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Human GPR hGPR was originally isolated in as an orphan
2021-09-17

Human GPR55 (hGPR55) was originally isolated in 1999 as an orphan GPCR with high levels of expression in human striatum (Sawzdargo et al., 1999) (Genbank accession # NM_005683.3). hGPR55 was mapped to human chromosome 2q37, and in the human CNS it is predominantly localized to the caudate, putamen,
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Generally speaking the regulation of GnIH on gonadotropins s
2021-09-17

Generally speaking, the regulation of GnIH on gonadotropins synthesis and release, although controversial, could be direct and/or indirect via GnRH, among others peptides. In this sense, different scenarios have been reported in vertebrates. In mammalian and avian species, GnIH fibers reach the medi
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On the other hand it is quite possible that
2021-09-17

On the other hand, it is quite possible that strychnine-sensitive glycine sites are responsible for mediating the anticonvulsant effects of GlyT1 inhibitors. Strychnine, which acts as an antagonist at these sites, is a well-known as a convulsant drug, and elevation of endogenous glycine levels at th
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In silico analysis revealed structural similarities between
2021-09-17

In silico analysis revealed structural similarities between the CpMutY and the EcMutY which share typical domains and structural motifs (Fig. 5), common to a wide range of structurally related DNA repair enzymes. These include an endonuclease III domain, involved in excision of damaged pyrimidines,
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Darifenacin HBr Ubiquitination of GlyRs subunit on plasma
2021-09-17

Ubiquitination of GlyRs-α1 subunit on plasma membrane has been shown to initiate the receptor Darifenacin HBr 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 conse
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how do you calculate molarity The aims of the present study
2021-09-17

The aims of the present study were to further investigate the localisation of glycine and GABAA receptors on individual neurons and how closely these two receptor types were associated with each other by carrying out double immunofluorescent labelling and imaged using confocal laser scanning microsc
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To help resolve the question of
2021-09-17

To help resolve the question of simple binding versus transport, we reasoned that if quercetin is transported by GLUT1, we should be able to block its uptake by other GLUT1 inhibitors. We initially investigated the effects of two newly identified GLUT1 inhibitors, BAY-876 and WZB-117. WZB-117 was fi
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Importance of glucokinase in glucose homeostasis and a possi
2021-09-17

Importance of glucokinase in glucose homeostasis and a possibility to change its activity using the activators define the scientific interest in the development of new allosteric activators of GK (Liu et al., 2012, Pfefferkorn et al., 2011, Waring et al., 2013, Behera et al., 2015). Activation of gl
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Interruption of glucagon signaling pathway targeting glucago
2021-09-17

Interruption of glucagon signaling pathway targeting glucagon receptor (GCGR) by gene knockout, antisense oligonucleotides or specific antagonists induces α-cell hyperplasia and alleviates hyperglycemia and other metabolic symptoms in diabetic animals and patients [[7], [8], [9]]. Here we used a ful
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br Acknowledgments br Introduction Postmenopausal osteoporos
2021-09-17

Acknowledgments Introduction Postmenopausal osteoporosis, which is primarily caused by CHAPS deficiency, has been a worldwide health problem and threatens postmenopausal women of all races. An estimated 80% of osteoporosis patients in the United States are women, and approximately 30% of post
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As shown in Table the results of individual prediction
2021-09-17

As shown in Table 3, the results of individual prediction modeling with chemicals at 0.4 mM, 0.6 mM, and 0.8 mM would lead to lesser sensitivity of 60.0%, 65.0%, and 65.0%, respectively, in microsome-unused group, and 85.0%, 85.0%, and 90.0%, in microsome-used group. If we consider only the results
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In conclusion a novel series of
2021-09-17

In conclusion, a novel series of GPR40 agonists containing nitrogen heterocyclic rings derived from TAK-875 were designed and synthesized. The structural activity relationship studies indicated that the substituents on the nitrogen Vatalanib had a remarkable effect on the GPR40 agonistic activity.
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Focal adhesion kinase FAK is a
2021-09-17

Focal adhesion kinase (FAK) is a non-receptor type tyrosine kinase that can further cooperatively interact with receptor tyrosine kinase signaling to regulate adhesion, migration, survival, proliferation, polarization, and differentiation [12]. Following activation, phosphorylated extracellular regu
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Not only has the cortical actin
2021-09-17

Not only has the cortical GSK3787 network been found to influence plasma membrane properties but also to interact with exo- and endocytic vesicles (Gormal et al., 2015, Tomatis et al., 2013). The interplay between actin and membranes is integrally regulated by the phosphoinositide composition of th
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It is interesting that SEC significantly inhibited cell migr
2021-09-16

It is interesting that SEC significantly inhibited cell migration and EMT in PC3 cells expressing a low RKIP level and HEK293T RKIP−/− cells, while had no effect on HEK293T RKIP+/+ cells. These observations can be interpreted that the RKIP-ANXA7 association may block SEC-induced ANXA7 GTPase activat
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