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Cys loop GABA receptors are well
2022-06-14

Cys-loop GABA receptors are well-studied targets for insecticides and also play an important role in nematode biology. These receptors are also targets for the anthelmintic piperizine (Accardi et al., 2012). The nematode GABA receptor most studied is the UNC-49 receptor which plays a role in muscle
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br Acknowledgements We apologize to our distinguished collea
2022-06-14

Acknowledgements We apologize to our distinguished colleagues whose work has not been cited owing to space limitations. This work was funded by the Italian Association for Cancer Research (AIRC, Milan, Italy, IG 14732 to A.M.); Italian Ministry of University and Education (Finanziamenti per la Ri
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OCA has recently been approved for the treatment of patients
2022-06-14

OCA has recently been approved for the treatment of patients with PBC and is under study for diseases such as NASH, PSC and biliary atresia [30], [49]. Up to now, the beneficial effects of OCA have been related to its anti-cholestatic, anti-inflammatory and anti-fibrotic properties. We have here rep
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A great number of proteins entering the
2022-06-14

A great number of proteins entering the nucleus possess a characteristic nuclear localization sequence (NLS) in their primary structure. One of such sequences is the KKKGK motif [30]. It is present in all known muscle (but not liver – except human liver) FBPase sequences (human, rabbit, rat and mous
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po1 australia MMV s distinct mode of inhibition addresses ke
2022-06-14

MMV019313's distinct mode of inhibition addresses key impediments in the development of PfFPPS/GGPPS inhibitors as antimalarial drugs. First, it is the first non-bisphosphonate inhibitor of Plasmodium FPPS/GGPPS with drug-like physicochemical properties satisfying the “Rule of 5” (Van Voorhis et al.
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LY335979 receptor The product chain length determination mec
2022-06-14

The product chain-length determination mechanism of -prenyltransferases has not yet been elucidated, although mutational analyses of highly conserved residues and of characteristic amino LY335979 receptor residues in each subfamily of -prenyltransferases have enabled the understanding of the basic c
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br Experimental br Results and discussion One of the major
2022-06-14

Experimental Results and discussion One of the major challenges of oral drug delivery via nanocarriers is the fairly low efficiency of crossing the intestinal barrier. While there is the possibility of a paracellular transport for polar substances below 1000 Dalton [26], the key mechanism of o
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This connection is supported by studies in the
2022-06-13

This connection is supported by studies in the SIV macaque model of HIV, where treatment with methamphetamine, which greatly enhances CNS dopamine levels (Truong, 2005); increased Pseudo-UTP viral load. Methamphetamine also increased expression of the HIV co-receptor CCR5 in CNS macrophages, thereby
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While more detailed molecular studies on the mechanistic bas
2022-06-13

While more-detailed molecular studies on the mechanistic basis for heightened H3 receptor function in PAE rats are underway, we have also been exploring whether PAE alters other markers of histaminergic neurotransmission in affected brain regions. One question is whether PAE affected the number of h
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These and other observations presented
2022-06-13

These and other observations presented in the elegant, rigorous study by Thomas et al. (2018) clarify a puzzling enigma regarding the Rab specificities of yeast TRAPP complexes and further highlight an important though under-appreciated role for the C-terminal HVD of Rabs in GEF substrate selection.
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br Introduction Depressive disorder is a syndrome characteri
2022-06-13

Introduction Depressive disorder is a syndrome characterized by a group of heterogeneous symptoms that affect more than 350 million people worldwide, 4% of world population (WHO, 2012). The WHO estimates depression will be the leading global cause of disability in 2020, with tremendous economic c
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We previously evaluated the immuno modulatory efficacy of GS
2022-06-13

We previously evaluated the immuno-modulatory efficacy of GSNO in different EAE models and reported prophylactic and therapeutic efficacy of GSNO against the clinical disease of EAE [22], [36]. GSNO inhibited the IL-6-induced STAT3 activation (Tyr705 phosphorylation) by S-nitrosylation of the STAT3
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The ability of FFA to elevate intracellular levels
2022-06-13

The ability of FFA4 to elevate intracellular levels of Ca2+5, 38, 39, 40 provided early predictions of a key role of the phosphoinositidase C-linked G proteins Gq and/or G11 in transduction of signals from this receptor, while later studies that examined production of inositol phosphates [41] provid
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Starting from commercially available dioxaspiro decan
2022-06-13

Starting from commercially available 1,4-dioxaspiro[4.5]decan-8-ol, was prepared by the synthetic sequence illustrated in . Aromatic nucleophilic substitution of 1,4-dioxaspiro[4.5]decan-8-ol, followed by an Exendin-4 catalyzed deprotection efficiently gave . A - enriched mixture of (/=∼3/2) was
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Through a large scale phylogenetic analysis of UDG superfami
2022-06-13

Through a large-scale phylogenetic analysis of UDG superfamily in more than 1000 completely sequenced genomes, it is shown that family 3 Mithramycin A can be separated into two clades with the traditional family 3 SMUG1 as one of them (Fig. 1) [31]. UDG enzymes in another clade are present in eubac
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