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In an immunohistochemical analysis of gastric cancer samples
2022-07-01
In an immunohistochemical analysis of 117 gastric cancer samples, reduced Cx43 and E-cadherin expression were shown to contribute to the development of primary gastric cancer; however, increased Cx43 and E-cadherin expression contributed to lymph node metastasis [13]. In primary urothelial KNK437 c
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jak stat The effects of galanin on anxiety may
2022-06-30
The effects of galanin on anxiety may depend on the site of drug administration, on the galanin receptor subtypes activated and on the animal models of anxiety employed (Barrera et al., 2005, Holmes and Picciotto, 2006, Soares et al., 2016a, Soares et al., 2016b). For instance, administration of gal
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Neovascularization upon IMQ treatment was observed to differ
2022-06-30
Neovascularization upon IMQ treatment was observed to different degrees in WT and GAL3-KO mice, whereas the increase in vascular endothelial growth factor mRNA levels was genotype independent. Because we observed lower levels of the cytokines IL-17A, IL-22, IL-23, and TNF-α in IMQ-treated skin of GA
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One effective approach to fine tuning the lipophilicity prof
2022-06-30
One effective approach to fine-tuning the lipophilicity profile of FFA1 agonists is to ‘decorate’ the 3-phenylpropahoic Ecdysterone synthesis scaffold with polar heterocyclic moieties. Alternatively, this scaffold could be replaced with heterocyclic isosteres (as in Takeda’s compounds 1,2 and 3 as
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br Medium to long chain fatty acids
2022-06-30
Medium- to long-chain fatty acids Medium- to long-chain fatty acids impart a wide range of physiological effects. Medium-chain and long-chain fatty acids have 6–12 carbons and >12 carbons, respectively. As the energy source, these fatty acids are supplied primarily by food intake, biosynthesis, a
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amide pka receptor It has been reported that aberrant GPR ex
2022-06-30
It has been reported that aberrant GPR120 expressions were detected in colorectal carcinomas, compared with normal tissues. In addition, GPR120 stimulated cell motile activity and angiogenic property in colon cancer cells [10]. Recently, we indicated that GPR40 suppressed cell motile and invasive ac
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A great number of proteins entering the nucleus possess
2022-06-30
A great number of proteins entering the nucleus possess a characteristic nuclear localization sequence (NLS) in their primary structure. One of such sequences is the KKKGK motif [30]. It is present in all known muscle (but not liver – except human liver) FBPase sequences (human, rabbit, rat and mous
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Next we were interested in replacing the
2022-06-30
Next, we were interested in replacing the ketobenzimidazole fragment of our inhibitors with a noncarbonyl bearing heterocycle. We reasoned that if we could replace the carbonyl while maintaining comparable FAAH inhibition, it would provide evidence for a noncovalent mechanism of action. Thus, we eva
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Finally the optimized leads and were tested
2022-06-30
Finally, the optimized leads (−)- and (−)- were tested in rat model of CIPN (3 and 30 mg/kg, po, qd, administered for 7 days) and the results have been shown in . Under acute set up, after single oral administration at 30 mg/kg, both the compounds exerted significant improvement of the NP condition
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EZH interaction with HADC and HDAC through the EED subunit
2022-06-30
EZH2 interaction with HADC1 and HDAC2 through the EED subunit is known to recruit histone deacetylases [113,114]. Given that PRC2-mediated repression of transcription may be partly dependent on the function of HDACs in specific cell contexts [115], the leukemia cell treatment with hydroxamic (+)-Apo
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Acknowledgments The authors would like to thank members of t
2022-06-30
Acknowledgments The authors would like to thank members of the Department of Discovery Synthesis (DDS) and Biocon-Bristol Myers Squibb Research Center (BBRC) for scaling up key intermediates, analytical team for analytical experiments, lead profiling group for evaluating compounds in an in vitro AD
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In humans polymorphisms in the lengths of GT sequences from
2022-06-30
In humans, polymorphisms in the lengths of GT sequences (from 11 to 40) within the HMOX1 promoter impact the magnitude of HO-1 expression profiles. Long GT repeats code for less stable (Z-conformational) DNA with blunted transcriptional activity resulting in lower resting and stimulated HO-1 protein
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Apo E is defined as a polym http
2022-06-30
Apo E is defined as a polymorphic protein arising from three alleles. The human Apo E gene was widely studied and described to be located on chromosome 19, closely linked to the Apo C-I/C-II gene complex [9]. The three major alleles, termed Epsilon-2, Epsilon-3 and Epsilon-4 have been reported [10].
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br Methods br Results br Discussion Our results show
2022-06-29
Methods Results Discussion Our results show that the DRG and the spinal cord express significant amount of GPR35, a previously orphan Gi protein coupled receptor whose stimulation with zaprinast or with KYNA may reduce inflammatory pain. The receptor is also expressed in primary cultures of
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br The mode of binding of
2022-06-29
The mode of binding of ligands to GPR35 As noted above, although kynurenic CGP 35348 synthesis is an agonist at GPR35, this is true for neither kynurenine [8] nor kynurenic acid ethyl ester [13]. This implicates a key role for the carboxylate group in binding and/or activation of GPR35. Importan
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