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A high throughput small molecule ACK biochemical inhibition
2023-02-03
A high-throughput small molecule ACK1 biochemical inhibition screen was performed in-house and led to the identification of 1μM inhibitor furanopyrimidine (). Further binding studies found caffeic acid to be both ATP-competitive and reversible. Early structure-activity relationship (SAR) work was pe
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The srd a isoforms showed
2023-02-02
The srd5a isoforms showed unique expression profiles in early FHM development (Fig. 2). Similar to amphibian embryos, there was a high abundance of both srd5a1 and srd5a3 at 1dpf in FHMs, suggesting that mRNA for these enzymes may be maternally deposited and that these enzymes may play a key role in
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A different mechanism has been suggested for
2023-02-01
A different mechanism has been suggested for the role of TRX1 in ASK1 regulation based on disulfide bond-mediated ASK1 multimerization and its reduction through the thiol-reductase activity of TRX1 (Nadeau et al., 2007, Nadeau et al., 2009). In this model, oxidative stress induces intermolecular dis
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ARG I is one of the most
2023-02-01
ARG I is one of the most important mammalian enzymes responsible for nitrogen metabolism since it comprises the main route for the elimination of excess nitrogen resulting from amino z vad fmk and nucleotide metabolism [18]. ARG I deficiency leads to hyperargininemia, characterized by progressive n
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Probenecid br The role of apelin
2023-02-01
The role of apelin in hypertension diseases The role of apelin and its receptor APJ in cardiovascular diseases has been described in numerous studies (Table 2) [36,37]. It has been revealed that exogenous apelin may lower blood pressure. Tatemoto et al. [6] have discovered that different forms of
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It remains unclear to what
2023-02-01
It remains unclear to what extent UCP2 and UCP3 are subject to the same acute molecular regulation as UCP1 (and the extent to which they share the same mechanism of uncoupling). Although they lack sequence homology in a matrix-localised region reportedly critical for fatty T0901317 activation of UCP
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Finally we argue that the estimated penetrance of CI
2023-02-01
Finally, we argue that the estimated penetrance of 0.45% (95% CI 0.02%, 9.35%) calculated by leveraging the gnomAD (Lek et al., 2016) population data indicate that T201S is at most a low-risk gene variant for CJD. If we arbitrarily consider a central estimate of 10% or higher as the clinically signi
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Although many factors influence the effects of medications d
2023-02-01
Although many factors influence the effects of medications, during recent years it has become evident that genetic factors could explain the differences between individuals in drug response. These differences are due to variants in genes encoding drug targets [8]. The challenge for pharmacogenetics
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Recent retrospective cohort studies have supported these pre
2023-02-01
Recent retrospective cohort studies have supported these preclinical findings in animals indicating the correlation of AR activation with the induction of Pregnenolone Carbonitrile carcinogenesis. First, men with prostate cancer who underwent androgen deprivation therapy were shown to have a signifi
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Sixth significant progress has been made during the last few
2023-02-01
Sixth, significant progress has been made during the last few years regarding the molecular mechanisms underlying the activation of AMPK and this should aid to develop more potent and specific compounds. Information from crystallographic structures combined with computer-based drug design hold promi
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br Rapid nongenomic effects of
2023-02-01
Rapid nongenomic effects of corticosterone in an amphibian model Studies in the model organism, the roughskin newt, Taricha granulosa, over 30 years ago led to the discovery that stress can rapidly (within minutes) suppress sexual behavior (amplectic clasping) of male T. granulosa, an effect that
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br Introduction ACK or Activated Cdc Associated Kinase
2023-02-01
Introduction ACK1, or Activated Cdc42-Associated Kinase, located on chromosome 3q, is a ubiquitously expressed non-receptor tyrosine kinase cloned from a human Oligomycin A cDNA library (Manser et al., 1993). It was first identified to bind to activated Cdc42, a small Ras GTPase via its CRIB dom
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In this study in an effort to
2023-02-01
In this study, in an effort to explore the possible role of 5-HT6 receptors in mediating the memory-enhancing effects of YL-0919, we first assessed the memory-enhancing effects of YL-0919 in the Morris water maze, object recognition test and step-down passive avoidance task. In addition, we then inv
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The present study showed for the first time that hirsutine
2023-02-01
The present study showed, for the first time, that hirsutine, hirsuteine, rhynchophylline, isorhynchophylline, corynoxeine, and isocorynoxeine in yokukansan can inhibit the 5-HT3 receptor current. These data indicate that part of the effect of yokukansan against the behavioral and psychological symp
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br Dihydrotestosterone in adult fish
2023-02-01
Dihydrotestosterone in adult fish and frogs New perspectives and next directions Similar to other androgens, DHT can modulate reproductive endpoints in both fish and amphibians. However, predicting the effects of DHT can be challenging, as reproductive homeostasis is dependent upon the balance
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