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We further evaluated the possibility whether
2024-04-19
We further evaluated the possibility whether letrozole mediates its effect through diverting the pathway towards 5α-DHT and further to 3α-Diol. For this purpose, we measured the concentrations of 5α-DHT and 3α-Diol in mice hippocampus and found that letrozole elevated both 5α-DHT and 3α-Diol levels
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Apelin is a peptide hormone and
2024-04-19
Apelin is a peptide hormone and an endogenous ligand for a G protein-coupled receptor named APJ [7], [8], and apelin and APJ are widely expressed in human organs including hypothalamus, heart, lungs, kidneys, adipose tissue, muscles, and others [9]. Apelin is initially synthesized as a 77-amino-acid
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br Acknowledgements br Introduction Diabetic complications a
2024-04-18
Acknowledgements Introduction Diabetic complications are responsible for increased morbidity and mortality of diabetic patients. Increased flow of faah inhibitor through the polyol pathway under conditions of hyperglycemia contributes to the development of diabetic complications. Aldose reduc
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The aldehyde reductase AKR A and aldose reductase AKR B
2024-04-18
The aldehyde reductase (AKR1A1) and aldose reductase (AKR1B1) belong to aldo-ketoreductase (AKR) superfamily catalyzing the reduction of corresponding aldehydes and ketones involved. Both the closely related enzymes AKR1A1 and AKR1B1 have 65% structural similarity and differ only at the active site.
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Gliomas and Aldehyde Dehydrogenase Aldehyde dehydrogenases A
2024-04-18
Gliomas and Aldehyde Dehydrogenase Aldehyde dehydrogenases (ALDHs) are key metabolic enzymes involved in regulation of glycolysis/gluconeogenesis pathways as well as in the detoxification of endogenous and exogenous aldehydes, regulating cell function and homeostasis. ALDHs play important roles in
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br Downstream signalling of AKT A consensus phosphorylation
2024-04-18
Downstream signalling of AKT A consensus phosphorylation motif has been described for AKT substrates: R-X-R-X-X-S/T-B where X represents any amino IOX4 and B represents bulky hydrophobic residues (Alessi, Caudwell, Andjelkovic, Hemmings, & Cohen, 1996). Numerous AKT substrates have been publishe
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ido1 inhibitor Introduction Adenosine monophosphate cAMP is
2024-04-18
Introduction Adenosine 3′,5′-monophosphate (cAMP) is a general-purpose signaling molecule present in most branches of life. Intracellular cAMP levels control diverse cellular functions. In bacteria, cAMP regulates metabolism by activation of the catabolite activator protein (CAP), also known as cAM
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pmsf In the past years the role of
2024-04-18
In the past 10 years, the role of the CD73-adenosinergic pathway in suppression of anti-tumor immunity has increasingly been recognized [13], [14]. In this review, we discuss the latest findings dealing with the regulation of anti-tumor immunity by CD73 and adenosine. We also discuss ongoing clinica
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Adenosine is a ubiquitous homeostatic purine nucleoside that
2024-04-18
Adenosine is a ubiquitous homeostatic purine nucleoside that accumulates extracellularly in response to metabolic stresses such as hypoxia and inflammation. Activation of either G protein-coupled adenosine receptors (ARs; A1R, A2AR, A2BR, and A3R) by extracellular adenosine can modulate cell signali
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The rapidity of this specific immunosuppressive therapy sugg
2024-04-18
The rapidity of this specific immunosuppressive therapy suggests that it inhibits or apoptoses plasma cells. Most serum autoantibodies to AChR are produced by long-lived plasma cells residing in spleen and bone marrow. These terminally differentiated cells are resistant to most non-specific immunosu
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During myeloid cell maturation expression of LO mRNA and
2024-04-18
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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The first rationally designed dual
2024-04-18
The first rationally designed dual mPGES-1/5-LO inhibitor was reported in 2008 and represents a structural derivative of pirinixic TMPyP4 tosylate - a synthetic agonist of PPARα with lipid-lowering properties (Koeberle et al., 2008b). Further α-alkyl- and α-aryl-substituted derivatives have been syn
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However although in vitro studies
2024-04-18
However, although in vitro studies in heterologous systems have provided very important indications of potential novel pharmacology, the studies with endogenous receptors in native tissues are essential to provide evidence for GPCR heteromerization in vivo and to confirm its physiological relevance.
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Acknowledgments br P c is expressed in several
2024-04-18
Acknowledgments P450c17 is expressed in several steroidogenic tissues, including the adrenal cortex, the ovary, and the testes (). Thus, 17α-hydroxylase/17,20-lyase is a key enzyme required for the production of both cortisol and sex steroids. This enzyme defect blocks the synthesis of cortisol,
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yohimbine hydrochloride The consensus amino acid recognition
2024-04-18
The consensus amino yohimbine hydrochloride recognition sequence for p38α substrates is (Ser/Thr)Pro (Cuadrado and Nebreda, 2010), typically assisted by upstream docking motifs (Remenyi et al, 2005, Sharrocks et al, 2000). P450c17 has 32 Ser and 25 Thr residues, of which only Thr 341 and Ser 427 ar
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