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Molecular docking simulations were carried out for ligands
2023-05-26
Molecular docking simulations were carried out for ligands – in the ACE crystal structure (1O86) and DPP4 crystal structure (2G5P). Comparison of the binding mode of – () with enalaprilat (a) in ACE shows that the phenethyl group (–, enalaprilat) occupies the S1 pocket and the adjacent carboxylic Re
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While the direct effects of ARI lead
2023-05-26
While the direct effects of 5-ARI lead to a dramatic caspase inhibitor in serum DHT levels, other laboratory values are also affected by 5-ARI use. Serum testosterone elevations are known to occur with both finasteride and dutasteride use, but values will typically remain within the normal laborator
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An AXL decoy receptor with enhanced GAS binding properties
2023-05-26
An AXL decoy receptor with enhanced GAS6-binding properties, MYD1, was engineered as a therapeutic tool to disrupt GAS6/AXL signaling in vivo (Kariolis et al., 2014). MYD1 was shown to block metastasis of human ovarian cancer 73122 and a murine breast cancer cell line in grafting assays in mice. The
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In this scenario the receptor tyrosine kinase inhibitors
2023-05-26
In this scenario, the receptor tyrosine kinase inhibitors (TKI), sunitinib, an anti-angiogenic agent, was tested in phase III trial, leading to a longer progressing free survival when compared to interferon (median: 11 vs. 5mo, respectively, hazard ratio (HR) = 0.42; 95% CI: 0.32–0.54; P5 alpha redu
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br Materials and methods br
2023-05-26
Materials and methods Results Dried gssg used were 48.46 g C. benghalensis, 857.98 g T. zebrina and 25.09 g T. fluminensis. The samples gave 12.9% C. benghalensis, 0.078% T. zebrina and 3.06% T. fluminensis methanol extracts. The methanol extracts were evaluated for their lipoxygenase inhibi
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Neuropathic animals display increased sensitivity
2023-05-26
Neuropathic animals display increased sensitivity to the anti-nociceptive effect of baclofen and whilst the number and affinity of GABAB Bioactive Compound Library in the dorsal horn are not altered (Smith et al., 1994; Zemoura et al., 2016), GABAB receptors subunits (B1 and B2) are both down-regul
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br Acknowledgements br Introduction Microbial enzymes have g
2023-05-25
Acknowledgements Introduction Microbial enzymes have gained interest for their widespread uses in industries and medicine owing to their stability, catalytic activity, and ease of production and optimization than plant and animal enzymes (Singh et al., 2016). Microbial aminopeptidases (amino-a
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Within the thrombus there is heterogeneity in
2023-05-25
Within the thrombus, there is heterogeneity in the activation of Thienoguanosine synthesis based on the concentration gradients of soluble agonists emanating from the site of vascular injury, which has been excellently reviewed by Tomaiuolo et al.[1]. As part of the coagulation cascade, active throm
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Several ceritinib resistant mutations following the second l
2023-05-25
Several ceritinib-resistant mutations following the second-line treatment of ALK+-NSCLC have been discovered [64]. These mutations include C1156Y, F1174L, and L1152R, which were first observed in crizotinib-resistant tumor samples. The G1202R ceritinib-resistant mutation occurs within the hinge and
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br Materials and methods br Results br Discussion
2023-05-25
Materials and methods Results Discussion Competing financial interests Acknowledgements The work was partially supported by grants from the National Natural Science Foundation of China (Grant no. 31530053 and 31401424) and National Science and Technology Support Plan (Grant no. 2013BA
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APPL is highly expressed in pancreatic
2023-05-25
APPL1 is highly expressed in pancreatic β cells, but its levels are significantly decreased in several mouse models of obesity and diabetes, including HFD-induced obese mice and db/db mice [6], [73], suggesting that the dysregulation of APPL1 may be associated with malfunction of the pancreas in obe
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br Conclusions and clinical relevance Astrogliosis and
2023-05-25
Conclusions and clinical relevance Astrogliosis and an increase in ADK is a pathologcial hallmark of epilepsy. The consequence of increased ADK in the epileptic GSK-LSD1 hydrochloride is a decrease in the ambient adenosine tone and A1R activity. As a result, systemic administration of A1R agonis
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ARM1 We have previously reported that interfering
2023-05-25
We have previously reported that interfering with ARM1 assembly dynamics by knocking down cofilin-1 in hMSCs increased polymerized actin that promoted osteoblast cell differentiation through a mechanism of enhancing focal adhesion kinase (FAK), p38 and c-Jun N-terminal kinase (JNK) signaling (Chen
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Compounds were profiled for their
2023-05-25
Compounds – were profiled for their inhibitory activity against dipeptidyl peptidase-IV Activity and/or Structure Homologues (DASH) [e.g. DPP2, DPP8 and DPP9] and non-DASH [eg. post-proline cleaving enzyme (PPCE), neutral endopeptidase (NEP), aminopeptidase P (APP), aminopeptidase N (APN)] enzymes.
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Introduction The lysosomal storage disorder Gaucher
2023-05-25
Introduction The lysosomal storage disorder Gaucher disease (Mendelian Inheritance in Man, OMIM #230800) results from the recessively inherited deficiency of lysosomal glucocerebrosidase (GCase, EC 3.2.1.45), caused by mutations in the gene GBA1 (MIM# 606463) located on chromosome 1q21. The enzymat
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