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Various compounds have been designed to inhibit aldose reduc
2023-10-18
Various compounds have been designed to inhibit aldose reductase (AR) [12]. These compounds can be classified into two main categories, the first category comprises those containing a carboxylic SM-164 moiety, for example, 3-thiazolidineacetic acid derivative, which has been reported to be a potent
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The AhR molecule is composed of multiple functional
2023-10-18
The AhR molecule is composed of multiple functional domains [38]. In the N-terminal end, the AhR contains bHLH domain which is involved in DNA binding, dimerization with ARNT and association with chaperone proteins. The PAS domain, which is situated next to the bHLH domain consists of two structural
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Adiponectin is an adipokine whose circulating
2023-10-18
Adiponectin is an adipokine whose circulating level is depleted in a number of metabolic diseases including insulin resistance, diabetes and cancer (Khan et al., 2015, Singh et al., 2014a, Singh et al., 2014b, Yamauchi et al., 2014). Despite its importance in health and pathophysiology, adiponectin
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During myeloid cell maturation expression of LO mRNA and
2023-10-18
During myeloid cell maturation, expression of 5-LO mRNA and protein is strongly induced (60–130-fold) by calcitriol (1,25(OH)2D3) and transforming growth factor-β (TGFβ) [6,7]. The upregulation of 5-LO mRNA transcription is mainly due to transcript elongation and mRNA maturation [8,9]. Interestingly
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Notably our preliminary results confirmed that
2023-10-18
Notably, our preliminary results confirmed that fluoxetine (SSRIs, 5–10 mg/kg) and duloxetine (SNRIs, 5–10 mg/kg) could not enhance memory function in the novel object recognition or step-down passive avoidance tasks (data not shown). In the present study, we also found that vilazodone showed had no
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Jesus et al discovered a new series of azaindole as
2023-10-18
Jesus et al. discovered a new series of azaindole as Aurora inhibitors through various modification of GSK1070916 (47). They synthesized series from modification of the GSK1070916 and evaluated for in-vitro Aurora-B/INCENP and Aurora-A/TPX2 inhibition assays. Modified FK-228 australia 48 and 49 show
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Crystal structures were obtained of sulfonamide and amide as
2023-10-18
Crystal structures were obtained of sulfonamide 18 and amide 19 as a derivative of amide 36 (Fig. 7A and B). The precise rotameric orientation of amide 36 was of significant interest to understand the compound's interaction with the protein. As it would be difficult to assign the rotomer of 36, the
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Several structural classes of ASK inhibitors mostly from
2023-10-18
Several structural BIBW2992 of ASK1 inhibitors, mostly from industry but also from academia, have been identified over the last decade. In 2012, Terao et al. (Takeda) reported imidazo[1,2-α]pyridine () as a potent ASK1 inhibitor derived from structure-based drug design. GSK, Merck and Gilead revea
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It is well known that neurosteroids such
2023-10-18
It is well-known that neurosteroids such as testosterone and their metabolites endogenously modulate neural excitability in animals and humans. Testosterone has protective effects against seizures induced by KA and PTZ (Frye et al., 2001b; Reddy, 2004b). Estrogens, on the other hand, have proconvuls
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Using the same techniques we found that
2023-10-17
Using the same techniques, we found that UCP3 also has a half-life of between 1 and 4h [117]. In prescription 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 cytosolic prot
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br Acknowledgments br Introduction Alzheimer s disease AD is
2023-10-17
Acknowledgments Introduction Alzheimer's disease (AD) is a severe neurodegenerative disorder primarily affecting the elderly population. Senile plaques in the brain, one of the pathological hallmarks of AD, are formed by the accumulation of aggregated β-amyloid (Aβ) with an extensive β-sheet s
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br Special report Financial and personal benefits of early
2023-10-17
Special report – Financial and personal benefits of early diagnosis Acknowledgments The Alzheimer’s Association acknowledges the contributions of Joseph Gaugler, Ph.D., Bryan James, Ph.D., Tricia Johnson, Ph.D., Allison Marin, Ph.D., and Jennifer Weuve, M.P.H., Sc.D., in the preparation of 201
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br Actin cytoskeleton in protrusion Pushing force driving me
2023-10-17
Actin cytoskeleton in protrusion Pushing force driving membrane protrusion is generated by polymerizing kras-pdeδ inhibitor filaments organized either into branched networks or parallel bundles. Branched networks are assembled through Arp2/3 complex-dependent actin nucleation and drive protrusio
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br Co http www apexbt com media diy images wb
2023-10-17
Conclusions This paper is the first meta-analysis about the association between SRD5A2 V89L polymorphism and hypospadias risk. The results of this meta-analysis have revealed that V89L polymorphism definitely increases the risk of hypospadias, and the C allele is a genetic risk factor for hypospa
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Taken together our results indicated that LOX can be induced
2023-10-17
Taken together, our results indicated that 5-LOX can be induced in mice by MPTP injection, and the 5-LOX inhibitor MK-886 reduced the death of dopaminergic neurons. MK-886 also reduced the LTB4 ret pathway induced by MPTP. The development of the novel 5-LOX or FLAP inhibitors may provide a new ther
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