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Our co IP data show that
2023-11-16
Our co-IP data show that 5HT1A or 5HT2A receptors do not heterodimerize with mGluR1α receptors. Given that both 5-HT and mGlu receptors are GPCRs and produce anxiolytic effects, a degree of cooperativity via a functional cross-talk may still exist between these receptors [11]. In addition to the fun
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G-1 Finasteride has been shown to be
2023-11-15
Finasteride has been shown to be a mechanism-based inhibitor of 5AR-2 [9]. Finasteride acts as an alternate substrate for 5AR-2 and is initially bound in an extremely stable enzyme-bound NADP-dihydrofinasteride adduct which is ultimately processed to dihydrofinasteride. The NADP-dihydrofinasteride a
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Another significant group of reductase
2023-11-15
Another significant group of 5α-reductase inhibitors is the steroidal 3-carboxylic VX-702 derivatives (relevant examples in Fig. 5), which were designed to mimic the putative enzyme-bound enolate intermediate. This was achieved by introducing sp2-hybridized centers at C3 and C4 and an anionic carbo
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br The human CYP A gene is located on chromosome
2023-11-15
The human CYP17A1 gene is located on chromosome 10q24.3 (1) and spans 6.6 kb, which contain eight exons (2) and 1.6 kb of coding region. From this gene, the same 2.1-kb mRNA species is transcribed in both the adrenals and gonads (3), which yields a 57-kDa microsomal cytochrome P450c17 enzyme (CYP1
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Among the most important Ca regulatory mechanisms
2023-11-15
Among the most important Ca regulatory mechanisms are the Plasma Membrane Calcium ATPase (PMCA) and Sarcoplasmic Reticulum Calcium ATPase (SERCA). These pumps belong to the family of P-ATPases, which share the formation of an acid-stable phosphorylated intermediate as part of their reaction cycle. P
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Although TP status has been shown to
2023-11-15
Although TP53 status has been shown to play a role in ATR inhibition and platinum resistance [7], [27], [38], in inhibition of ATM and sensitivity to IR [39], and in the activation of Chk1 and Chk2 [3], [4], ATM and ATR signaling can occur through the p38MAPK/MK2 pathway in p53-deficient LY2801653 [
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Introduction the DNA damage response important implications
2023-11-15
Introduction: the DNA damage response — important implications for tumour development and treatment Cells are invariably challenged by tens of thousands of lesions inflicted on their DNA everyday (Lindhal, 1993). This DNA damage can be caused exogenously by exposure to different types of radiation
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Since at least prospective cohort studies have been
2023-11-15
Since 2005, at least 14 prospective cohort studies have been conducted to clarify inconsistencies in the field, ten of which suggested a direct correlation between antibiotic use and atopy or wheezing later in life [51–60], three found no association [61–63], and one found positive association only
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Since ARBs strongly reduce inflammation it was hypothesized
2023-11-15
Since ARBs strongly reduce inflammation, it was hypothesized that the protective effects on cognition were the result of reduction of inflammation and amelioration of neurogenic decrease. However, ARB treatment did not normalize increased inflammation and neurogenic loss. For this reason, the protec
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br Acknowledgement Work in the
2023-11-15
Acknowledgement Work in the McEwan Laboratory is funded by the Chief Scientist Office of Scottish Government: Grants ETM-258 and ETM-382. BE is supported by an Erasmus scholarship (D -JENA01). Introduction The equine placenta is a noninvasive transient organ, classified as diffuse and epithel
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Second the phosphorylation events e g Thr
2023-11-15
Second, the phosphorylation events (e.g., α-Thr172 and β-Ser108) needed for AMPK activation by small molecules binding at the ADaM or other sites remains unclear. Within the β-GBD, phosphorylation of β1-Ser108 was shown to be required for the activation by small molecules binding in the ADaM site, s
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br Introduction Nonalcoholic fatty liver disease
2023-11-15
Introduction Nonalcoholic fatty liver disease (NAFLD) is a clinicopathologic spectrum of liver pathologies associated with excessive accumulation of fat in the liver. This spectrum is continuous but can be graded based on pathological features; in increasing severity, these are: bland steatosis,
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Through an extensive SAR optimization campaign
2023-11-15
Through an extensive SAR optimization campaign with the 4-((2-hydroxy-3-methoxybenzyl)amino)-benzenesulfonamide-based scaffold researchers have developed ML355 ((N-benzo[d]thiazol-2-yl)-4((2-hydroxy-3 methoxybenzyl)amino)benzenesulfonamide) [5]. ML355 is a nonreductive, noncompetitive, reversible 12
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In the MT SGL two regularization parameters need to be
2023-11-15
In the MT-SGL, two regularization parameters need to be specified: λ1 and λ2. Using recent results on norm regularization (Banerjee et al., 2014), it is possible to express both parameters via a single parameter as follows: and (Meier et al., 2008, Banerjee et al., 2014), where and are computed as:
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In a working group exposed month
2023-11-15
In 2008, a working group exposed 12-month-old transgenic mice (mutation for human amyloid precursor protein expression) and their non-transgenic littermates to isoflurane and halothane for 120min per day for five days. It was concluded that in the transgenic mouse there was overload of amyloid prote
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