intracellular parasite that permanently infects warm-blooded vertebrates through its ability to convert into a latent tissue cyst form. The latent form (bradyzoite) can reinitiate a life-threatening acute infection if host immunity wanes, most commonly in
Déborah Tribouillard-Tanvier et al.
PloS one, 3(5), e2174-e2174 (2008-05-15)
6-Aminophenanthridine (6AP) and Guanabenz (GA, a drug currently in use for the treatment of hypertension) were isolated as antiprion drugs using a yeast-based assay. These structurally unrelated molecules are also active against mammalian prion in several cell-based assays and in
Jing Yuan et al.
Nature chemical biology, 5(10), 765-771 (2009-09-08)
Studies of gene function and molecular mechanisms in Plasmodium falciparum are hampered by difficulties in characterizing and measuring phenotypic differences between individual parasites. We screened seven parasite lines for differences in responses to 1,279 bioactive chemicals. Hundreds of compounds were
Anais Mockel et al.
The Journal of biological chemistry, 287(44), 37483-37494 (2012-08-08)
Ciliopathies, a class of rare genetic disorders, present often with retinal degeneration caused by protein transport defects between the inner segment and the outer segment of the photoreceptors. Bardet-Biedl syndrome is one such ciliopathy, genetically heterogeneous with 17 BBS genes
Pavel Tsaytler et al.
Science (New York, N.Y.), 332(6025), 91-94 (2011-03-10)
Many biological processes are regulated through the selective dephosphorylation of proteins. Protein serine-threonine phosphatases are assembled from catalytic subunits bound to diverse regulatory subunits that provide substrate specificity and subcellular localization. We describe a small molecule, guanabenz, that bound to
Froylán Ibarra-Velarde et al.
Annals of the New York Academy of Sciences, 1149, 183-185 (2009-01-06)
The aim of the present study was to evaluate the fasciolicide activity of three experimental drugs, selected by an in silico system called TOMOCOMD-CARDD, in sheep. Drugs were identified by the computer system, and, after statistical selection, 24 Pelibuey sheep
Pharmacological modulation of the ER stress response ameliorates oculopharyngeal muscular dystrophy.
Alberto Malerba et al.
Human molecular genetics, 28(10), 1694-1708 (2019-01-17)
Oculopharyngeal muscular dystrophy (OPMD) is a rare late onset genetic disease leading to ptosis, dysphagia and proximal limb muscles at later stages. A short abnormal (GCN) triplet expansion in the polyA-binding protein nuclear 1 (PABPN1) gene leads to PABPN1-containing aggregates
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