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br Introduction The discovery that the nitric
2022-05-17
Introduction The discovery that the nitric oxide (NO), soluble guanylate cyclase (sGC), and cyclic guanosine monophosphate (cGMP) pathway mediates erection has led to the use of phosphodiesterase type 5 (PDE-5) inhibitors as the gold standard for treating erectile dysfunction (ED) through the inh
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Subcellular domains where Rac is active show
2022-05-17
Subcellular domains where Rac is active show limited Rho activity and vice versa (Fig. 4). This distinctive patterning in Rho activity is achieved via the downstream Rac effector Par6, an important part of the so-called Par polarity complex. In primary epithelium, the cytoskeleton and associated Rho
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br Acknowledgments We thank Dr
2022-05-17
Acknowledgments We thank Dr Kathleen Sullivan of Merck Research Laboratories for providing the CHO-K1 M 1145 australia expressing an NFAT-β-lactamase reporter and the Gα subunit Gqi5, Dr. Chen Liaw (Arena Pharmaceutical), Ms. Rebecca Kaplan, Mr. Frank Xiaodong Gan for technical assistance, Dr. A
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As part of our discovery
2022-05-17
As part of our discovery efforts searching for small molecule GPR119 agonists, we analyzed active pharmacophores of known agonists from the literature, and found that -methylsulfonylphenyl and substituted 4-hydroxyl piperidine are common fragments. In our initial efforts, we linked these two fragmen
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There are three classes of receptors for herpes
2022-05-16
There are three classes of receptors for herpes virus gD have been described [18,24]. Among those three, herpes virus entry mediator A (HveA) is also known as HVEM. This receptor is a member of the tumor necrosis factor receptor (TNFR) superfamily [25]. The other class of receptors is HveC which is
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GPR can signal through not only
2022-05-16
GPR40 can signal through not only IP3 but also cAMP depending upon the type of agonist ligand used. A full agonist engages both signaling mechanisms in contrast to the endogenous long-chain fatty Dehydroepiandrosterone receptor (LCFA) ligands and partial agonists. Thus, stimulation of GPR40 by endo
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ICH induced striatal lesion produced a reduction of
2022-05-16
ICH-induced striatal lesion produced a reduction of EAAT1 expression analogous to the decreased glutamate uptake at 6 h. The combined reduction of excitatory amino ligand gated ion channels transporters and of glutamate uptake activity might explain the well-known glutamate excitotoxicity following
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br Signals transmitted via MEGJ MEGJ facilitate the direct
2022-05-16
Signals transmitted via MEGJ MEGJ facilitate the direct transfer of ion currents or small molecules between EC and VSMC. Molecules passing through MEGJ are mainly second messengers such as Ca2+, IP3, and cAMP [31,32,] or endothelium-derived hyperpolarization (EDH) signals [34, 35, 36]. Moreover,
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Gap junction intercellular communication GJIC facilitates
2022-05-16
Gap junction intercellular communication (GJIC) facilitates the exchange of ions, metabolites, Ca2+, inositol phosphates, and/or cyclic nucleotides of up to 1.8 kD in size between neuraminidase inhibitor through contact-dependent mechanisms [3,4]. Oocyte growth and development (as depicted in Fig.
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In order to facilitate the preparation of aminothiazoles con
2022-05-16
In order to facilitate the preparation of 2-aminothiazoles containing novel D-ring substitutions, a convergent synthetic route was selected which requires the synthesis of common precursor . Straightforward aromatic substitution of 3,4-difluoroacetophenone using 4-methylimidazole provided access to
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The galactosidase from Aspergillus oryzae is
2022-05-16
The β-galactosidase from Aspergillus oryzae is a monomeric enzyme of 113 kDa [58] that has been widely used in GOS synthesis [49,53,[59], [60], [61]], exhibiting a high activity of lactose transgalactosylation [62]. Different immobilization methods have been used for the synthesis of lactose-derived
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RDL is of interest as it is the
2022-05-16
RDL is of interest as it is the target of highly effective insecticides (Buckingham et al., 2005, Raymond-Delpech et al., 2005). Point mutations, particularly an alanine to serine or glycine mutation in TM2, underlie resistance to several insecticides, including dieldrin, picrotoxinin and fipronil (
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Ning et al showed that LPC appeared
2022-05-16
Ning et al. showed that LPC 18:1 appeared to increase insulin release through both GPR119-dependent and -independent mechanisms (Ning et al., 2008). In our study, we have shown that not only GPR119 but also GPR40 and GPR55 participate in LPC-stimulated insulin secretion (Fig. 4, Fig. 5) and target p
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With the nitrogen containing heterocycle components and the
2022-05-16
With the nitrogen-containing heterocycle components and the acidic components in hand, the final products were synthesized according to the procedure as depicted in . Reaction of – with various β-substituted phenylpropionic CD 2665 (, and ), followed by deprotection by TFA, smoothly provided the cor
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br Fenton reaction based nanomaterials for
2022-05-16
Fenton reaction-based nanomaterials for ferroptosis In Fenton reaction, H2O2 is converted by Fe2+ or Fe3+ to highly oxidative ROS (Eqs. (1) and (2)), which is commonly used to catalyze the degradation of refractory organics [34]. Since the tumor microenvironment is characterized by low acidity an
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