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The benzimidazole group seems to
2024-03-22
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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Drug resistance development often involves
2024-03-22
Drug resistance development often involves structurally un-related drugs and, specifically both conventional and targeted agents. IGROV-1/Pt1 DMSO are characterized by resistance to cisplatin and reduced sensitivity to inhibitors of EGF-R and MEK, the up-stream activator of ERK1/2, associated with
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br Materials and Methods br Author Contributions br
2024-03-22
Materials and Methods Author Contributions Conflicts of Interest Acknowledgments This study was funded by the NIH Common Fund (UH2TR000943) through the Office of Strategic Coordination/Office of the NIH Director, an NCI/NIH grant (1R21CA199050), the MD Anderson Cancer Center support gran
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Naltrindole hydrochloride receptor br Acknowledgments br Int
2024-03-22
Acknowledgments Introduction Cancer is the leading cause of mortality in the United States for those between the ages of 40–79 years, surpassing heart diseases by more than 100,000 deaths [1]. The cause of most cancer subtypes remains idiopathic and may arise out of ‘bad luck’ among otherwise
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br Conflict of interest br Introduction Ovarian cancer is
2024-03-22
Conflict of interest Introduction Ovarian cancer is the most lethal gynecological malignancy, and ranks as the fifth leading cause of cancer death among women. The American Cancer Society estimates that about 22,280 new ovarian cancer cases and 14,240 deaths will occur in the United States in
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The overall mechanism of the Cdc complex resembles that of
2024-03-22
The overall mechanism of the Cdc48 complex resembles that of the 19S regulatory subunit of the proteasome, which also uses receptor proteins to bind polyubiquitin chains attached to a substrate and employs a translocation mechanism (for review, see Kish-Trier and Hill, 2013). As with Cdc48, full su
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Acl converts cytosolic citrate CoA
2024-03-22
Acl converts cytosolic citrate, CoA and ATP into acetyl-CoA, ADP+Pi and oxaloacetate (Fig. 1). This cytosolic enzyme is present in few Prokaryotes and in all Eukaryotes, but not in non-oleaginous yeasts [14]. Thus, this enzyme was presumed to be essential for FA synthesis [1], [13], [15]. In most mi
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We have shown that an extensive region
2024-03-22
We have shown that an extensive region in SERBP1 (amino acids 354 to 474, using co-ordinates based on the full-length isoform, Figs. 1a and 2) is necessary for it to interact with RACK1; since this region has substantial homology to the corresponding region of HABP1 (Fig. 3) it is a reasonable hypot
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In a recent issue of Minokoshi
2024-03-22
In a recent issue of , Minokoshi and colleagues have added more light to our understanding of the role of hypothalamic AMPK in the regulation of energy balance. Previous seminal work from the same group suggested that AMPK in the PVH might be involved in the modulation of feeding . Here, they show
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AdipoR and AdipoR have been reported to
2024-03-21
AdipoR1 and AdipoR2 have been reported to be present in almost all type of tissues and low LCL161 levels have been observed in white adipose tissue (Inukai et al., 2005). These receptors have been observed to become deregulated with the onset of obesity, resulting in a reduced level of APN expressi
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The activation of the A BR subtype triggers different intrac
2024-03-21
The activation of the A2BR subtype triggers different intracellular metabolic pathways, often linked to the activation of adenylyl cyclase and increased levels of intracellular cAMP (Lynge et al., 2003, Bernareggi et al., 2015). The nAChR-channel NB-598 Maleate synthesis mediated by the cAMP/PKA pa
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br Perspectives and challenges Previously the main focus of
2024-03-21
Perspectives and challenges Previously, the main focus of development of adenosine targets for pain was on A1Rs, due to prominent antinociception in multiple preclinical models and preliminary observations in human trials. However, delivery of agonists can be limited by other (e.g. cardiovascular
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Although ACE genetic variance does not
2024-03-21
Although ACE genetic variance does not influence the level of bradykinin significantly, the bradykinin level tends to be affected by ACE inhibitor therapy used by patients. ACE inhibitor reduces the ACE activity that may lead to the accumulation of serum bradykinin. The level of bradykinin tends to
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To maintain ATP levels postmortem muscle mobilizes its
2024-03-21
To maintain ATP levels, postmortem muscle mobilizes its glycogen reserves to yield PXD101 6-phsphate that proceeds through glycolysis. Glycogen degradation was affected by the interaction between treatment and time (Pinitiation of the experiment. We expected that if myosin ATPase is limiting, then
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br Introduction O Dowd et al identified a gene
2024-03-21
Introduction O’Dowd et al. identified a gene very similar to angiotensin type-1 receptor in 1993 (O’Dowd et al., 1993). The specific selective ligand of this receptor called APJ receptor was determined by Tatemoto et al. in 1998 as apelin (Tatemoto et al., 1998). The high expression of apelin and
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