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Under increased drug pressure more protease variants with mo
2021-11-08

Under increased drug pressure, more protease variants with more than one substitution will likely become clinically relevant. The accumulation of additional substitutions can allow RAS variants to emerge that alone are not viable, but in combination can rescue the viral fitness. We previously demons
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Our findings demonstrated that the expression level of
2021-11-08

Our findings demonstrated that the expression level of full-length α1 sGC protein was higher in the malignant and benign breast tumors than that of normal tissues. Similarly, an increase in the expression of α1 sGC subunit has been detected in glioma cell lines [34]. Higher expressions of sGCα1 and
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All experiments in this study were performed at pD
2021-11-08

All experiments in this study were performed at pD 6.1 for reasons described above. This leaves a question about the implications of stereochemistry in vivo. At physiological pH the GSTP1-1 catalyzed rate of EASG formation is only 1.1-fold higher than the non-enzymatic rate [26]. However, when human
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Screening of the compounds allowed for a
2021-11-08

Screening of the compounds allowed for a number of interesting SAR observations. First of all, pyridyl analogue demonstrated that a pyridine ring would be beneficial for both log as well as increasing the potency (entry 2 versus entry 1). Electron-poor aryl groups next to the oxadiazolone were detri
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Wasting syndrome is a common complication of HIV
2021-11-08

Wasting syndrome is a common complication of HIV infection and is marked by progressive weight loss and weakness, often associated with fever (Weinroth et al., 1995). Fever is a highly complex process initiated by the action on the nefiracetam synthesis thermosensitive cells of a number of endogeno
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br Materials and methods br Results br Discussion Ghrelin is
2021-11-08

Materials and methods Results Discussion Ghrelin is reported to regulate a number of processes related to cancer progression including tumor cell proliferation, apoptosis and metastasis [3,7,[15], [16], [17], [18], [19], [20], [21], [22]]. In the present study, we examined the potential eff
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FXR agonists represent an attractive class of drugs for pati
2021-11-08

FXR agonists represent an attractive class of drugs for patients with PFIC. Synthetic and semi-synthetic FXR agonists, with higher affinity and potency to activate FXR, have been successfully tested in animal models of cholestasis. In these murine models, the semi-synthetic steroidal FXR ligand obe
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The Ala to Leu substitution would
2021-11-08

The Ala116 to Leu110 substitution would reduce the size of the active-site cavity disfavoring the production of longer allylic compounds as a result of steric hindrance, according to the observations of Poulter and co-workers [29], [30]. However, this explanation appears to be unlikely since several
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The primary cancer lesion was mostly
2021-11-08

The primary cancer lesion was mostly in the uterus and adnexa, followed by the gastrointestinal tract, brain, blood, and kidney and HBTU synthesis (Fig. 2A). Histopathological findings indicated that most cancers were adenocarcinomas, followed by squamous cell carcinomas, glioblastomas, malignant ly
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Increasing trans epithelial transport efficiency is
2021-11-08

Increasing trans-epithelial transport efficiency is another area where different strategies are being developed for overcoming transcytosis. Enhancing the affinity for the basal membrane and weakening apical exocytosis through the optimisation of surface hydrophobicity have been demonstrated [79]. S
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Despite these data implicating Kdm
2021-11-08

Despite these data implicating Kdm6b as a positive regulator of neuronal differentiation, and surprisingly, given the evidence that germline knockouts die perinatally due to an inability to breathe, the brains of Kdm6b knockout mice are remarkably normal in gross morphology [26,]. Interestingly, Kdm
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More recently the JmjC domain histone H K di
2021-11-08

More recently, the JmjC domain histone H3K36 di-demethylase KDM2B/FBXL10 has also been shown to play an important role in definitive hematopoiesis [17]. Kdm2b is highly expressed in the HE, and its deletion (Tie2) caused embryonic lethality due to a precipitous drop in the number of hemogenic endoth
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As a possible back up to
2021-11-08

As a possible back-up to Sch 503034 (), we explored inhibitors that contained alternative electrophiles to ketoamides. Boronic acids have been extensively investigated as possible electrophiles that could react with nucleophilic serine in the context of developing inhibitors of thrombin receptor and
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br Conclusion br Disclosure of interest br Acknowledgement b
2021-11-08

Conclusion Disclosure of interest Acknowledgement Introduction Vitamin B6 has long been recognized as a cofactor for many enzymes, especially those involved in amino SKL2001 metabolism. Apart from its role as coenzyme, recent studies are unveiling a new role of vitamin B6 as a chemoprev
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Signaling pathways that control the redox
2021-11-06

Signaling pathways that control the redox stress response in P. brasiliensis are poorly known, but in other dimorphic fungi, the involvement of MAPK is an important factor in this process [[13], [14], [15]]. For example, when alveolar macrophages are challenged with Aspergillus or Cryptococcus conid
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