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Numerous small molecule CRF receptor antagonists have been r
2021-03-22
Numerous small molecule CRF receptor antagonists have been reported in the literature. Some representative examples are shown in . In preclinical studies (DMP696), , was found to be efficacious in preclinical behavioral models for anxiety and depression. In an open label clinical trial with (R121919
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Besides being an energy storing
2021-03-22
Besides being an energy storing tissue, adipose tissue acts as an active endocrine organ that secretes a number of biologically active adipokines involved in multiple physiological processes such as inflammation and lipid and glucose metabolism, with direct and indirect effects on reproduction [15,1
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Two major mechanisms including apoptosis and
2021-03-22
Two major mechanisms including apoptosis and oxidative stress have been suggested for MTX-induced cytotoxicity (Hafez et al., 2015; Neuman et al., 1999; El-Sheikh et al., 2015). It has been reported that MTX promotes cell death via apoptosis in both cancerous and non-transformed cells (Mazur et al.,
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br Results and discussion br Conclusion In this research sev
2021-03-22
Results and discussion Conclusion In this research, several anti-inflammatory agents with pyrazolo[3,4-d]pyrimidine cores were synthesized. Such choice of large core than regular pyrazole was valid as a proper modification. That most of the prepared compounds showed excellent AI activity. In a
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In summary our present work establishes the ability of
2021-03-22
In summary, our present work establishes the ability of the mammalian intestine to function as an environmental sensor able to retain an active metabolic memory for early postnatal nutritional conditions. Epigenetic silencing of the expression of the main cholesterol MK-2206 transporter Npc1l1 conce
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br Concluding remarks Some of the clinical trials
2021-03-22
Concluding remarks Some of the clinical trials of putative neutral competitive ERAs have been less successful than anticipated 6, 8, 11. This might be because of underestimation of the complexity of the molecular pharmacology of ETA. To resolve this, it will be necessary to define the signaling
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br Clinical studies br Practical implications for young wome
2021-03-22
Clinical studies Practical implications for young women Conclusion Research on the oncogenic mechanism of hormones has advanced dramatically in the latter years. The finding that progestogens are more powerful determinants of risk than estrogens in breast cancer has been added to advances i
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br Funding This work was supported by the
2021-03-22
Funding This work was supported by the National Natural Science Foundation of China (grant number 81671411); Beijing Natural Science Foundation (grant number 7162062); Beijing Nova Program Interdisciplinary Cooperation Projects (grant number Z161100004916045); Beijing Municipality Health Technol
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It has previously been shown that human melanocytes are resp
2021-03-22
It has previously been shown that human melanocytes are responsive to a multiplicity of hormonal triggers [10], particularly to pituitary or ovarian hormones [11]. Studies concerning the effects of Pyroxamide on human melanocytes led to inconsistent data [12], [13]. Im et al. [14] reported that the
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Sulbactam The prospects of the use
2021-03-22
The prospects of the use of this novel approach for the selective local thermo-activation of enzymes include biomedical and biotechnological applications. As NPs could be engineered to gain access to Sulbactam through the endosomal compartment [47] or through non-endocytotic pathways [48], [49], [5
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br Materials and methods br Results br
2021-03-22
Materials and methods Results Discussion Fluoride has multiple effects that contribute to caries prevention. S. mutans is 20- to 40-fold more sensitive to NaF than Lactobacillus casei and seven-fold more sensitive than some species of Actinomyces[10]. There are some specific metabolic effec
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Despite the weak and transient nature of
2021-03-22
Despite the weak and transient nature of E2–E3 interactions, this binding is required for the transfer of ubiquitin to the substrate. The low affinity characteristics of this interaction may be due to the fact that E2s use the same surface to interact with E1s and E3s, and hence while binding to an
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naphthalimide a well known DNA intercalator has been extensi
2021-03-22
1,8-naphthalimide, a well-known DNA intercalator, has been extensively investigated in the development of antitumor agents [10]. Some of the naphthalimide derivatives, such as amonafide, elinafide and bisnafide (Fig. 1), have entered into phase II clinical trials stage [10]b), [11]. Among them, elin
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br Conclusions In conclusion we identified
2021-03-22
Conclusions In conclusion, we identified and overexpressed DGAT2 in fast growing, oleaginous N. oceanica for the first time. The engineered N. oceanica overexpressing DGAT2 resulted in enhanced neutral lipid accumulation and altered fatty casein kinase 2 composition. Altogether, our findings dem
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Edaravone The identification of CRF receptor subtypes has le
2021-03-22
The identification of CRF Edaravone subtypes has led to a number of studies addressing its functional properties. This paper examines the evidence for CRF1 and CRF2 mediation of fear and anxiety. Recent reviews discussing specific CRF receptor functions associated with other conditions including ea
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