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In conclusion while class I HDAC inhibitors isoform specific
2022-07-12

In conclusion, while class I HDAC inhibitors, isoform-specific HDAC3 and HDAC6 inhibitors may represent novel therapeutic targets for prevention of clinical AF onset and progression, the specific HDAC3 and HDAC6 inhibitors may be more appropriate because of their limited off-targets effects. Besides
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br Conclusion br Disclosure of
2022-07-12

Conclusion Disclosure of interest Acknowledgement Introduction Vitamin B6 has long been recognized as a cofactor for many enzymes, especially those involved in amino Pyridoxal 5 phosphate metabolism. Apart from its role as coenzyme, recent studies are unveiling a new role of vitamin B6
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br Conclusions and future perspectives br Declarations
2022-07-12

Conclusions and future perspectives Declarations of interest Acknowledgements The authors thank Mrs. Kamala Pandey for the help in the preparation of this manuscript. This work was supported by NIH grants R01HL057531 and R01HL062147. Introduction Separation of short exons by long non-co
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br Materials and methods br Results
2022-07-12

Materials and methods Results Discussion Reduced glutathione is considered to be one of the important regulators of REDOX balance in the biological system. The cellular concentration of 4-HNE under physiological conditions ranges from 0.1 to 3μM and has no detrimental effect in the biologic
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SW033291 br Acknowledgments br Introduction Obesity and
2022-07-12

Acknowledgments Introduction Obesity and type 2 diabetes (T2D) are two major chronic non-communicable diseases that are increasing worldwide at an alarming rate; the majority of people with T2D are overweight or obese, and T2D associated with obesity is expected to have doubled by 2030 (Chen e
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br Introduction Marijuana remains the most widely used illeg
2022-07-12

Introduction Marijuana remains the most widely used illegal drug (Murray et al., 2007), and its validated targets include plasma membrane cannabinoid receptors, many of which are found in the central nervous system. The diverse physiological effects produced by marijuana and cannabinoid ligands s
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With this goal in mind we proceeded to explore
2022-07-12

With this goal in mind, we proceeded to explore the C5-heteroaryl class of pyrazole-acids. Initial efforts, focused on a thiophene replacement, demonstrated little improvement. The 2-thiophene derivative (0.25μM and 0.24μM), a surrogate to the phenyl moiety, demonstrated only a modest boost in acti
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The precise mechanisms of action of PBA are
2022-07-11

The precise mechanisms of action of 4-PBA are as yet ambiguous. Its capacity as a chemical chaperone has been thoroughly documented for the ABC transporter family in particular (Prulière-Escabasse et al., 2007; Iram and Cole, 2014; Gordo-Gilart et al., 2016; Pomozi et al., 2017). 4-PBA has been clas
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Ubiquitination of GlyRs subunit on plasma membrane has been
2022-07-11

Ubiquitination of GlyRs-α1 subunit on plasma membrane has been shown to initiate the receptor iib iiia inhibitors and subsequent degradation in lysosomes (Buttner et al., 2001). However, the specific E3 ligase responsible for GlyRs-α1 ubiquitination is largely unknown as yet. Also, the functional c
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In respect of clinical development Takeda has pioneered the
2022-07-11

In respect of clinical development Takeda has pioneered the field with the GPR40 agonist TAK-875 or fasiglifam (Figure 2A), which in phase-II studies decreased HbA1c as efficiently as sulfonylurea without signs of hypoglycemia [24]. This was obtained with surprisingly little effect on systemic insul
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A significant contribution to the discovery
2022-07-11

A significant contribution to the discovery of novel Hh inhibitors is given by natural compounds [11,17,22,31,32]. The first Hh inhibitor ever discovered has been Cyclopamine, a steroidal alkaloid isolated from plants of the Veratrum species [13,33]. Subsequently, many natural compounds belonging to
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Introduction galactosidase d galactoside galactohydrolase or
2022-07-11

Introduction β-galactosidase (β-d-galactoside galactohydrolase or lactase; EC 3.2.1.23) is an important type of glycoside hydrolase that can catalyze the conversion of lactose to chir99021 and galactose. Furthermore, it can also catalyze transglycosylation reactions, which are usually used for the
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In the course of our
2022-07-11

In the course of our ongoing attempts to photolabel allosteric binding sites of γ-aminobutyric DPQ type A (GABAA) receptors, we were met with the need for relatively large (near mg) quantities of recombinant protein. Rather than establishing a stable cell line we sought to optimise the process of t
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br Material and methods br Results and discussion
2022-07-11

Material and methods Results and discussion Discussion It is well established that the guanosine-rich DNA sequences within telomeric DNA repeats, and in the promoter regions of a number of oncogenes or proto-oncogenes such as c-myc [20,23], VEGF [28,48,49] and Bcl-2 [21,50], can readily ass
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In the case of acute inflammation such as ischemic injury
2022-07-11

In the case of acute inflammation such as ischemic injury of heart, brain, lung and kidney as wells as in the case infection related injury it is now well established that the leukocytes particularly polymorphonuclear (PMNs) 1 98 are the first responders. Under normal circumstances these leukocytes
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