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Species specificity of small molecular GPR agonists have bee
2022-10-11
Species specificity of small molecular GPR40 agonists have been reported by Takeda scientist. In the binding pocket of TM5, a Leu186 in human GPR40/FFA1 is replaced with Phe in rat, resulting in dramatic inter-species GPR40 activity discrepancy in certain scaffolds of small molecular GPR40 agonists.
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Introduction RNA splicing occurs in the nucleus
2022-10-11
Introduction RNA splicing occurs in the nucleus when noncoding sequences (introns) are removed from the pre-mRNA transcript and coding sequences (exons) are joined to form a mature mRNA [1,2]. This reaction is catalyzed by a multiprotein complex called spliceosome. The spliceosome consists of five
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br Conclusions In summary our results demonstrate that
2022-10-10
Conclusions In summary, our results demonstrate that in short term effect, TBT induced concentration-dependent vasorelaxation of HUA rings. Regarding the long term effects, exposure to a concentration of 100 μM TBT the human umbilical Dapivirine have a dual effect, and a decrease of the 5-HT2A e
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To promote biomimetic growth of HAp
2022-10-10
To promote biomimetic growth of HAp, Li et al. [20] developed a technique to modify cellulose nanofibers using P2O5. It was ascertained that the negative phosphate groups bonded with Ca2+ through coordination bonds and subsequently guided the growth of the Ca–P crystals throughout the scaffolds. Sim
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Intracellular signaling pathways leading to IR injury
2022-10-10
Intracellular signaling pathways leading to IR injury are initiated by an increase in reactive oxygen species (ROS). This occurs principally at the time of initiation of reperfusion, which is accompanied by the re-admission of oxygen to the ischemic tissue. The resulting cascade of downstream events
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In fact most PIs are
2022-10-10
In fact, most PIs are susceptible to substitutions at Asp168, which are often present in patients who fail therapy (Pawlotsky, 2016). Notably, the polymorphism Gln168 at this position underlies reduced efficacy of PIs against GT3 (Soumana et al., 2016a). Glecaprevir and voxilaprevir have improved re
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The LOD and linear range of
2022-10-10
The LOD and linear range of the cobas HBV test using the cobas 4800 system in this study were similar to those provided by the manufacturer. We found a strong correlation between the results of the cobas HBV test and CAP/CTM v2.0 systems; however, 7.7% of samples yielded detectable results only with
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In conclusion three heat stable
2022-10-10
In conclusion, three heat-stable cyclic peptides, guanylin, uroguanylin and renoguanylin are expressed in the intestine and kidney of the European eel, Anguilla anguilla. Their physiological functions are likely to be mediated, at least in part, by two isoforms of the guanylate cyclase type C recept
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br Materials and methods br Results br Discussion Directly m
2022-10-10
Materials and methods Results Discussion Directly modulating specific target proteins and signaling pathways with small-molecule drugs or agonistic 8-Azido-ATP synthesis is widely used for cancer metastasis therapies [[39], [40], [41]]. ANXA7 acts as a metastasis suppressor in prostate canc
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Type diabetes mellitus T DM causes
2022-10-10
Type 2 triptolide (T2DM) causes vascular complications and is a major public health problem associated with lifestyle diseases such as obesity, liver steatosis, hypertension, and so on. Although serum lactate is reportedly elevated in diabetic patients [12], [13], the physiological effects remain u
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br Acknowledgments We thank Dr Kathleen Sullivan
2022-10-10
Acknowledgments We thank Dr Kathleen Sullivan of Merck Research Laboratories for providing the CHO-K1 sildenafil mesylate 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
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For the study described herein analogues of CID were selecte
2022-10-10
For the study described herein, analogues of CID1792197 (2) were selected for exploration. There are a variety of reasons for this decision. First, the synthetic approach, described hereafter, is modular in nature to rapidly enable the independent modification of either end of the molecule. Second,
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br Evolution of multiple GnRH forms and GnRH
2022-10-10
Evolution of multiple GnRH forms and GnRH receptors across vertebrates GnRH is an evolutionary ancient peptide that first appears prior to the protostome-deuterostome split, and is a member of the GnRH-adipokinetic hormone-corazonin superfamily of peptides (Roch et al., 2011, Roch et al., 2014).
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ikk inhibitor The unique ability of R PabI to specifically e
2022-10-10
The unique ability of R.PabI to specifically excise ikk inhibitor from a palindromic sequence is based on a novel structural architecture that is distinct not only from other DNA glycosylases but also from other proteins [88]. In the absence of DNA, R.PabI forms a dimer with a central, highly twist
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Until recently the mechanism of how
2022-10-09
Until recently the mechanism of how GSMs shifted γ-secretase cleavage was poorly understood. Today, building on the sequential cleavage model developed by Ihara and colleagues [14], there is evidence that GSMs act as processivity enhancers, and iGSMs as inhibitors of processivity [120]. At least for
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