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rs G allele was previously associated with a
2023-03-16

rs523349 G allele was previously associated with a decrease in the conversion rate of testosterone to DHT (Beesley et al., 2007). This SRDA52 variant may have a trend towards higher testosterone availability, which according to the US Food and Drug Administration is described as a teratogen of categ
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Small kinase inhibitors have been developed to block AXL
2023-03-16

Small kinase inhibitors have been developed to block AXL by interacting with the kinase cytoplasmic ATP binding site. Up to date, no AXL selective kinase inhibitors are marketed. As depicted in , some marketed kinase inhibitors such as Bosutinib and Cabozantinib or kinase inhibitors in clinical pha
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Having taken a step back
2023-03-16

Having taken a step back from affinity to gain better exposure and solubility, we started work to replace the unstable oxazolinone, and address the selectivity over the hERG channel. Keeping in mind the binding mode of the series from crystal structures, triazole was identified as another mildly aci
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br ACL Inhibition Lowering Blood
2023-03-16

ACL Inhibition: Lowering Blood LDL-C to Reduce ASCVD Risk Given its strategic position in the lipid biosynthesis pathway, ACL has been considered an attractive target for lipid-lowering even before statins and their effects on cholesterol homeostasis were elucidated (Box 2). Cells carefully maint
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Tumor suppressor ARF regulates the activity of p
2023-03-16

Tumor suppressor ARF regulates the activity of p53 by inhibiting the functions of Mdm2. ARF is induced by hyperproliferative signals emanating from oncogenic Ras, overexpressed c-myc, and from deregulated E2F . ARF prevents p53 degradation and leads to increased p53 function by sequestering Mdm2 to
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br Conclusions and future direction ER PgR breast cancers
2023-03-16

Conclusions and future direction ER(−)/PgR(+) breast cancers have a distinct clinical course, response to treatment, and molecular features when compared to other breast cancer types, however some of them are actually technical artifacts or consequences of too high definitions of positivity. Acco
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br Regulatory mechanisms of ASK activity br The functions
2023-03-16

Regulatory mechanisms of ASK1 activity The functions of ASK1 in disease ASK1 inhibitor As mentioned above, ASK1 plays a pivotal role in the pathogenesis of various diseases; hence, an ASK1 inhibitor has therapeutic potential. Although inhibitors of the ASK1 downstream kinases p38 and JNK ar
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Placental cells also express P aromatase
2023-03-16

Placental cells also express P450 aromatase (CYP19A1, encoded by CYP19A1). In the placenta, this enzyme requires an external source of androgens, provided by the adrenal gland of the fetus, to form estrogen. The fetal adrenal gland produces dehydroepiandrosterone (DHEA) [9] and, in the placenta, it
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Natural Product Library ARG I is one of the most important
2023-03-16

ARG I is one of the most important mammalian enzymes responsible for nitrogen metabolism since it comprises the main route for the elimination of excess nitrogen resulting from amino Natural Product Library and nucleotide metabolism [18]. ARG I deficiency leads to hyperargininemia, characterized by
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br Concluding remarks It is clear that
2023-03-16

Concluding remarks It is clear that a disordered l-arginine homeostasis by changes in arginase, NOS and ADMA activity and expression, is not only vital in the chronic airway diseases, Medroxyprogesterone and COPD, but also seems to play an important role in many co-morbidities. Unknown, however,
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In addition to calpain I
2023-03-16

In addition to calpain I activity, cathepsin activities have been proven to be linked to apoptotic signaling. Cathepsin B and cathepsin D are two of the most abundant and well-investigated lysosome acid-dependent proteases that are involved in the apoptotic regulation (Ferri & Kroemer, 2001). Cathep
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Sixth significant progress has been made
2023-03-15

Sixth, significant progress has been made during the last few years regarding the molecular mechanisms underlying the activation of AMPK and this should aid to develop more potent and specific compounds. Information from crystallographic structures combined with computer-based drug design hold promi
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azidothymidine Neural activity resulting from sensory experi
2023-03-15

Neural activity resulting from sensory experience is required for the refinement and maturation of neural circuits during cortical critical periods. This refinement is thought to be important for functional optimization of primary sensory cortices, enabling critical functions such as feature detecti
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br Results The newly synthesized leucine ureido derivatives
2023-03-15

Results The newly synthesized leucine ureido derivatives were firstly evaluated for their enzymatic inhibition using porcine kidney APN (Microsomal, Biocol) with bestatin as the positive control (Table 1). One isoleucine ureido derivative 14 and phenylglycine ureido derivative 15 were also synthe
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br Materials and methods br Results br Discussion Intracellu
2023-03-15

Materials and methods Results Discussion Intracellular metabolic pathways of sugar, such as glycolysis and TCA cycle, provide material and energy for the synthesis of other substances, including amino acids. Thus, the content of sugars and their metabolic pathways are important for amino KC
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