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Although the interactions of PhLP with G and
2024-10-26
Although the interactions of PhLP with Gβγ and its other partners have been convincingly documented through in vitro studies, it is not clear how PhLP controls monooxygenase signaling in vivo. C. elegans provides a powerful genetic model to analyze Phosducin function and study its interacting partn
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In summary present evidence suggests
2024-10-26
In summary, present evidence suggests that antimicrobial therapy for intra-abdominal sepsis can be shortened in patients exhibiting a clinical response to treatment. Hence, clinicians should use the resolution of clinical signs of infection as a guide to determine when during the 4–7-day window anti
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br Materials and methods br
2024-10-26
Materials and methods Results Discussion Our results revealed that LPS injection in rats impaired fear memory in the PA task. This results are in agreement with the most of previous studies reported that following acute [23,24,39,[45], [46], [47]] or chronic systemic dub inhibitor [30] fear
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br Conflict of interest statement br
2024-10-26
Conflict of interest statement Introduction Tanshinone IIA (Tan IIA) is a major active component of Salvia miltiorrhiza (S. miltiorrhiza), a well-known Chinese traditional medicine that is used for the treatment of cardiovascular and cerebrovascular diseases [1]. Tan IIA exhibits diverse pharm
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br Development of lorlatinib from
2024-10-26
Development of lorlatinib from crizotinib (1) to a clinical candidate (6) Xalkori (1, PF-02341066, crizotinib), was the first-in-class ALK inhibitor approved by the Unites States Food and Drug Administration (FDA) in 2011 as a first-line treatment for ALK+- NSCLC patients. This section describes
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The lactam emerged as lead candidate due to
2024-10-26
The lactam (6) emerged as lead candidate due to its high selectivity, outstanding potency (against ALK or in clinically known ALK mutants), low in vitro clearance, and low efflux potential. The lactam (6) was selected for further profiling against the resistant ALK mutants. Preclinical rat pharmacok
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Previous studies to investigate the functions of AHR in Treg
2024-10-26
Previous studies to investigate the functions of AHR in Treg phalloidin have employed a loss-of-function approach, using AHR complete-null mice, or a gain-of-function approach by ligand administration. However, these approaches may confound the interpretation of the results. For example, the broad e
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There is a growing literature on ABCA expression in
2024-10-26
There is a growing literature on ABCA2 expression in human biopsies, where it has been described as a potential biomarker of leukemias. In childhood T-cell acute lymphoblastic leukemia, ABCA2 and ABCA3 were expressed at high levels, which upon treatment with methotrexate, vinblastine and doxorubicin
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Among all the compounds the novel L derivative
2024-10-26
Among all the compounds, the novel L-748,337 derivative (23d) showed the potent human β3-AR antagonist activity and high lipolysis inhibitory activity in vitro. The L-Glutathione Reduced mg 23d displayed 23-fold more potent β3-AR antagonist activity (EC50 = 0.5117 nM) than that of L-748,337 (EC50 =
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However although in vitro studies in heterologous systems ha
2024-10-26
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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br Discussion Here we focused on seven
2024-10-26
Discussion Here, we focused on seven plant alkaloids extracted from yokukansan. These alkaloids individually inhibited 5-HT-mediated 5-HT3A and 5-HT3AB receptor currents weakly. Simultaneous administration of these alkaloids, however, inhibited the 5-HT3A and 5-HT3AB receptor currents strongly. T
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Fig A shows a schematic
2024-10-26
Fig. 2A shows a schematic representation of histological results according to the Franklin and Paxinos Mouse Brain Atlas (2001). The black circles represent the sites of drug infusion that were on-target within the amygdala. Gray circles represent the animals that had infusion locations outside the
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Osteoblasts have been thought to be the
2024-10-26
Osteoblasts have been thought to be the major cell type that expresses RANKL (Suda et al., 1999) which is a ligand for osteoprotegerin (OPG) and which functions as a key factor for osteoclast differentiation and activation. Recently, Nakashima and his colleagues (Nakashima et al., 2011) demonstrated
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LO is a soluble kDa enzyme
2024-10-26
5-LO is a soluble 78 kDa enzyme, composed of an α-helix-rich catalytic domain and a regulatory β-sheet-rich C2-like domain. Depending on the cell type, 5-LO may be located in the cytosol, in the nucleoplasm, or in both compartments (Werz, 2002). Upon cell stimulation by agents that elevate intracell
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Oocytes from the African clawed frog Xenopus
2024-10-25
Oocytes from the African clawed frog Xenopus laevis have been widely used as an expression system to study the modulation of NMDA receptors by metabotropic receptors, such as metabotropic glutamate receptors [12], μ opioid receptors [13], insulin receptors [14] and serotonin receptors [15]. No data
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