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Most human diseases e g cancer
2024-11-23

Most human diseases (e.g., cancer, diabetes, and neurodegenerative diseases) are complex and multifactorial. Several investigations in the literature focused on new multi-target drug development, which implies active pharmacophores incorporation in one scaffold (Meunier, 2008, Lazar et al., 2004, Te
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Recently AFF was used to convert an FN based
2024-11-23

Recently, AFF was used to convert an FN3-based binder specific to the Src homology 2 (SH2) domain of cAbl kinase into an allosterically regulated, intermolecular fluorescent switch (Figure 2D). Binding to cAbl kinase co-operatively stabilized the assembly of the FN3-based binder from two partial fra
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Using the same techniques we found that
2024-11-23

Using the same techniques, we found that UCP3 also has a half-life of between 1 and 4h [117]. In CAY10499 synthesis to UCP2 and UCP3, UCP1 and ANT had much longer half-lives and could not be degraded in the cell-free reconstituted system, suggesting their degradation is not mediated by the cytosoli
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EPSP analogs were retrieved from PubChem database
2024-11-23

EPSP analogs were retrieved from PubChem database and docking procedure yielded about eight best binding analogs (Fig. 10). The selected molecules were further assessed for their theoretical Ki values using AUTODOCK software version 4. The predicted binding efficiency of retrieved analogs was estima
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hinokitiol br Conclusions In sum enhanced
2024-11-23

Conclusions In sum, enhanced incentive motivation in obesity-prone rats is mediated by NAc CP-AMPARs. These neurobehavioral differences may render obesity-susceptible populations more sensitive to the motivational influence of food cues, producing more intense, focused, “wanting” that may limit t
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The present study determined the effect of
2024-11-22

The present study determined the effect of DCA on VSMC calcification in vitro and in atherosclerotic ApoE-/- mice in vivo. We found that Pyridostatin non-toxic concentrations of DCA, did not affect VSMC viability, induced calcification of VSMC in culture and increased atherosclerotic vascular calcif
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AhR is also known to cross talk with a variety
2024-11-22

AhR is also known to “cross-talk” with a variety of other cell signaling pathways, which has been the focus of a number of recent reviews [40], [41], [42]. It has long been known that TCDD is anti-estrogenic. For example, activation of AhR by TCDD and related HAHs inhibits estrogen dependent uterus
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br Methods br Results br
2024-11-22

Methods Results Discussion Chronic stress renders individuals vulnerable to diseases, and this effect might be, at least partially, mediated by stress hormone-induced immunosuppression. Therefore, investigating the effects of catecholamines on immune UNC1999 synthesis is of high relevance.
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However although in vitro studies in heterologous systems ha
2024-11-22

However, although in vitro studies in heterologous systems have provided very important indications of potential novel pharmacology, the studies with endogenous receptors in native tissues are essential to provide evidence for GPCR heteromerization in vivo and to confirm its physiological relevance.
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The reduced IFN production seen with
2024-11-22

The reduced IFNγ production seen with BPAL10-primed splenocytes could potentially be attributed to the impaired intracellular survival of B. pertussis, thereby leading to a weakened induction of cell-mediated immunity. Earlier studies have suggested an antimicrobial role of IFNγ in mediating the eli
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The gene SRD A encodes the
2024-11-22

The gene SRD5A2 encodes the 5-α-reductase enzyme, which converts testosterone into dihydrotestosterone. Although dihydrotestosterone levels are considerably lower than testosterone, dihydrotestosterone has a five-fold stronger binding capacity to the androgen receptor and, thereby, a considerably mo
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The diagnosis of ICP is currently based on the presence
2024-11-22

The diagnosis of ICP is currently based on the presence of pruritus, raised fasting serum TBS levels above 10μmol/L, and/or elevated serum transaminases (in the absence of diseases that cause cholestasis or pruritus) as well as spontaneous relief of signs and symptoms within four to six weeks after
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br Introduction Lipoxygenases LOXs are a heterogeneous famil
2024-11-22

Introduction Lipoxygenases (LOXs) are a heterogeneous family of enzymes that catalyze the peroxidation of polyunsaturated fatty acids (PUFAs). By oxidizing free PUFAs, they were shown to contribute to the generation of various bioactive lipid mediators. However, LOX-mediated oxidation of PUFAs es
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br Acknowledgements This work was supported by
2024-11-22

Acknowledgements This work was supported by the Victorian Government Operational Infrastructure Support Program. KAB is supported by the Mavis Robertson Fellowship from the National Breast Cancer Foundation (NBCF; ECF-16-004), by an NBCF Novel Concept Award (NC-14-011), and by NHMRC project grant
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br Introduction Arginase deficiency is a rare metabolic diso
2024-11-22

Introduction Arginase deficiency is a rare metabolic disorder resulting from a loss of arginase 1 (ARG1), the final enzyme in the urea cycle, which is the major pathway for the detoxification of ammonia in terrestrial mammals. ARG1 is expressed most prevalently in hepatocytes and red blood cells.
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