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The fact that the BPloopAsn regains its Btx binding
2023-09-18

The fact that the α1-BPloopAsn141 regains its α-Btx binding with a Kd similar to that of the wild type α1 ECD [18], suggests that the AChBP Cys-loop does not interfere with the correct conformation of the mutant ECD. Data from analogous mutants of the human neuronal α7 subunit ECD showed improved li
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The extent to which GPCR oligomerization is a regulated
2023-09-18

The extent to which GPCR oligomerization is a regulated process still remains unclear. Reported effects of ligands on both GPCR homo- and heteromers are highly variable and depend on GPCR subtypes and the specific ligand used. According to our data, chronic treatment of mice with both paroxetine or
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Application of the broad acting HTR
2023-09-18

Application of the broad-acting 5-HTR antagonist methiothepin (Bard et al., 1996, Hoyer et al., 1994, Peroutka, 1990) converted the TBS-induced response of both thalamocortical and intracortical A1 synapses from LTP to LTD, an effect that was mimicked by the selective 5-HT2R antagonist ketanserin (L
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Introduction hydroxytryptamine HT is found throughout the bo
2023-09-18

Introduction 5-hydroxytryptamine (5-HT) is found throughout the body and influences smooth muscle activity in various tissues including the intestine, vasculature and urinary 4E1RCat (Kim and Camilleri, 2000, Klarskov and Horby-Petersen, 1986, Mohammad-Zadeh et al., 2008). The current classificati
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We conducted the largest drug
2023-09-18

We conducted the largest drug screen to date in HPV-positive cancers and identified Aurora kinase inhibitors as effective and understudied drugs in HNSCC and CESC. These drugs cause apoptosis and cell cycle arrest in vitro and decrease tumor size in vivo. This is the first published study to demonst
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Here we report discovery of highly selective pan
2023-09-18

Here we report discovery of highly selective pan-Aurora kinase inhibitors through phenotypic screening. The co-crystal structure of A-317491 bound in the ATP binding site of Aurora A is described, and provides insight into the possible structural basis for the selectivity of the interaction. To i
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br Conclusions In summary the
2023-09-18

Conclusions In summary, the present results showed that ageing diminished arginase activity only in clearance tissues and that l-arginine supplementation did not induce major changes in arginase activity thus refuting a role of arginase in the potential deleterious effects of l-arginine supplemen
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br Concluding remarks and future perspectives While the
2023-09-18

Concluding remarks and future perspectives While the rational engineering of protein-based switches has yet to be fully developed, emerging empirical rules facilitate the construction of tailor-engineered Tankyrase Inhibitors 22 with custom input and output parameters. Both in the context of mole
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Studies have demonstrated that AT plays a greater
2023-09-16

Studies have demonstrated that AT2 plays a greater role in modulating arterial pressure in females than in males. Chronic low-dose infusion of Ang II decreased blood pressure in female rats at a dose that had negligible effects in males. Furthermore, AT2 blockade eliminates the depressor response to
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Evodiamine receptor br The lipoxygenase pathway in diseases
2023-09-16

The 12/15-lipoxygenase pathway in diseases of the nervous system Conclusions and future perspectives Arachidonic Evodiamine receptor and other polyunsaturated fatty acids, and their lipid metabolites, play very important roles in human health and disease. This review has outlined the function
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br ABCA and cancer drug
2023-09-16

ABCA2 and cancer drug response Overall, the expression of ABC transporters has been linked with multidrug resistance phenotypes through the efflux of drugs via ATP-dependent transport. For example, 13 distinct transporters (ABCA2, ABCB1, ABCB4, ABCB11, ABCC1–6 ABCC10, ABCC11 and ABCG2) have been
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br Detection and possible treatments for prostate
2023-09-16

Detection and possible treatments for prostate cancer PC can be diagnosed, by screening for prostate-specific antigen (PSA) and after diagnosis, treatments may include intense observation, radical prostatectomy, radiation, chemotherapy, hormone therapy or vaccination depending on the type and sta
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wee1 br Conclusion br Conflicts of
2023-09-15

Conclusion Conflicts of interest Compliance with ethical standards Introduction Tuberculosis is one of the leading causes of morbidity and mortality, amongst infectious diseases. India is a high burden country for Tuberculosis. Caused by Mycobacterium tuberculosis, it wee1 can present as
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Multiple ASD susceptibility genes converge on cellular pathw
2023-09-15

Multiple ASD susceptibility genes converge on cellular pathways that intersect at the postsynaptic site of glutamatergic synapses (Bourgeron, 2015; Peca & Feng, 2012), the development and maturation of synaptic contacts (Gilman et al., 2011) or synaptic transmission (Li et al., 2014). The majority o
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Based on currently available knowledge autophagy supports ad
2023-09-15

Based on currently available knowledge, autophagy supports adipocytes development and differentiation. In animals with specific skeletal muscle SB 239063 of Atg7, reduced adipogenesis was shown. In rodents, autophagy was decreased in adipose tissue of animals fed with high-fat diet (HFD). In contra
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