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Functional implications notwithstanding the intermolecular c
2024-06-18
Functional implications notwithstanding, the intermolecular contact appears to shield the Y361 side chain (Fig. 3) from being accessible for regulation by phosphorylation/dephosphorylation as has been proposed [18,19]. It is, therefore, likely that Src kinase and PTP1B phosphatase bind to an AROM mo
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Fusaric Acid receptor br COPD As in asthma also in COPD incr
2024-06-18
COPD As in asthma, also in COPD, increased expression of arginase has been reported, and tobacco smoke may increase expression of arginase in human subjects [46, 47]. Increased ADMA levels have also been reported in COPD, and both the increased expression of arginase and ADMA contribute to remode
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gonadotropin releasing hormone receptor br Experimental EPR
2024-06-18
Experimental EPR spectra of probes 1a–f were recorded on a Bruker EMX-1572 operating at X-band (9.0–9.9 GHz), at 21 ± 1 °C. The EPR parameters were the same in all experiments: microwave power, 1 mW; modulation amplitude, 5 G; time constant, 10.24 ms; and conversion time, 40.96 ms. Reduced gluta
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br Discussion Herein we demonstrate that mice deficient
2024-06-18
Discussion Herein, we demonstrate that mice deficient in L-12/15 LO are more sensitive to 3-NP-induced toxicity although a substantial individual variability in striatal lesion size in response to 3-NP in both genotypes was observed. This variability is not atypical; several studies demonstrate s
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br Discussion Missense mutations transversions of the first
2024-06-18
Discussion Missense mutations (transversions) of the first nucleotide of the phenylalanine gw501516 at position 1174 (F1174) of the anaplastic lymphoma kinase gene can result in substitutions to leucine or valine (F1174L/V) while missense mutation (transversion) of the second nucleotide of the p
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br Aldehyde sensors to monitor substrate levels
2024-06-18
Aldehyde sensors to monitor substrate levels Previous efforts to ameliorate metabolic diseases frequently relied on biochemical methods which could measure the levels of toxic substrates in sodium fluoride or bodily fluids (blood and serum or plasma, urine, cerebrospinal fluid). Therapeutic eff
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67 8 br Materials and methods br
2024-06-18
Materials and methods Results Discussion Several major signaling and developmental pathways (e.g. EGFR, ALK, KRAS, TGFβ, Notch and Wnt/β-catenin) have been shown to be involved in lung carcinogenesis and they are being exploited as targets of the non-small cell lung cancer therapy (for revi
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Synthesis pharmacological evaluation for the binding at hA
2024-06-17
Synthesis, pharmacological evaluation for the binding at hA, hA and hA ARs, and efficacy at hA subtype of the synthesized compounds, together with the assessment of their theoretical ADME properties were the guidelines in this preliminary drug discovery investigation. The synthetic pathways which y
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The theoretical calculations of ADME parameters molecular we
2024-06-17
The theoretical calculations of ADME parameters (molecular weight (MW), log P, topological polar surface are (tPSA), number of hydrogen donors (nON) and acceptors (nOHNH), and volume) and DLS are presented in along with the violations of Lipinski’s rule. According to these data, all compounds (–) c
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It is already established in the
2024-06-17
It is already established in the literature that products synthesized by 5-LO, such as lipoxin A4, can activate PPARγ in a setting of experimental stroke [43]. Interestingly, experiments using 5-LO knockout mice in an endotoxemia model to mimic septic conditions, demonstrated reduced multiple organ
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In earlier experiments on snails a behavioral model
2024-06-17
In earlier experiments on snails, a behavioral model was employed of certain food rejection to study the mechanisms of the reconsolidation of long-term associative memory. It was found that conditioned food stimuli (reminder) presentation, combined with injections of NMDA glutamate receptor antagoni
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The gene SRD A encodes the
2024-06-17
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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Another significant group of reductase inhibitors is
2024-06-17
Another significant group of 5α-reductase inhibitors is the steroidal 3-carboxylic β-Tocotrienol australia 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
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An AXL decoy receptor with enhanced GAS binding properties M
2024-06-17
An AXL decoy receptor with enhanced GAS6-binding properties, MYD1, was engineered as a therapeutic tool to disrupt GAS6/AXL signaling in vivo (Kariolis et al., 2014). MYD1 was shown to block metastasis of human ovarian cancer interleukin 2 receptor and a murine breast cancer cell line in grafting a
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At present the role of autophagy in neurons remains controve
2024-06-17
At present, the role of autophagy in neurons remains controversial. Autophagy has homeostatic and waste-recycling functions and plays a protective role in neurodegeneration diseases. Moreover, it has been thought as a programmed cell death participating in the occurrence and development of various d
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