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The benzimidazole group seems to be a
2023-03-03

The benzimidazole group seems to be a key feature for the excellent anti-tumor activity of galeterone (159), which motivated the synthesis of new steroidal inhibitors containing N-heterocyclic groups structurally related to benzimidazole. Thus, several 1H- and 2H-indazole derivatives of dehydroepian
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XMD17-109 In PMCA Mg favors the conversion
2023-03-03

In PMCA, Mg2+ favors the conversion E1P → E2P [13] and, as in SERCA [11], it accelerates the phosphorylation displacing the E1–E2 equilibrium towards E1. In SERCA, Sørensen et al. [41], proposed that ATP reacts by an associative mechanism mediated by two Mg2+ ions to form an aspartyl-phosphorylated
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Cerebral ischemia occurs following the occlusion
2023-03-03

Cerebral ischemia occurs following the occlusion of a cerebral artery by a thrombus and causes cell swelling due to cytotoxic edema and BBB disruption with vasogenic edema (Loreto and Reggio, 2010, Nakaji et al., 2006, Shibata et al., 2004). Vasogenic edema is directly linked to alteration of the BB
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The physiologic conditions and signaling mechanisms that reg
2023-03-03

The physiologic conditions and signaling mechanisms that regulate apelin secretion and APLNR expression in malignant tissues appear to be multifactorial. Previous studies have shown that hyperplastic and neoplastic cholangiocytes secrete a variety of hormones, peptides, and growth factors that help
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We further conducted stratified analyses to observe changes
2023-03-02

We further conducted stratified analyses to observe changes in enzyme levels across the periods by subgroups. Fig. 1 shows the changes in GPx levels by subgroups of age, sex, and smoking status. In all participants, GPx levels decreased when air pollution levels declined but increased after the Olym
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The binding of TQ to hsALDH changes
2023-03-02

The binding of TQ to hsALDH changes the characteristic nadph oxidase spectrum of the enzyme. Therefore, TQ forms a complex with hsALDH and changes its absorption properties [39]. Ksv and Kb values indicate that the binding of TQ to hsALDH is very strong and of the order of static binding (complex fo
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br Detection and possible treatments for prostate cancer PC
2023-03-02

Detection and possible treatments for prostate cancer PC can be diagnosed, by screening for prostate-specific antigen (PSA) and after diagnosis, treatments may include intense observation, radical prostatectomy, radiation, chemotherapy, hormone therapy or vaccination depending on the type and sta
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br Conclusions br Funding br
2023-03-02

Conclusions Funding Acknowledgements and Disclosures We would like to thank veterinarian Angelina Williams and assistants Justin Courson, Ashutosh Jnawali, Mythri Puella, Santoshi Ramachandran, and Zhihui She for support during dissections. We also thank Drs. Vallabh Das, Deborah Otteson an
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br Acknowledgements This work was supported by the
2023-03-02

Acknowledgements This work was supported by the National Key Technology Research and Development Program (2012BAD19B01) and General Financial Grant from the China Postdoctoral Science Foundation (2015M581754). Introduction Cough is one of the most important defensive reflex brought into actio
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The protective role of HMW HA in inflammatory diseases and
2023-03-02

The protective role of HMW-HA in inflammatory diseases and pulmonary damage led us to investigate whether PM2.5-induced ALI could be attenuated by HMW-HA and the underlying mechanisms. In this study, we used a rat model to evaluate the effect of HMW-HA on pulmonary histology, lung inflammation, oxid
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br Results br Discussion Evaluation of antimicrobial usage i
2023-03-01

Results Discussion Evaluation of antimicrobial usage is standardized using the DDD as a recommended strategy for comparison with similar hospitals [13]. The use of risk adjustment is needed to overcome the challenge of benchmarking. Two patient characteristics are associated with clinical outc
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ERAP has been crystallized in two different conformations wh
2023-03-01

ERAP1 has been crystallized in two different conformations, wherein the C-terminal domain IV is either closely interacting with domains I/II and enclosing the active site (termed ‘closed’), or is rotated away in a hinge motion which exposes the active site (‘open’). This large motion correlates with
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Comparatively cell based assays appear to be the
2023-03-01

Comparatively, cell-based assays appear to be the most sensitive method to detect patient autoantibodies directed at neurotransmitter receptors. Leite et al. demonstrated that many α-BTX RIA seronegative myasthenic patients do have autoantibodies against the AChR when a highly sensitive immunofluore
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In vitro studies with soman inhibited non aged AChE revealed
2023-03-01

In vitro studies with soman-inhibited, non-aged AChE revealed a species dependent reactivating potency of HI-6 and MMB-4. With guinea pig AChE second order reactivation rate constants of 0.051 and 0.038mM−1min−1 were determined for HI-6 and MMB-4, respectively (Luo et al., 2007). Corresponding value
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In conclusion we have produced some highly potent
2023-03-01

In conclusion, we have produced some highly potent inhibitors of P450 in comparison to the standard EG00229 KTZ. Also, due to the limited specificity of these compounds against lyase in comparison to the 17α-OHase component, these compounds would be expected to have a major impact on corticosteroid
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