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To further investigate the possible interaction of L
2022-03-03
To further investigate the possible interaction of L1 with β1-sGC, a protein-ligand docking experiment was performed. Calculations were carried out with the program GOLD (version 5.2) [18], [34] and performed with the chemPLP scoring function [19], [34]. The ten lowest energy solutions presented a r
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Several studies have found that
2022-03-03
Several studies have found that GPR55 possesses a distinct pharmacology from that of CB1 and CB2, and that only certain cannabinoids act at this receptor. In transfected Azaperone expressing hGPR55, out of more than 20 synthetic and endogenous cannabinoids evaluated, only 2 compounds, SR141716A (Ri
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br TGR Agonists br FXR TGR Dual Agonists In
2022-03-03
TGR5 Agonists FXR/TGR5 Dual Agonists In 2010, a FXR/TGR5 dual agonist, 51 (INT-767), was reported [57]. Using an AlphaScreen coactivator recruitment assay, the potency of 51 at FXR was 30nM. In NCI-H716 cells, 51 stimulated intracellular cAMP secretion with an EC50 of 0.63μM. Its TGR5 potency
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Diabetes induced damage results in peripheral nerve patholog
2022-03-03
Diabetes-induced damage results in peripheral nerve pathology that ret inhibitor correlates with clinical signs and symptoms. Nerve injury that results in structural changes can be measured through clinical neurological assessment, quantitative sensory testing, nerve conduction studies, and periphe
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ER 50891 australia br The glyoxalase system has not yet been
2022-03-03
The glyoxalase system has not yet been studied in E. histolytica or G. lamblia. Searches in the G. lamblia genome (GiardiaDB.org) revealed two genes encoding hydroxyacylglutathione hydrolases (Morrison et al., 2007), but no glyoxalase I gene was found. The genome of E. histolytica does not have a
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Here we performed TEM and
2022-03-03
Here, we performed TEM and AFM imaging to study APE1–DNA interactions. The results showed that APE1 can dynamically polymerize on DNA in an apparently sequence-independent manner. We propose that this protein polymerization allows for scanning of the structural properties of DNA with short residence
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In vitro studies have shown that some antidepressant
2022-03-03
In vitro studies have shown that some antidepressant drugs bind to NMDA receptors and inhibit the binding of NMDA receptor ligands [18]. Similarly, several research teams have reported that tricyclic antidepressants can modulate the release and/or uptake of glutamate [19]. In this study, we found th
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br Declaration of interest br Acknowledgments This work was
2022-03-03
Declaration of interest Acknowledgments This work was financially supported by the National Natural Science Foundation of China (No. 31471615), the Introduction of Talent Research Start-up Fund of Anhui Polytechnic University (No. 2017YQQ017) and the Pre-research Project of National Natural Sc
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Three main transport systems are involved in
2022-03-02
Three main transport systems are involved in solute loss and red cell dehydration (summarised in Fig. 1: Lew and Bookchin, 2005): the deoxygenation-induced cation conductance (sometimes termed Psickle), the Ca-activated K+ channel (or Gardos channel) and the KCl cotransporter (KCC). Psickle is activ
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br Acknowledgement We like to thank
2022-03-02
Acknowledgement We like to thank the Austrian Federal Ministry of Science, Research and Economy for financial support (GZ402.000/00014-WF/V/6/2016 within the Sino-Austria project) as well as Andrea Szabo and Patricia Haiss for support regarding the drawing of figures and tables. Farnesoid X Re
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Recently Bristol Myers Squibb and Merck reported their GPR
2022-03-02
Recently, Bristol-Myers Squibb and Merck reported their GPR40 agonist research focused on the modification of α,β-position of phenylpropionic CP-809101 hydrochloride derivatives. For example, in recent published patent applications, Bristol-Myers Squibb claimed the pyrrolidine and dihydropyrazole GP
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Here we showed that microinjection of siRNA at the MII
2022-03-02
Here we showed that microinjection of siRNA at the MII stage efficiently reduced endogenous EZH2 mRNA and protein. Although the percentage of cleaving embryos was not affected, Reparixin L-lysine salt formation and blastocyst cell number were both reduced in EZH2 knockdown groups (Table 1). Similar
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br Introduction It is well
2022-03-02
Introduction It is well known that conventional cancer treatment strategies, such as surgery, radiotherapy, and chemotherapy all have their own limitations, which lead to an unsatisfactory therapeutic effect. Under this situation, the combination of two or more therapeutic strategies has recently
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This crosstalk may be responsible
2022-03-02
This crosstalk may be responsible for the beneficial effects of histamine H2 receptor inverse agonists on chloroquine phosphate pathologies and may also explain unwanted effects of these drugs on other tissues. In this way, Allen et al. reported an anaphylactoid reaction following cessation of high-
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br Structural Homology and Functional Implications Amino aci
2022-03-02
Structural Homology and Functional Implications Amino FTI 277 HCl sequence analyses of Disp and the Shh receptor Ptch indicate that both proteins share structural homology with a family of bacterial efflux pumps that function in resistance, nodulation, and division (RND) transporter complexes (Fi
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