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In summary A is a potent orally available endothelin
2021-04-14
In summary, A-216546 is a potent, orally available endothelin receptor antagonist with a high selectivity for the endothelin ETA receptor. The potency and bioavailability of A-216546 suggest that it will have important utility for preclinical evaluation of the pathophysiology of the endothelin syste
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The N B method has the overall
2021-04-14
The N&B method has the overall advantage that it is not restricted to certain dyes specific for energy transfer [55], and is also able to detect higher order receptor adrenergic receptors on the focal point in living cells. Conclusion The N&B method has shown to be a powerful tool to locate and
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PKA signalling in the nucleus was thought to
2021-04-13
PKA signalling in the nucleus was thought to be due to the translocation of the catalytic subunit upon activation from the c-di-AMP synthesis to the nucleus via diffusion [72]. However, a new understanding has emerged, as both the regulatory and catalytic subunits have been identified in the nucleu
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put off br A brief history of
2021-04-13
A brief history of RBR E3s RBR E3s were originally defined based on sequence alignments that predicted a tripartite motif of three zinc (Zn)-binding domains: two RING domains (RING1 and RING2) connected via an in-between-RING (IBR) domain [28], [29]. The prediction together with initial observati
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MuRF and MuRF in http www
2021-04-13
MuRF1 and MuRF3 in cooperation with the E2 ubiquitin-conjugating enzymes UbcH5a, -b, and -c were found to mediate degradation of myosin heavy chain β/slow (MHC β/slow) and MHC IIa via UPS, both, in vitro and in vivo [60]. Mice lacking both MuRF1 and MuRF3 developed skeletal muscle myopathy and hyper
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br Materials and methods br Results br Discussion The
2021-04-13
Materials and methods Results Discussion The first DGAT1 gene was described in the mouse in 1998 [28], and a few years later DGAT2 was identified from the oleaginous fungus Mortierella ramanniana[29]. Although both of them are known as the primary enzymes for de novo TAG biosynthesis, they
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br Four active site residues of
2021-04-13
Four active site residues of Δ1-KSTD1 are fully conserved in Δ1-KSTDs from different species (Supplementary Figure S2). These residues are Tyr-119, Tyr-487, and Gly-491 from the FAD-binding domain and Tyr-318 from the catalytic domain. The structure of the Δ1-KSTD1•ADD complex revealed that the hy
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br Results and discussion To check
2021-04-13
Results and discussion To check the MDL 28170 that the charge of α-synuclein can be altered due to the glycation, we measured zeta potential of native α-synuclein and α-synuclein glycated by two different glycating agents, methylglyoxal (MG) and glyceraldehyde-3-phosphate (GA-3-P). The value for
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br Results br Discussion Prostate cancer dissemination and
2021-04-13
Results Discussion Prostate cancer dissemination and skeletal metastases represent major therapeutic challenges. Once the skeletal metastasis occurs, the incurable patient could just be symptomatically treated to alleviate the pain. Therefore it is of great necessity to disclose the molecular
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guggulsterone In summary the reduction of one or more
2021-04-13
In summary, the reduction of one or more pro-inflammatory cytokines, such as TNF-α, IL-1β, IL-6, IL-8 was observed in almost all the monoterpenes studied. Increased levels of the anti-inflammatory cytokine IL-10 was shown to play a prominent function in the anti-inflammatory effect of monoterpenes,
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In conclusion our work provides the
2021-04-13
In conclusion, our work provides the preclinical evidence showing the potent in vivo efficacy of AT7519 on chemoresistant cancer Ranolazine 2HCl and its underlying mechanisms of action. Our work supports the biological rationale behind the clinical trials initiated with AT7519, particularly for the
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Beside the previously reported Topo I inhibition time
2021-04-13
Beside the previously reported Topo I inhibition, time and concentration dependent CRM1 inhibitory properties of klavuzon derivatives have been shown as a second mechanism of action in this work. Especially, compounds 3 and 20 are the most effective derivatives and they completely inhibit CRM1 activ
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Recently we have observed that pharmacological PPAR and PPAR
2021-04-13
Recently, we have observed that pharmacological PPARα and PPARβ/δ activation regulates the expression of genes involved in FA metabolism such as FAT/CD36, CPT1, LCAD and MCAD in Sertoli cells. We have also observed that PPARβ/δ activation can simultaneously regulate the expression of the above-menti
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Our study has several limitations As this study was
2021-04-13
Our study has several limitations. As this study was performed at a single institution, it had a limited sample size and was not powered to detect specific differences in assay performance by organ group or waitlist status. In the two CMV seropositive subjects with potential passive antibodies, the
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Pam2CSK4 synthesis It should be noted that the long
2021-04-13
It should be noted that the long-lifetime binding-responsive luminescence of ARC-1528 and ARC-1530 becomes evident only upon illumination with radiation at near-UV range where the excitation of ATB or ASB moiety is possible. At higher wavelength range (visible light), the fluorophore (5-TAMRA) can b
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