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Recently a Phase III study
2024-08-15
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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Adiponectin is an adipokine whose circulating level
2024-08-15
Adiponectin is an adipokine whose circulating level is depleted in a number of metabolic diseases including insulin resistance, diabetes and cancer (Khan et al., 2015, Singh et al., 2014a, Singh et al., 2014b, Yamauchi et al., 2014). Despite its importance in health and pathophysiology, adiponectin
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br ACK signaling partners ACK interacts with
2024-08-14
ACK1 signaling partners ACK1 interacts with and tyrosine phosphorylates many cellular proteins regulating critical cellular processes [11]. While ACK1 shares common intracellular effectors such as AKT with other signaling pathways, it imparts specificity to signaling by phosphorylating effectors
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br Materials and methods br Functional demonstrations of
2024-08-14
Materials and methods Functional demonstrations of ACh/GABA cotransmission The cotransmission of GABA and ACh has been best characterized in starburst amacrine cells (SACs) of the retina. SACs are a subtype of amacrine cell, a diverse set of retinal interneurons that are crucial for processing
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The acetylcholinesterase AChE inhibitor tacrine THA exerts n
2024-08-14
The acetylcholinesterase (AChE) inhibitor, tacrine (THA), exerts neuroprotective effects in time- and does-dependent manners against glutamate neurotoxicity (Takada-Takatori et al., 2006a, 2006b) and amyloid-β protein toxicity in PC12, a pheochromocytoma line (Wang et al., 2002; Xiao et al., 2000).
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Although experiments on animals and cells indicate
2024-08-14
Although experiments on animals and cells indicate that antioxidant and free radical scavenging agents have protective effects against brain damage, the results of preclinical trials are not as encouraging. Edaravone is a type of free radical scavenging drug that was first used as a neuroprotective
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Another significant group of reductase inhibitors is the ste
2024-08-14
Another significant group of 5α-reductase inhibitors is the steroidal 3-carboxylic H-Lys(Ac)-OH.HCl australia derivatives (relevant examples in Fig. 5), which were designed to mimic the putative enzyme-bound enolate intermediate. This was achieved by introducing sp2-hybridized centers at C3 and C4
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Herein we disclose novel dihydropyrano c
2024-08-14
Herein, we disclose novel 2,4-dihydropyrano[2,3-c]pyrazoles that inhibit human ATX (hATX). Our results demonstrate and further support previous findings showing that a desired biological action can be achieved without targeting the catalytic site of the enzyme. Moreover, this study validated hen egg
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We wanted to investigate the
2024-08-14
We wanted to investigate the influence of substituents on the pyrazole ring on the activity, but only a few substituted pyrazole-3-carboxylic acids/esters were commercially available in useful amounts at a reasonable price, for example, 4- and 5-nitro-pyrazole-3-carboxylic acid. The preparation of 4
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Another hypothesis is angiogenesis inhibition Angiogenesis i
2024-08-14
Another hypothesis is angiogenesis inhibition. Angiogenesis is a process that involves the growth, migration and differentiation of endothelial pterostilbene to form new blood vessels. Angiogenesis favorably influences tumor growth and also influences tumor invasion of vessels, resulting in tumor m
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Various compounds have been designed to
2024-08-13
Various compounds have been designed to inhibit aldose reductase (AR) [12]. These compounds can be classified into two main categories, the first category comprises those containing a carboxylic 5α-dihydro-11-keto Testosterone moiety, for example, 3-thiazolidineacetic acid derivative, which has bee
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br Materials and methods br Results and discussion
2024-08-13
Materials and methods Results and discussion Conclusion Amino-functionalized mesoporous TiO2-NH2 microparticles were used to immobilize ADA, followed by GLU cross-linking. The mesopores provided a natural microenvironment with sufficient room for the enzyme to efficiently perform its cataly
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HT receptors are distributed throughout the
2024-08-13
5-HT3 receptors are distributed throughout the brain, within the brainstem (e.g., nucleus tractus solitarius, area postrema and spinal trigeminal nucleus) and colometric (e.g., hippocampus, amygdala, nucleus accumbens, putamen and caudate) (Abi-Dargham et al., 1993, Barnes et al., 1989, Bufton et a
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The c C T mutation identified
2024-08-13
The c.286C>T mutation identified in subject K20-1 was also reported in other ethnic groups, including Brazilian, French-Canadian, Italian, and Arabs from the United Arab Emirates [20], [21], [22], whereas c.318A>G mutation in subjects K10-1 was previously reported in Asian and Caucasians [13], [23],
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br Materials and methods br
2024-08-13
Materials and methods Results Discussion CUs, which have been used as traditional medicine for thousands of years in East Asian countries, have the potential to be used for cancer chemoprevention and chemotherapy [17], [18], [19], [20]. CuB is one of the most promising agents as it is repor
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