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br AMPK as a druggable target AMPK signaling has
2024-11-23
AMPK as a druggable target AMPK signaling has attracted considerable attention within the past decades, owing to the capacity of pharmacological compounds (e.g., 5-aminoimidazole-4-carboxamide-1-β-D-ribofuranoside [AICAR] and metformin) or natural compounds (e.g., resveratrol) to activate AMPK in
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However relatively little information is available concernin
2024-11-23
However, relatively little information is available concerning the biochemical properties and other features of such enzymes in Taeniid species. In the current report, a M17 leucine aminopeptidase gene of T. pisiformis (TpLAP) was cloned and expressed, and its enzymatic activity, biochemical propert
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The inflammatory cytokine IL is an additional factor
2024-11-22
The inflammatory cytokine IL-6 is an additional factor that has been hypothesized to contribute to epinephrine-mediated repression of drug detoxifying proteins such as CYP3A4 (Aninat et al., 2008). Indeed, this CYP is well-known to be repressed by IL-6 (Dickmann et al., 2011) and epinephrine has pre
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AMPK is an essential player in adiponectin
2024-11-22
AMPK is an essential player in adiponectin signaling pathway that regulates energy metabolism. The fact that suppression of AMPK activity by compound C largely diminished candesartan-mediated inhibition of NFκB via blocking AT1 also suggests that the AT1-mediated effect is at least partly resulted f
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The first natural product described as LO inhibitor
2024-11-22
The first natural product described as 5-LO inhibitor was the polyphenol nordihydroguaiaretic cetp inhibitor from the Mexican dessert plant Larrea divaricata in 1981 (Bokoch and Reed, 1981), short after the initial identification of 5-LO in 1979 (Borgeat and Samuelsson, 1979). Long time before mPGE
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rs G allele was previously associated with a decrease in
2024-11-22
rs523349 G allele was previously associated with a decrease in the conversion rate of testosterone to DHT (Beesley et al., 2007). This SRDA52 variant may have a trend towards higher testosterone availability, which according to the US Food and Drug Administration is described as a teratogen of categ
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monocrotaline As mentioned above variation of the
2024-11-22
As mentioned above, variation of the A-ring was undertaken in order to improve microsomal stability and kinase selectivity relative to monocrotaline (). 1-Imidazole-2-carboxamides with substitution at the 4-position (–) were mostly tolerated with 4-cyano-imidazole-2-carboxamide () having comparable
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Regarding brain tumors AXL has been implicated in gliomagene
2024-11-22
Regarding sodium fluoride australia tumors, AXL has been implicated in gliomagenesis and chemoresistance [39]. Previous investigations found that AXL is constitutively phosphorylated in many glioma cell lines, murine xenograft tumors and primary patient tumor samples [40]. Immunohistochemical anal
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Autotaxin has been linked to chemoresistance through its
2024-11-22
Autotaxin has been linked to chemoresistance through its ability to inhibit apoptosis induced by paclitaxel in breast cancer TL32711 [15] and LPA can inhibit cell death induced by cisplatin [40]. Autotaxin was included in the present study because it was identified as being over-expressed in patien
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Skeletal pain associated with bone fracture
2024-11-22
Skeletal pain associated with bone fracture is another area of critical need for a novel pain medication. NSAIDs and opiates are the two major therapies currently used to manage bone fracture pain. However, both of these therapies lead to significant unwanted side effects. Using the osteotomy model
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Aurora Kinase Inhibitor III Here we report discovery of
2024-11-22
Here we report discovery of highly selective pan-Aurora kinase inhibitors through phenotypic screening. The co-crystal structure of Aurora Kinase Inhibitor III bound in the ATP binding site of Aurora A is described, and provides insight into the possible structural basis for the selectivity of the
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Analyzed by qRT PCR Fig
2024-11-22
Analyzed by qRT-PCR (Fig. 8), the variation of the expressions of DtACLA and DtACLB was fairly consistent in response to nitrogen deficiency, suggesting that DtACLA and DtACLB may be coordinate to function in the catalysis. It was reported that in Arabidopsis, the coordinated ACLA and ACLB mRNA accu
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We demonstrated clearly that the overexpression
2024-11-22
We demonstrated clearly that the overexpression of sFlt-1 significantly increased arginase N1-Methylpseudouridine and enhanced arginase activity in HUVECs (Fig. 3). NO formation is related inversely to serum levels of sFlt-1 in preeclampsia [11]. The disorder of NO formation, which was involved in h
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Most human diseases e g cancer diabetes and neurodegenerativ
2024-11-21
Most human diseases (e.g., cancer, diabetes, and neurodegenerative diseases) are complex and multifactorial. Several investigations in the literature focused on new multi-target drug development, which implies active pharmacophores incorporation in one scaffold (Meunier, 2008, Lazar et al., 2004, Te
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Numerous investigators have shown that RACK has
2024-11-21
Numerous investigators have shown that RACK1 has several important, possibly related, roles in mRNA splicing and in translation. RACK1 interacts directly with specific components of the 40S ribosomal subunit (specifically, the 18S rRNA and ribosomal proteins rpS16e, rpS17e, and rpS3e [new names: uS9
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