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Having established the structural requirements for potency
2023-03-16

Having established the structural requirements for potency in both the biochemical and biomarker (CRA) assays, we evaluated key compounds in the metabolic stability assay. Disappointingly, we found that all compounds had high intrinsic clearances in mouse microsomes. To ascertain whether the in vitr
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Fencilli et al reported derivatives of
2023-03-16

Fencilli et al. reported derivatives of PHA-680626 (15) which demonstrated strong anti-proliferative activity against large group of leukaemia cell lines including IM-resistant BAF3 cells expressing mutants like T315I, M351T and E255K. Decrease in Histone H3 phosphorylation led to induction of endo-
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br Introduction In addition to ATP
2023-03-16

Introduction In addition to ATP production, an important role of mitochondria in the pancreatic beta cell is anaplerosis, which is the net synthesis of citric Phosphatase Inhibitor Cocktail 2 (100X in ddH2O) cycle intermediates that are exported to the cytosol where they are converted to numerous
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br Dysregulated aromatase expression the link between obesit
2023-03-16

Dysregulated aromatase expression: the link between obesity and breast cancer Obesity has been associated with abnormally high expression of the enzyme aromatase in the breast, influencing the local production and bioavailability of estrogens (Morris et al, 2011, Subbaramaiah et al, 2012). Bowers
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br Identification of the croaker
2023-03-16

Identification of the croaker mAR cDNA Testosterone (T) was observed to alter steroidogenesis through a nongenomic mechanism (not blocked by the transcription inhibitor, actinomycin D) in Atlantic croaker ovarian tissues (Braun and Thomas, 2003). This action of T was mimicked by T conjugated to B
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While there is much in vivo work
2023-03-15

While there is much in vivo work on prion-like Aβ, it has not been shown that one can induce inclusions of Aβ in cultured cells as has been shown for tau and α-synuclein. One reason is practical; Aβ is a low molecular weight metabolite cleaved from within the larger amyloid precursor protein (APP) a
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br Materials and Methods br
2023-03-15

Materials and Methods Author Contributions Conflicts of Interest Acknowledgments We thank Francine Jodelka for technical assistance and Gopal Thinakaran for the CTM-1 antibody. This work was financially supported by RFUMS internal research funding and NIHS10 OD 010662. Introduction A
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br Parkinson s Disease and the immune system Parkinson
2023-03-15

Parkinson’s Disease and the immune system Parkinson’s Disease (PD) is the second most common neurodegenerative disorder, after Alzheimer’s, which affects 10 million people globally and is characterized by rigidity, bradykinesia, tremors, and gait instability (O’sullivan et al., 2007). The patholo
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In summary the role of HT and differe http www
2023-03-15

In summary, the role of 5-HT and different types of 5-HTRs in gating plasticity induction in neocortical circuits remains unclear, with variable and seemingly contradictory effects reported for LTP induction in cortical sensory fields (e.g., V1, enhanced LTP: Inaba et al., 2009, Kojic et al., 1997,
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Phagosomes acquire some hydrolases early during
2023-03-13

Phagosomes acquire some hydrolases early during their journey from the cell surface to lysosomes. An example for such hydrolase is cathepsin H which is most concentrated in the early phagosome at a pH of approximately 6.3 (Claus et al., 1998), the pH optimum of enzyme activity (Schwartz and Barrett,
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FH535 australia Pathological angiogenesis occurs when an imb
2023-03-11

Pathological angiogenesis occurs when an imbalance of endogenous proangiogenic and antiangiogenic factors occurs. Although the focus of angiogenesis-related drug development has been geared to the discovery of antiangiogenic compounds for use in pathologies where excessive angiogenesis occurs (cance
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Finally intracrine androgen synthesis metabolism can be acti
2023-03-11

Finally, intracrine androgen synthesis/metabolism can be activated thus allowing ACP-196 to bypass the low levels of androgens in the circulation by producing androgens themselves (Cai and Balk, 2011, Rahman et al., 2004). Moreover, changes in AR co-regulators like the overexpression of steroid rece
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Treatment of RAW cells with
2023-03-11

Treatment of RAW264.7 JNJ26481585 with AP(+)-exosomes caused an increase in their phagocytic activity. In the presence of amastatin, phagocytic activity was not completely suppressed, suggesting that at least two components were responsible for the activity; one of which is aminopeptidase(s). When
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br The lipoxygenase pathway and microvascular complications
2023-03-11

The 12/15-lipoxygenase pathway and microvascular complications of diabetes The 12/15-lipoxygenase pathway in adipose tissue Only recently has adipose tissue been recognized as a highly metabolically active endocrine organ imparting profound local and systemic inflammatory effects. Adipose tiss
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Although several studies indicate that ALDH protects the
2023-03-11

Although several studies indicate that ALDH2 protects the heart from injury and maladaptive remodeling (reviewed in [11], [12], [13]), accumulating evidence indicates that deficiency of the enzyme could be protective as well. For example, mice expressing the defective Aldh2*2 mutation show lower ald
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