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Although encoded by a single gene GR displays considerable h
2022-09-16
Although encoded by a single gene, GR displays considerable heterogeneity through the combined effects of alternative mRNA splicing, alternative translation initiation, and complex post-translational modification. Differential expression of the various GR isoforms may contribute to tissue-specific f
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C steroids and their glycosylation products distribute widel
2022-09-16
C21 steroids and their glycosylation products distribute widely in Asclepiadaceae plants. Their anticancer activities have been shown in different human cell lines and in vivo animal experiments [[27], [28], [29], [30], [31], [32]]. However, the mechanisms of their anticancer activities are still un
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mth1 pathway One effective approach to fine tuning the lipop
2022-09-15
One effective approach to fine-tuning the lipophilicity profile of FFA1 agonists is to ‘decorate’ the 3-phenylpropahoic mth1 pathway scaffold with polar heterocyclic moieties. Alternatively, this scaffold could be replaced with heterocyclic isosteres (as in Takeda’s compounds 1,2 and 3 as well as A
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The G protein coupled receptor GPR also called FFAR
2022-09-15
The G protein-coupled receptor, GPR40 (also called FFAR1) responds to medium and long chain unsaturated fatty acids, resulting in increase of insulin secretion during elevated glucose levels. The glucose dependency of insulin secretion makes this receptor a very good target for developing therapies
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br The potential of EPA Ffar signaling as a
2022-09-15
The potential of EPA-Ffar4 signaling as a novel intervention for HFpEF Conclusions and future directions Optimization of ω3-PUFA/EPA-therapy based upon titration to achieve therapeutic levels: A pressing clinical challenge is to continue to define the benefit of ω3-PUFA/EPA-therapy. Recent ana
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growth hormone secretagogue receptor As a part of our
2022-09-15
As a part of our continuing efforts towards discovery of new class of compounds against different therapeutic areas and based on the literature reports, we designed a dual pharmacophore which possess a long aliphatic chain of free fatty acids and a phenyl propanoid part of known GPR40 agonists. Here
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It was then found that
2022-09-15
It was then found that TAZ, a YAP holomog, binds heteromeric SMAD2/3–4 complexes in a TGF-ß-dependent fashion, and is recruited to TGFβ response elements (Varelas et al., 2008). Knockdown experiments identified TAZ as critical for nuclear accumulation of SMAD2/3/4 complexes in response to TGF-ß, and
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Nitrotetrazolium Blue chloride br Conclusion br Conflict of
2022-09-15
Conclusion Conflict of interest Introduction The human epithelial receptor 2 (HER2 or erbb2) is a member of the epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases that act through the EGF signaling cascade [1,2]. Approximately 20% of breast cancers overexpress HER2
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br Disp Cleavage and Membrane Trafficking Knowledge
2022-09-14
Disp Cleavage and Membrane Trafficking Knowledge of how Disp is regulated in Shh-producing LDC000067 to control ligand deployment has, until recently, remained limited. Early studies examining Disp function in Madin–Darby Canine Kidney (MDCK) cells and Drosophila tissue suggested that it is likel
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br Disp Cleavage and Membrane Trafficking Knowledge
2022-09-14
Disp Cleavage and Membrane Trafficking Knowledge of how Disp is regulated in Shh-producing LDC000067 to control ligand deployment has, until recently, remained limited. Early studies examining Disp function in Madin–Darby Canine Kidney (MDCK) cells and Drosophila tissue suggested that it is likel
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The following are the supplementary
2022-09-14
The following are the supplementary data related to this article. Introduction Target therapies have achieved significant gains in the fight against cancer, however, they are still a long way from providing generally curative treatments for the majority of cancers. Targeted agents can be used wi
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a23187 The beta catenin TCF complex is an important target
2022-09-09
The beta-catenin/TCF complex is an important target in the Wnt/beta-catenin pathway. This complex has proven challenging to target. However, natural inhibitors of this complex have been identified. One group of inhibitors is called the inhibitors of Wnt response (IWR-1/2). IWR-1/2 targets Axin and s
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In three groups independently proposed two different mechani
2022-09-09
In 2001, three groups independently proposed two different mechanisms for the catalytic reaction of GlxI [5], [6], [7]. Richter and Krauss (RK) used HF/4–31G calculations of the active site, coupled with a frozen effective fragment potential description [8], [9] of eleven residues in the binding sit
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In conclusion we have designed and characterized
2022-09-09
In conclusion, we have designed and characterized a novel series of EAAT-blockers, exemplified by (-[4-(2-bromo-4,5-difluorophenoxy)phenyl]--asparagine)—a potent, selective, competitive non-substrate inhibitor of EAAT-2. As one of the most potent and selective EAAT-2 inhibitors identified to date,
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The EEGs of these six patients interestingly
2022-09-09
The EEGs of these six patients interestingly showed focal, multi-focal and generalized spikes, which was an exclusion criteria in our study as we selected our cohort to exclusively represent focal epilepsy. Remarkably all of these cases were diagnosed with paroxysmal exercise-induced dyskinesia (PED
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