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In conclusion our results provide
2021-02-02

In conclusion, our results provide a new mechanistic insight into the signaling pathways mediating TDCIPP-induced apoptosis in cultured neuronal cells. We showed that TDCIPP-induced neuronal cell cytotoxicity and death are mediated via the ER stress-regulated apoptotic pathway, wherein the inductio
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br Molecular modeling study Molecular modeling study
2021-02-02

Molecular modeling study Molecular modeling study was essentially needed to understand and interpret the DHFR inhibitory pattern of this new class of compounds. Computational docking is an algorithm designed to estimate two main terms. The first is to determine the suitable position and the orien
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DPQ br Experimental procedures br Introduction Protein kinas
2021-02-02

Experimental procedures Introduction Protein kinases represent one of the largest enzyme DPQ in the human genome and act as signaling mediators in a variety of cellular processes (Manning et al., 2002). Because many diseases are associated with aberrant protein kinase activity, targeted kinas
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br Conclusion br Conflicts of interest br
2021-02-01

Conclusion Conflicts of interest Acknowledgements This study was financially supported by The Science and Engineering Research Board (SERB), Department of Science & Technology (DST), Government of India under the Fast Track Scheme for Young Scientist to Dr. V. Dhananjayan (No: SB/FT/LS-140/
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Synthetic progestogens also known as synthetic gestagens syn
2021-02-01

Synthetic progestogens (also known as ‘synthetic gestagens’, ‘synthetic progestins’ or simply ‘progestins’) are designed to mimic the effects of progesterone (P4) and are the active pharmaceutical ingredient in many contraceptives and hormone replacement therapies. Since most progestins are derived
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Tibolone is also efficacious on bone in elderly
2021-02-01

Tibolone is also efficacious on bone in elderly women and induces a clear reduction in bone turnover markers [50], [51]. Rymer et al. showed that, after 10 years of treatment with tibolone, the difference in bone mineral density compared with a placebo group was more than 12% for both lumbar spine a
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Introduction Psoriasis is a chronic recurrent and inflammato
2021-02-01

Introduction Psoriasis is a chronic, recurrent and inflammatory skin disease, and it is characterized by erythema, skin hyperplasia, scales, and hyperproliferation of keratinocyte [1]. It is reported that the psoriasis occurrences are about 3% worldwide [2], but the number varies depending on ethni
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Methods br Results br Discussion It is well
2021-02-01

Methods Results Discussion It is well established that CRSwNP is characterized by TH2 inflammation and eosinophilia.22, 27 Yet it is becoming increasingly apparent that B cells might play an important role in the inflammatory response within the sinus tissue of patients with CRSwNP.8, 9 The l
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Although the formation and toxicity of DPC
2021-02-01

Although the formation and toxicity of DPC is theoretically acceptable, it is difficult to evaluate the specific role of DPC and its repair enzyme MGMT in the cytotoxic and mutagenic effects because DPCs are estimated to constitute only 1%–3% of total DNA damage when GSK1070916 are exposed to bis-el
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We elucidated that the ten DGK isozymes have different
2021-02-01

We elucidated that the ten DGK isozymes have different relative 1-MGK and 2-MGK activities vs DGK activity under the same conditions. However, because the octylglucoside-mixed micellar assay was developed for DGK, it is not known whether the DGKs exhibit maximum 1-MGK and 2-MGK activities in this as
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br Results br Discussion br Conclusions
2021-02-01

Results Discussion Conclusions The present study demonstrates that CRF1 receptor-deficiency prolongs whereas CRF2 receptor-deficiency shortens the duration of recognition memory deficits induced by morphine discontinuation, unraveling opposite roles for the two known CRF receptor subtypes i
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In BBR was reported to increase
2021-01-30

In 2004, BBR was reported to increase LDL receptor (LDLR) gene expression by stabilizing LDLR mRNA [4]. Following this report, the same groups conducted additional studies predominantly in HepG2 cells, with similar effects being observed [8], [11], [12], [4]. In addition to LDLR-mediated LDL cholest
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br Conclusions and future perspectives
2021-01-30

Conclusions and future perspectives It is now evident that selective ETA or nonselective endothelin receptor antagonism provides therapeutic potentials against a variety of cardiovascular diseases such as hypertension, PAH, and diabetic microvascular dysfunction (Fig. 1). However, PAH is currentl
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The development of novel approaches to study GPCR
2021-01-30

The development of novel approaches to study GPCR-mediated transactivation in live Quinupristin-Dalfopristin Complex mesylate is important, and this study describes a unique BRET-based quantification of Grb2 recruitment to the EGFR as a direct readout of GPCR-mediated transactivation. We have previ
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br Results and discussion br Conclusion We have constructed
2021-01-30

Results and discussion Conclusion We have constructed a series of potent and greatly selective DPP-4 inhibitors with pyrazolo[1,5-a]pyrimidin-7(4H)-one core surrogates. The modification of the core led us to b2 which has IC50 of 80 nM and > 1000 fold selectivity over DPP-8 and DPP-9. We utiliz
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