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br Acknowledgements This work was supported
2023-01-05
Acknowledgements This work was supported by National Natural Science Foundation of China (Nos. 21376172, 21528601 and 21621004) and the Natural Science Foundation of Tianjin from Tianjin Municipal Science and Technology Commission (Contract No. 16JCZDJC32300). Introduction Alzheimer’s disease
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87 8 We recently identified a G A dependent epigenetic mecha
2023-01-05
We recently identified a G9A-dependent epigenetic mechanism for transcriptional activation of the serine pathway in cancer cells (Ding et al., 2013). G9A, also known as EHMT2 and KMT1C, is a H3K9 methyltransferase that has a primary role in catalyzing H3K9me1 and H3K9me2 in euchromatin (Shinkai and
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The cavity volume of the binding pocket may differ not
2023-01-05
The cavity volume of the binding pocket may differ not only between species but also among various AhR/ARNT isoforms within a single species. It is noteworthy that even a single amino Cy7 NHS ester (non-sulfonated) substitution within a binding pocket may result in a change in the cavity volume. Thi
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To investigate the potential link between G and MT assembly
2023-01-05
To investigate the potential link between Gβγ and MT assembly in vivo, cultured NIH3T3 and PC12 cells were used. The role of Gβγ in MT assembly was demonstrated using nocodazole, a MT depolymerizing drug [14]. We found that Gβγ was preferentially bound to MTs in NIH3T3 and PC12 cells and treatment w
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Subsequently Palvimaki et al corroborated Ni and Miledi s
2023-01-05
Subsequently, Palvimaki et al. (1999) corroborated Ni and Miledi's study by demonstrating that treatment with fluoxetine leads to 43% occupancy of the 5-HT2C receptors. Moreover, the affinity of fluoxetine for 5HT2C receptors (Ki 65 nM) is close to its affinity for 5-HT transporters (Ki 33 nM) (Ni a
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To our knowledge BAY has not progressed to
2023-01-05
To our knowledge, BAY 60-6583 has not progressed to clinical development and remains to be the only ADORA2B agonist that has been developed.33, 34 Further development of similar compounds would be beneficial in future fibrosis research. One of the limitations of our study is being limited to in vit
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br Materials and methods br Results br Discussion In the
2023-01-05
Materials and methods Results Discussion In the present study, we aimed to elucidate the contribution of adenosine receptors to vascular tone in mice with T1D. We showed that diabetes resulted in decreased A1 adenosine receptor-mediated contraction in the aorta, which was accompanied by inc
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br Experimental section br Results and discussion br Conclus
2023-01-04
Experimental section Results and discussion Conclusions We present a simple, sensitive and selective assay of ADA activity and its inhibitor using the enzyme catalyzed reaction and the different interaction intensity of dye-labeled AD aptamer, aptamer/AD complex with GO. The as-proposed met
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An alternative to the agonist or antagonist potential
2023-01-04
An alternative to the agonist or antagonist potential in drug discovery is the positive allosteric modulator (PAM) approach, which can augment the normal processes of neurotransmission as opposed to directly replacing or antagonizing them. PAMs are thought to bind to sites that are distinct from the
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Several tertiary prevention studies are
2023-01-04
Several tertiary prevention studies are currently underway examining the use of dutasteride for prostate cancer treatment: (1) during expectant management of prostate cancer, (2) after radical prostatectomy in men at high risk for relapse, and (3) in men with metastatic disease. The Reduction by Dut
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br Acknowledgements DHA was funded by a research grant
2023-01-04
Acknowledgements DHA was funded by a research grant from Viamet and IMB and DHA were/are consultants for Viamet/Innocrin. DHA also supported by NIH P51-OD011106. Introduction Congenital adrenal hyperplasia resulting from 17alpha-hydroxylase and 17,20-lyase deficiency (17OHD) is a rare autosom
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Thus one possible target for
2023-01-04
Thus one possible target for CRPC treatment is the enzyme 17,20-lyase, which plays a crucial role in androgen biosynthesis. This is because inhibition of 17,20-lyase would be expected to decrease serum androgen levels secreted not only by the testes but also by the adrenal glands.7, 8, 9 In recent
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Recent studies have indicated that
2023-01-04
Recent studies have indicated that V-ATPase activity negatively regulates vacuolar fusion in vivo[17]. Since we have demonstrated that the pah1Δ 4-Aminobutyric acid have a more acidic vacuolar pH than the WT cells, and the genes involved in the pump activity are upregulated compared to WT, the pah1Δ
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In considering the roles of these enzymes in
2023-01-04
In considering the roles of these enzymes in normal physiology, given the importance of GLUT4-dependent glucose uptake and glucose-dependent fatty HAMI3379 synthesis synthesis for systemic metabolic homeostasis (Herman and Kahn, 2006, Herman et al., 2012), deletion of Acly in adipocytes results in
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Beside estrogen several classes of compounds
2023-01-04
Beside estrogen, several Ciclopirox of compounds have shown significant neuroprotective efficacy when administered shortly after the induction of animal models of stroke, including glutamate (NMDA) receptor antagonists and zinc chelators [25], [26], [27]. Effects of these or other neuroprotective a
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