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Molecular docking quantitative structure activity relationsh
2024-12-19
Molecular docking, quantitative structure–activity relationship (QSAR) and high-throughput virtual screening (HTVS) studies have a very widespread use in computer-assisted drug design.25, 26, 27, 28 Suvannang et al. used the published X-ray crystallographic data to examine known aromatase inhibitors
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br Experimental procedures br Results br Discussion
2024-12-19
Experimental procedures Results Discussion Major depressive disorder is among the leading causes of disability worldwide (Vos et al., 2015). One of the major causal or exacerbating factors of depression is long term stress or psychological trauma (Liu and Alloy, 2010). Dysregulation of the
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Weak and transient interactions of HMGB proteins in such hit
2024-12-19
Weak and transient interactions of HMGB proteins in such hit-and-run mechanisms are understandable given that “fluorescence loss in photobleaching” (FLIP) experiments employing GFP-labeled HMGBs have shown that in living cells they are the most mobile of all nuclear proteins [144]. The entire pool o
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Echinocandin resistance is systematically associated
2024-12-19
Echinocandin resistance is systematically associated with point mutations in either FSK1 or FSK2 genes [7], [104]. These mutations are located in two different not spot regions of these genes named HS1 and HS2. Hot spot mutations have been reported in C. albicans, C. glabrata, C. tropicalis, C. krus
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We recently identified a G A dependent epigenetic mechanism
2024-12-18
We recently identified a G9A-dependent epigenetic mechanism for transcriptional activation of the serine pathway in cancer cells (Ding et al., 2013). G9A, also known as EHMT2 and KMT1C, is a H3K9 methyltransferase that has a primary role in catalyzing H3K9me1 and H3K9me2 in euchromatin (Shinkai and
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Accumulating evidence suggest that patients with advanced po
2024-12-18
Accumulating evidence suggest that patients with advanced -positive NSCLC are at increased risk of VTE or coagulation disorders during the course of their disease, indicating that cancer genotype might play a role in the occurrence of cancer-related thromboembolism . Here we report the case of a pat
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Numerous studies have shown that PUFA
2024-12-18
Numerous studies have shown that ω-3 PUFA incorporation into the lipid raft can affect the distribution and function of protein in the lipid raft by altering raft composition [25], [26], [27]. For example, DHA treatment excluded phospholipase D (PLD) from lipid raft toward non-lipid raft, resulting
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Despite these efforts to prevent oxidative metabolic
2024-12-18
Despite these efforts to prevent oxidative metabolic degradation, and showed only marginal improvements in metabolic stability and still exhibited high plasma clearances as shown in . High molecular weight as well as relative high log values could be contributing factors to the poor PK profiles of
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Although ACE genetic variance does not influence the level
2024-12-18
Although ACE genetic variance does not influence the level of bradykinin significantly, the bradykinin level tends to be affected by ACE inhibitor therapy used by patients. ACE inhibitor reduces the ACE activity that may lead to the accumulation of serum bradykinin. The level of bradykinin tends to
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NSAIDs induce gastrointestinal toxicity and evoke asthma by
2024-12-18
NSAIDs induce gastrointestinal toxicity and evoke chk1 inhibitor by decreasing the production of gastroprotective prostanoids and by redirecting the COX substrate AA into LT biosynthesis, thereby causing vasoconstriction in gastric mucosa and airways (Celotti and Laufer, 2001; Koeberle and Werz, 201
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As mentioned above variation of the A ring was
2024-12-18
As mentioned above, variation of the A-ring was undertaken in order to improve microsomal stability and kinase selectivity relative to Dioscin australia (). 1-Imidazole-2-carboxamides with substitution at the 4-position (–) were mostly tolerated with 4-cyano-imidazole-2-carboxamide () having compara
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Moreover our present work suggests that AXL could be a
2024-12-18
Moreover, our present work suggests that AXL could be a modulator of sunitinib response, at least for cell lines that present high endogenous levels of this RTK activation, since we observed an increased responsiveness to sunitinib in porcn sale activated with AXL receptor ligand. A role for AXL in
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Since innate immune responses represent the first defense
2024-12-18
Since innate immune responses represent the first defense against incoming infectious microorganisms, they are particularly engaged during the early stages of viral infections. Many innate defense mechanisms rely on the engagement of pattern recognition receptors (PRRs) which are conserved, germ lin
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br Conclusion In conclusion the arginase from P aeruginosa I
2024-12-18
Conclusion In conclusion, the arginase from P. aeruginosa IH2 was purified with electrophoretic homogeneity. Purified enzyme was homo-dimer and showed significant activity and catalytic stability near to the pH of circulating system and temperature of human body. The prolonged serum and proteolyt
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We report here the first study on the inhibitory effects
2024-12-17
We report here the first study on the inhibitory effects of the organic nitrates – on human erythrocyte GR. The previous reports by Becker et al., investigated other nitro derivatives (including arylizoalloxazines) by using Beutler’s method, monitoring GR inhibition. Data of show inhibition of hGR b
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