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Since forskolin is known to
2024-06-25
Since forskolin is known to act directly at the catalytic site of adenylate cyclases near the ATP binding (Tesmer et al., 1997), the synergistic and/or permissive effect of gonadotropins on FSK activity must occur at the level of AC itself or very near, at the level of one of its direct partner. The
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Regarding A Rs and A ARs basal conditions generate
2024-06-25
Regarding A1Rs and A2ARs, basal conditions generate a low tone of endogenous adenosine and cause A1R activation, in contrast to situations of increased adenosine where A2AR activation becomes dominant. When adenosine concentrations rise, e.g. during hypoxia, also time appears likely important in reg
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Derivatives of M that possess either an alkyne or an
2024-06-25
Derivatives of (+)-M100907 that possess either an alkyne or an azide have been synthesized. The most active enantiomer was obtained by resolution of a relatively early intermediate in the synthesis. The ability of these PLX-4720 to maintain 5-HTR antagonist properties as (+)-M100907 was demonstrate
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We conducted the largest drug
2024-06-25
We conducted the largest drug screen to date in HPV-positive cancers and identified Aurora kinase inhibitors as effective and understudied drugs in HNSCC and CESC. These drugs cause apoptosis and cell cycle arrest in vitro and decrease tumor size in vivo. This is the first published study to demonst
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CHK has been reported to
2024-06-25
CHK1 has been reported to be the kinase responsible for H3.3S31 phosphorylation in human ALT cancer Oxybutynin . However, in our study, knockdown of CHK1 in HEK293F (Figs. S1c and S6) or HeLa S3 (data not shown) cells did not result in a significant decrease in H3.3S31ph, which is in agreement with
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Our results suggest that plasma membrane and a containing V
2024-06-25
Our results suggest that plasma membrane and a3-containing V-ATPases represent an important and novel target in the development of drugs to limit breast cancer metastasis. That knock-down of a3 has been shown to reduce metastasis of melanoma cells in an in vivo mouse model suggests that this role ma
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In humans the superior safety profile of lipid associated
2024-06-24
In humans, the superior safety profile of lipid-associated formulations is characterized by decreased acute infusion-related reactions and dose-related nephrotoxicity, allowing the administration of larger doses and therefore similar efficacy with fewer administrations. In vitro studies and human cl
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br Materials and methods br Results br
2024-06-24
Materials and methods Results Discussion Conclusions These studies provide important mechanistic insights to explain the long-established physiological observation that obese adipose tissue has higher rates of basal lipolysis. Increased lipolysis contributes to increased hepatic (R)-bacl
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To assess relative metabolic activity and proliferation of c
2024-06-24
To assess relative metabolic activity and proliferation of DTP3 mg attached to various substrates we used the MTT assay [29], [30]. In order to compare the metabolic activity of cells under the various conditions irrespective of the number or viability of the cells, we performed a PicoGreen DNA ass
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ADA catalyzes the deamination of adenosine and deoxyadenosin
2024-06-24
ADA catalyzes the deamination of adenosine and deoxyadenosine into their respective inosine nucleoside (Cristalli et al., 2001). This conversion is an initial step in a series of reactions responsible for lymphocyte proliferation and differentiation. Moreover, ADA is considered an indicator of cellu
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Salivary amylase activity was not significantly
2024-06-24
Salivary α-amylase activity was not significantly different between bitches with pyometra and healthy bitches, and there were no significant changes after ovariohysterectomy, similar to chromogranin A (Jitpean et al., 2015). Therefore, it is postulated that the SAM axis is not activated in bitches w
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In this study we make the first simultaneous
2024-06-24
In this study, we make the first simultaneous recordings of Metaphit australia 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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br In patients with spina bifida and spinal cord injury
2024-06-24
In patients with spina bifida and spinal cord injury, fecal incontinence is a serious issue that can impair activities of daily living and patient self-esteem. To address this Malone et al. first described the Antegrade Continence Enema (ACE) procedure in 1990 [1], which achieves continence by all
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The most potent compounds within the current series of
2024-06-24
The most potent compounds within the current series of compounds were therefore , , , , and , with Verapamil HCl possessing the best selectivity towards the lyase reaction in comparison to the hydroxylase reaction, indeed, this compound was found to possess an IC value of 1210nM against the 17α-O
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The benzimidazole group seems to be a key
2024-06-24
The benzimidazole group seems to be a key feature for the excellent anti-tumor activity of galeterone (159), which motivated the synthesis of new steroidal inhibitors containing N-heterocyclic groups structurally related to benzimidazole. Thus, several 1H- and 2H-indazole derivatives of dehydroepian
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