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br AhR Modulators It is now well recognized
2023-10-18
AhR Modulators It is now well recognized that ligand-activated AhR induces an immune tolerance response by acting directly on the antigen-presenting DCs and indirectly by increasing the population of immunosuppressive Tregs 24, 95, 96. In addition to inhibiting the formation or depleting the AhR
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It is also possible that adrenoceptor activation may
2023-10-18
It is also possible that α2-adrenoceptor activation may inhibit glutamate accumulation by upregulating the glutamate-buffering activity of Müller fasudil through EAAT1 or adjusting EAAT2 in bipolar cells, as well as the NMDA receptor. Therefore, we investigated whether topical administration of bri
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br Experimental procedures br Results
2023-10-18
Experimental procedures Results Discussion Acknowledgments Introduction β-Adrenergic receptors (β-ARs) belong to the superfamily of membrane proteins termed G protein-coupled receptors. β-ARs are distributed in the effector VRT752271 of most of the sympathetic nerve fibers, and the r
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In the vasculature it is known that A A
2023-10-18
In the vasculature, it is known that A2A and A2B adenosine receptors are stimulatory for adenylyl-cyclase, leading to cyclic-AMP (cAMP) production and vasodilation, while the A1 and A3 adenosine receptors are linked to the inhibitory Gi, suppressing adenylyl-cyclase and favoring contraction. However
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br Concluding remarks ROP is a major cause
2023-10-18
Concluding remarks ROP is a major cause of childhood blindness in the world. Current pharmacological therapy focus on anti-VEGF strategy, but this strategy is associated with the unintended effects on delayed eye growth and retinal vasculature development of preterm infants. Preclinical studies u
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In this paper we describe the formation of a
2023-10-18
In this paper, we describe the formation of a structure-based pharmacophore which lead to the discovery of several hydrophobic, yet non-lipid inhibitors of ATX. These compounds docked within the same volume occupied by the initial non-lipid inhibitors of ATX used to build the pharmacophore. Violatio
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br Results br Discussion Autophagy is considered
2023-10-18
Results Discussion Autophagy is considered as an important process in physiological and pathological ovarian function. It is related mainly to follicular atresia and CL regression (for review see [20]). However, an involvement in luteal cell survival is also proposed [21], [22]. The present st
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The resolution cocrystal structure of ACL in complex with
2023-10-18
The 2.10Å resolution cocrystal structure of ACL in complex with citrate indicates that the carboxyl (COH) groups of citrate forms a network of H-bonds with hydrophilic residues surrounding the ACL citrate binding domain (CBD) (A). The - carboxyl group forms a salt bridge with the guanidine moiety of
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These recommendations may be useful for the future
2023-10-18
These recommendations may be useful for the future to avoid misleading reports and pairings. However, the existing literature can also hold back current research on some given orphans. Before entering into drug development or further physiological conceptual framework, these pairings should be thoro
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Thus phosphorylation of p was used to measure the
2023-10-18
Thus, phosphorylation of p38 was used to measure the intracellular potency of ASK1 inhibitors. In this assay, HEK293/AP-1luc cyclohexamide expressing human full-length ASK1 were incubated with compound for 18 h and then lysed and the level of phospho-p38 was quantified using the HTRF assay [33].
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Because ASK signaling in microglia and astrocytes is importa
2023-10-18
Because ASK1 signaling in microglia and astrocytes is important during EAE, we hypothesized that a combination therapy that targets T cells along with microglia and astrocytes would further ameliorate the severity of EAE. We tested this hypothesis by applying valproic Deferiprone (VPA)—a short-chain
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br Aromatase inhibitors The aromatase enzyme P
2023-10-18
Aromatase inhibitors The aromatase enzyme, P450arom, belongs to the super-family of P450 proteins which includes more than 480 members divided in 74 different families. P450arom is a unique member of family 19 [39], and is located in the endoplasmic reticulum of mammalian Sunitinib Malate austral
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Apelin is involved in various physiological functions includ
2023-10-18
Apelin is involved in various physiological functions, including sapanisertib contraction (Ashley et al., 2005), vasodilatation (Jia et al., 2007), feeding control (Valle et al., 2008), and metabolic homeostasis (Higuchi et al., 2007, Dray et al., 2008, Attane et al., 2010). Its plasma level is elev
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Thiazole heterocycles constitute an interesting
2023-10-17
Thiazole heterocycles constitute an interesting class of molecules, which exhibit a broad spectrum of biological activity, including antifungal properties [[16], [17], [18], [19]]. Encouraged by our previous study that describes the activity of hydrazine-thiazole derivatives against C. gattii and C.
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What are the in situ effects
2023-10-17
What are the in-situ effects of multi-site CaM associations with AT1R? Kai et al. showed that synthetic peptides corresponding to residues 125–137 (rat sequence) in SMD2, 217–227 in the N-terminal side of SMD3, and 304–316 in SMD4JM inhibit to various degrees AngII-induced GTPase activity of isolate
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