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A phase I clinical trial has been completed for
2022-01-18

A phase I clinical trial has been completed for assessing CEP-26401 in cognitive impairment in healthy individuals without disclosing any results (NCT01903824). Although CEP-26401 is under clinical trial study, several projects are in progress for synthesizing novel irdabisant analogs in order to im
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Canine ANGPTL7 / Angiopoietin-like 7 Protein (Fc Tag) br Di
2022-01-18

Direct effect of HDACs on contractile function by deacetylating cytoskeletal and contractile proteins Role of HDACs in electropathology by transcriptional reprogramming Next to deacetylation of α-tubulin by HDAC6 in experimental and human AF, there is also evidence for transcriptional reprogra
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Acknowledgements We appreciated the contributions of Ana
2022-01-18

Acknowledgements We appreciated the contributions of Ana Carolina Galha, Selma XSL Pinheiro and Islene Azevedo for technical assistances. In addition, we wish to thank Adilson José de Almeida (in memoriam), Moyra M Portilho, Vanessa A Marques and Letícia P Scalioni, for data analysis during the set
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Currently the computational chemical biology has been applie
2022-01-18

Currently, the computational chemical biology has been applied in hepatitis B antiviral drug discovery research [18]. Tan et al. explored oxime ethers as HBV inhibitors by docking and screening [19]. Allen et al. clarified the resistance of HBV to the nucleoside drug lamivudine [20]. The results sug
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The involvement of prostaglandins on the effects
2022-01-18

The involvement of prostaglandins on the effects induced by 1-nitro-2-phenylethane is similarly unlikely because vasorelaxation was not changed by indomethacin [20]. The inhibition of adenylyl cyclase with MDL-12330A [21] or cAMP-dependent protein kinase A with KT-5720 [22] also did not interfere wi
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The identity of organelles is defined by a particular
2022-01-18

The identity of organelles is defined by a particular set of molecules present on their surface. Most organelles in the endomembrane system (i.e., endoplasmic reticulum, Golgi apparatus, endosomes, and lysosomes) carry Rab GTPases (hereafter referred to as Rabs), which serve as binding platforms for
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Various inhibitors have been developed to target molecules
2022-01-18

Various inhibitors have been developed to target molecules present in these pathways. They include both man-made monoclonal phospholipase c inhibitor as well as small molecule membrane permeable inhibitors that often target kinases or phosphatases [5], [338], [348], [364]. In summary, these pathway
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The opposite modulation observed for
2022-01-18

The opposite modulation observed for circulating LPI levels and WAT GPR55 NECA by nutritional status suggests that increased levels of LPI may down-regulate the expression of its receptor in WAT, whereas in conditions of low serum LPI levels, the expression of GPR55 is stimulated. However, during ge
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AT-101 australia Screening of the compounds allowed for
2022-01-18

Screening of the compounds allowed for a number of interesting SAR observations. First of all, pyridyl analogue demonstrated that a pyridine ring would be beneficial for both log as well as increasing the potency (entry 2 versus entry 1). Electron-poor aryl groups next to the oxadiazolone were detri
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br Materials and methods br Results br Discussion
2022-01-18

Materials and methods Results Discussion According to the literature, zaprinast is a high-affinity agonist of GPR35 (Berlinguer-Palmini et al., 2013, Divorty et al., 2015, Taniguchi et al., 2006, Zhao et al., 2010). GPR35 740 Y-P has been identified within discrete regions of the nervous s
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In recent years several DPP IV inhibitors have
2022-01-18

In recent years, several DPP-IV inhibitors have already been approved, such as sitagliptin, vildagliptin, saxagliptin, tenegliptin, alogliptin and linagliptin, etc. Among them, linagliptin (1, Fig. 1) is a non-peptide mimetic PHA 543613 hydrochloride receptor with a unique xanthine scaffold develop
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br Glucose metabolism and diet Glucokinase
2022-01-18

Glucose metabolism and diet Glucokinase is essential for sensing blood glucose levels, thus controls metabolism (Iynedjian, 1993, Iynedjian, 2009, Postic et al., 2001, Agius, 2008). Loss of glucokinase activity in humans and mice leads to diabetes (Printz et al., 1993b, Postic et al., 2001, Agius
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In the last years a plethora of
2022-01-18

In the last years, a plethora of studies overstepped the classic concept of the ENS as purely modulator of GI secretion and motility, focusing on its potential as source of substances acting on immune cells and consequently involved in the control of local inflammatory events, as in the Inflammatory
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However the clinical development of was terminated in
2022-01-18

However, the clinical development of was terminated in 2013 due to the concerns over liver toxicity, raising important questions regarding the long-term safety and viability of targeting GPR40 and, more specifically, about our understanding of the pharmacobiology and signaling spectrum of this recep
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br Conclusion In conclusion rats
2022-01-18

Conclusion In conclusion, rats in this model of HELLP syndrome demonstrated increased placental and circulating FasL and increased placental Fas when compared to NP rats. Administration of an ETA receptor antagonist to HELLP rats tended to decrease circulating FasL and placental Fas, while not af
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