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br Conclusions br Declarations br Introduction The classical
2023-10-24
Conclusions Declarations Introduction The classical term of endocrine disruption includes any agent that interferes with the action of hormones within the human body; these agents are therefore named endocrine disruptors. Among these agents, that are mainly environmental chemicals (pollutan
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fibronectin definition mg To elucidate this relationship we
2023-10-24
To elucidate this relationship, we developed a spatial model of Ca-influx through N-methyl-D-aspartate receptor (NMDAR), CaMKII/PP1 activation, and AMPAR insertion in a realistic spine geometry. Using this model, we show that i) variables in membrane voltage mediated Ca-influx, particularly the numb
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Recently a Phase III study demonstrated that alectinib
2023-10-24
Recently, a Phase III study demonstrated that alectinib, the second-generation ALK inhibitor, might have a better response to ALK-rearrangement patients than crizotinib [10]. Should alectinib replace crizotinib as the frontline treatment for ALK-rearranged patients? Or should those patients be treat
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Although several ARIs have reached various
2023-10-24
Although several ARIs have reached various phases of clinical experimentation however most of them have been withdrawn either due to an insufficient bioavailability, their poor efficacy or adverse side effects. Currently Epalrestat is in clinical use for the treatment of diabetic neuropathy. The sid
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The excellent potencies selectivities and improved
2023-10-24
The excellent potencies, selectivities and improved PK associated with the piperazine class triggered more extensive off-target screenings of the highlighted compounds. A screen of more than 100 enzymes, receptors, and ion channels resulted in activity at the norepinephrine transporter (NET). This
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The Cebu Longitudinal Health and Nutrition Survey CLHNS
2023-10-24
The Cebu Longitudinal Health and Nutrition Survey (CLHNS) genome-wide association study investigated the genetic loci associated with plasma adiponectin in 1776 unrelated Filipino women. Adiponectin was strongly associated with three genetic positions: the gene CDH13 (rs3865188, P ≤ 7.2 × 10−16), ne
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The same applies also to intermediate formally obtained
2023-10-24
The same applies also to intermediate , formally obtained by elimination of the R substituent from compound . If compared to the thienopyrimidine derivatives (series , C), the thieno[3,2-]pyridazin-5(4H)-ones – explored herein seem to maintain similar size and shape and also analogue structural char
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Synthesis pharmacological evaluation for the binding at
2023-10-24
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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Toxicity is the main reason for the failure at
2023-10-23
Toxicity is the main reason for the failure at all stages of the new drug development process. The major part of safety-related attrition occurs at preclinical phases while predicting preclinical safety liabilities earlier in the drug development process. This strategy enables the design and/or sele
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In this study we make
2023-10-23
In this study, we make the first simultaneous recordings of MRT68921 receptor release in multiple brain regions at a temporal resolution less than 1 s. One of the most striking findings is that acetylcholine release has a remarkably similar temporal profile in the mPFC and dHPC, suggesting a coordi
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Regarding the HT B receptors they act as terminal receptors
2023-10-23
Regarding the 5-HT1B receptors, they act as terminal receptors and are involved in the presynaptic regulation of the release of 5-HT. But at spinal level these receptors are principally situated post-synaptically (Sari, 2004). The ability of autoreceptors to regulate extracellular levels of 5-HT dur
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By performing knockdown of AXL
2023-10-23
By performing knockdown of AXL once HER2+ cancer Solasodine have achieved lung colonization, we demonstrated that AXL contributes to the establishment of macrometastases. While inhibition of AXL impairs the efficiency of metastasis, the later finding has major clinical implications since pharmacolo
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br Conflict of interest br Acknowledgements We
2023-10-23
Conflict of interest Acknowledgements We thank Ann Jackman, Mike Ormerod and members of Julian Downward's and Alan Ashworth's groups for helpful discussions. This work was supported by grant number PEM/GME/D391/40 from the Kidani Trust (S. Kaye) and by Keele University. Introduction Autota
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ATM dependent initiation of radiation induced
2023-10-23
ATM-dependent initiation of radiation-induced G2/M checkpoint arrest is well established [11], [34], [35]. However, the ATR pathway may also be involved [36], [37]. Brown and Baltimore generated Cre/lox-conditional cell lines or MK2 inhibitor with a kinase inactive allele of ATR (ATRkd) to evaluate
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Why do glutamate and glycine bind to the
2023-10-23
Why do glutamate and glycine bind to the AACOCF3 in such different ways? Given the overall structural similarity between the GluN2A and GluN1 LBDs, one might conclude that the LBDs also bind ligands via similar processes. NMDA receptors with engineered disulfide linkages that lock the GluN1 lobes s
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