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Previous research has suggested that the acetylcholine
2021-08-24

Previous research has suggested that the acetylcholine-gated chloride channels (ACCs) in Caenorhabditis elegans (Putrenko et al., 2005) exhibit the characteristics of promising drug targets. The genes that encode the various subunits of this family are present across the nematode phylum and appear t
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Interestingly increased level of both circulating ET
2021-08-24

Interestingly, increased level of both circulating ET-1 and urinary excretion of ET-1 have been observed in patients treated with nephrotoxic immunosuppressive agents as cyclosporine A and tacrolimus (Slowinski et al., 2002). Other nephrotoxic agents, such as cisplatin, also increase urinary excreti
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br Materials and methods br Results br
2021-08-24

Materials and methods Results Discussion Our previous study showed that ERRγ negatively regulates osteoblast differentiation via inhibiting Runx2 transactivity (Jeong et al., 2009). In the present study, we found that ERRγ also induced miR-433 in osteogenic mesenchymal cell lineage C3H10T1/
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It is noteworthy that little is known as to
2021-08-24

It is noteworthy that little is known as to the role of autophagy in regulation of eNOS phosphorylation and eNOS uncoupling. eNOS monomers, but not eNOS dimers could be degraded by ubiquitination [39], harbingering the existence of protein degradation pathways in modulation of eNOS turnover and acti
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Although enantioselective accumulation of metalaxyl in organ
2021-08-24

Although enantioselective accumulation of metalaxyl in organisms is an integrated outcome of bio-process including absorption, transportation, and transformation, it is observed in our study that catalysis of CYP450 may lead to the enantioselective accumulation of metalaxyl. However, the mechanisms
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To assess whether the described cooperation between
2021-08-24

To assess whether the described cooperation between the EGFR and FGFR receptors was relevant at the clinical level, we determined the effect on progression-free survival of FGFR1 expression in patients with adenocarcinoma who were receiving erlotinib or gefitinib. As we had observed EGFR-FGFR1 coope
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Cancer patients may develop cachexia a deleterious wasting
2021-08-24

Cancer patients may develop cachexia, a deleterious wasting syndrome that is associated with muscle atrophy and has an impact on the well-being of patients and on the response to the treatment. Indeed, cachexia is a devastating and often irreversible syndrome observed in up to 80% of cancer patients
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As an endogenous negative modulator CRBN inhibits AMPK s
2021-08-24

As an endogenous negative modulator, CRBN inhibits AMPK’s activation (phosphorylation of Thr172) by directly binding to the α-subunit of AMPK, disrupting γ-subunit recruitment to the AMPK complex (Lee et al., 2011, Lee et al., 2013). In our study, we did not focus on AMPK activation, since only a si
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HOIP s ability to build linear Ub chains arises
2021-08-24

HOIP's ability to build linear Ub chains arises from a unique domain that follows directly after the RING2 domain, the linear ubiquitin chain-determining domain (LDD) (Fig. 1). Structures have revealed that the LDD is structurally integrated into RING2, creating a single RING2–LDD unit (Fig. 2D) [40
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aminoisobutyric acid BAIBA is a natural catabolite of the br
2021-08-24

β-aminoisobutyric LDN-212854 (BAIBA) is a natural catabolite of the branched-chain amino acid thymine. BAIBA was recently found to reduce inflammation in skeletal muscle via the AMP-activated protein kinase (AMPK)-peroxisome proliferator-activated receptor (PPAR)δ signaling pathway. BAIBA reportedl
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In anticipation of an approach based on modification of the
2021-08-23

In anticipation of an approach based on modification of the cyclohexylacetic droperidol subunit of 1 as a means of improving permeability, a set of analogs were prepared to map out the optimum display of the acidic functionality. Homologated acids 25 and 26 were found to be equipotent to 1, although
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In contrast DGAT does not interact with mitochondria and LDs
2021-08-23

In contrast, DGAT1 does not interact with mitochondria and LDs but can form dimers and tetramers [76]. It has been reported that the hydrophilic N-terminal region of DGAT1, which is not required for acyltransferase activity, has the roles in regulating enzyme activity and the formation of dimers and
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Our study demonstrates that the duration of
2021-08-23

Our study demonstrates that the duration of storage under the conditions analysed did not have a major effect on the recovery efficiency for any of the swabs (Fig. 1). However, up to 4-fold differences in the recovery efficiencies were observed between the different swabs tested (Fig. 2). Using the
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Based on the above we hypothesized that a PROTAC strategy
2021-08-23

Based on the above, we hypothesized that a PROTAC strategy would be effective to induce CK2 protein degradation. Herein reported is an approach for the preparation of novel PROTACs via “click reaction” for degradation of CK2 protein (Fig. 2). Importantly, “click reaction” is a very facile, selective
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Since the aggregation of neurotoxic forms
2021-08-23

Since the aggregation of neurotoxic forms of Aβ plays a pivotal role in AD pathogenesis, an approach that using small molecules to bind Aβ monomers and prevent their assembly into cytotoxic oligomers attracts great interest for the development of AD drugs. Therefore, the potential inhibitory activit
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