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In particular we focused our attention on beta adrenergic
2024-07-05
In particular, we focused our attention on beta2 adrenergic receptors, since their commercial inhibitors are effective in lowering IOP, the primary indication of glaucoma. The hypotensive action of a commercial sequence of beta2 adrenergic receptor siRNA was tested in rabbits. The results confirmed
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cyclic amp function To the best of our knowledge
2024-07-04
To the best of our knowledge, only 3 cases of an E196K mutation have been described since it was first identified in 2000 [15], [16], [17], although 5 cases, accounting for 1.1% of all genetic TSE cases, were reported with no precise data on the clinical phenotypes in the EUROCJD collaborative surve
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The incremental reduction albeit not statistically significa
2024-07-04
The incremental reduction, albeit not statistically significant, in collagen I with LCZ696 compared to perindopril treated animals, may therefore be related to a more compliant ventricle in LCZ696-treated animals. This is not so surprising given the incremental anti-fibrotic effect of the active met
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Similar to Cys Met can undergo ROS mediated oxidation
2024-07-04
Similar to Cys, Met can undergo ROS-mediated oxidation to Met sulfoxide, which can result in changes in protein conformation and activity [43]. In our results, the Met content in wild ginseng is higher compared to cultivated ginseng (1.3 times, Table 1). Met is a substrate for the synthesis of vario
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br Conclusions Triptans are HT B
2024-07-04
Conclusions Triptans are 5-HT1B/1D/(1F) receptors agonists and are considered as the gold standard for acute migraine treatment that have been proven effective. Unfortunately, they are contraindicated in patients with cardiovascular diseases due to their vasoconstrictor (side) effects (MaassenVan
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br Results br Discussion Today
2024-07-04
Results Discussion Today, enzymes play important roles in various fields. A good assay for enzyme activity is of great value, especially when it has good specificity, sensitivity, reproducibility and economy. ADK is the first identified enzyme in the metabolic pathway of adenosine salvage [15,
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Our initial approach to identify hits was two pronged
2024-07-04
Our initial approach to identify hits was two-pronged and included a high-throughput screening (HTS) campaign of the OSI YM 58483 library as well as a virtual screening (VS) campaign, utilizing a publically available crystal structure of ACK1 (PDB code: ). A tolerance for protein flexibility was in
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Finasteride has been shown to
2024-07-04
Finasteride has been shown to be a mechanism-based inhibitor of 5AR-2 [9]. Finasteride acts as an alternate substrate for 5AR-2 and is initially bound in an extremely stable enzyme-bound NADP-dihydrofinasteride adduct which is ultimately processed to dihydrofinasteride. The NADP-dihydrofinasteride a
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Matthew et al synthesized and carried
2024-07-03
Matthew et al. synthesized and carried out SAR studies of imidazo-[1,2-a]-pyrazine as Aurora kinase inhibitors with enhanced kinase selectivity and found that methylergometrine synthesis 39 showed optimal potency on Aurora-A and Aurora-B with IC50 value of 4 nM and 13 nM while on phosphorylation hi
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In addition to drawing attention to Ser
2024-07-03
In addition to drawing attention to Ser454 of ACL as a phosphosite that is regulated by both BDK and PPM1K, our phospho-proteomics screen identified several additional sites in other proteins. For example, Ser25, Ser29, and Ser79 of the lipogenic enzyme acetyl-coA carboxylase 1 (ACC1) were found to
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624 br Material and methods br
2024-07-03
Material and methods Results Discussion T2D is a substantial threat to global human health [31]. Obesity-associated chronic low-grade inflammation promotes insulin resistance and T2D [32]. In obese individuals, the production of numerous inflammatory molecules including IL-6 and TNF-a is up
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In a study highlighted the usefulness of arginase
2024-07-03
In 2010, a study highlighted the usefulness of arginase-1 as a sensitive and specific marker of hepatocytic differentiation for diagnostic pathology [9]. Subsequent studies have validated the high sensitivity and specificity of arginase-1, in particular its added value in evaluating poorly different
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Wound healing without blastema formation causes partial
2024-07-03
Wound healing without blastema formation causes partial restoration of lost tissue, and gives rise to fibrotic scars. Healing by fibrotic scarring rather than by regeneration leads to tissue dysfunction, and can place a huge burden for the health of the animal [4]. Therefore, understanding the molec
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br Material and methods br Results br Discussion Didox
2024-07-03
Material and methods Results Discussion Didox was originally created asa cytostatic drug to inhibit cancer cell proliferation by antagonizing RNR [11]. When used to target highly proliferative cells, Didox has extensive activity in vitro and in vivo. It has also been employed in clinical s
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In recent years the higher lipophilicity thus better perform
2024-07-03
In recent years, the ‘higher lipophilicity’-thus-‘better performance’ tenet, derived from the polar paradox theory applied to micro-structured media, was challenged by novel and unexpected experimental results. In particular, the synthesis of many complete series of fatty sr 75 esters of natural an
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