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The introduction of a pyrazole moiety into any
2025-02-28

The introduction of a pyrazole moiety into any position of the sterane core by cross-coupling reactions [13] or by Knorr construction from a CCC bis-electrophilic sterane precursor and an N,N binucleophile building block [17], [19] may serve as an example. Very few reports are to be found, however,
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Another significant group of reductase inhibitors
2025-02-28

Another significant group of 5α-reductase inhibitors is the steroidal 3-carboxylic cdk7 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 carboxy
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An AXL decoy receptor with enhanced GAS binding properties
2025-02-28

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 KH CB19 and a murine breast cancer cell line in grafting assays in mice. T
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Among the most important Ca regulatory mechanisms are the
2025-02-28

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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The transcription factor activator protein
2025-02-28

The transcription factor activator protein-1 (AP-1) is a redox-sensitive transcription factor whose activity is controlled by agents that perturb intracellular thiol concentrations [10,11]. AP-1 is mainly composed of Jun, Fos, and ATF protein dimers [12,13]. AP-1 mediates the regulation of numerous
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Intriguingly androgens may also have an indirect
2025-02-28

Intriguingly androgens may also have an indirect effect on AR gene expression through inhibition of the GATA2 transcription factor gene (He et al., 2014) (Table 1). Using ChIP-seq, GATA2 was found to bind to a regulatory element 5.5 kb upstream of the TSS of the AR gene and enhanced transcription, w
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The molecular mechanisms that mediate the plasticity of the
2025-02-28

The molecular mechanisms that mediate the plasticity of the NMJ are not well understood. PGC-1α is a master regulator of the NMJ gene expression program 23, 24, and thus AMPK might indirectly regulate the NMJ via its broad influence on the coactivator. Cerveró et al.[6] recently provided more direct
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Taken together the results reveal a complex feedback and fee
2025-02-28

Taken together, the results reveal a complex feedback and feedforward signaling network between the tryptophan metabolic enzymes IDO1/TDO2, the KP metabolite KYN, and the ligand-activated transcription factor AhR (Figure 2). Cancer Amyloid Beta-peptide (25-35) highjack this signaling circuitry to de
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In summary the different types of
2025-02-28

In summary, the different types of interstitial cells found in the current study are illustrated in Fig. 7A (see legend for further details), which is suggestive of a heterogeneous complex network of interstitial cells communicating with each other. The possible signaling pathways involving this int
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The synthetic adipoR agonists AdipoRon and
2025-02-27

The synthetic adipoR agonists, AdipoRon (1) and 112254 (2), are both detectable in human plasma [18]. However, with increasing knowledge about their metabolism [19], a method for detection from human urine is conceivable and would be preferred given the easier accessibility and greater frequency of
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br Functional consequences of ADK regulation on neuronal
2025-02-27

Functional consequences of ADK regulation on neuronal excitability Adenosine modulates neuronal excitability via activation of the high affinity A1 or A2A, low-affinity A2B, or low abundance A3 adenosine receptors that feed into a multitude of different neuronal and astrocytic pathways (Blum et a
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A more versatile cellular delivery system for adenosine was
2025-02-27

A more versatile cellular delivery system for adenosine was generated by engineering mouse embryonic stem cells to lack both estrogen related receptor of Adk (Fedele et al., 2004). Using a step-wise differentiation protocol (Okabe et al., 1996) Adk−/− ES cells were differentiated into transplantabl
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Moreover our results indicate that ADP
2025-02-27

Moreover, our results indicate that ADP is by far a better phosphate donor than AMP (Table 2). Yet, the bindings of AMP and ATP are mutually exclusive, whereas the bindings of ADP and ATP are additive (Fig. 7). The multiplicity of the phosphate donors in the TgAK reaction (Tables 1 & 2), suggests th
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This study was funded and supported by Tehran
2025-02-27

This study was funded and supported by Tehran University of Medical Sciences and Health Services; and Iran National Science Foundation. Introduction The enzyme acetylcholinesterase (AChE) plays a central role in the signal transduction in the nervous system, hydrolyzing the neurotransmitter acet
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In conclusions MPE effects in causing lesser increase in
2025-02-27

In conclusions, MPE effects in causing lesser increase in vaginal fluid pH could partly restore the vaginal acidity in sex-steroid deficient state. MPE could exert its effect via enhancing both H+ generation as well as H+extrusion into the vaginal lumen. Although gallic PF2341066 is the main consti
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