• br Results and discussion br Conclusion A series

  2023-05-15

  

  Results and discussion Conclusion A series of aminobenzothiazole derivatives were investigated as possible Aurora B kinase inhibitors. Bioisosteric replacement of the heterocyclic core of the lead compound was performed regarding the docking analysis. Replacement of the oxygen pak 4 of the bi

• br Author contributions br Conflicts of interest The authors

  2023-05-15

  

  Author contributions Conflicts of interest The authors declare no competing financial interests. Acknowledgement This work was supported by grants from the Deutsche Forschungsgemeinschaft (Sonderforschungsbereich/Transregio 166–Project C1 and grant CA 1014/1-1 to D.C.) and the IZKF Würzbur

• CBiPES hydrochloride synthesis br Introduction Sustained ove

  2023-05-15

  

  Introduction Sustained over-activation of neurohormonal systems is a hallmark in the pathophysiology of cardiac dysfunction following myocardial infarction (MI) and heart failure (HF). Inhibitors of the renin-angiotensin CBiPES hydrochloride synthesis system (RAAS) constitute cornerstones of pha

• A number of studies indicate the

  2023-05-15

  

  A number of studies indicate the involvement of the classical AR or a splice variant that translocate to the membrane, via a palmitoylation mechanism, similar to ERα (Acconcia et al., 2005, Acconcia et al., 2004, Acconcia et al., 2003), since AR equally contains the required nine amino TPEN palmito

• A candidate protein for the regulation of AMPAR transport is

  2023-05-15

  

  A candidate protein for the regulation of AMPAR transport is CaMKII, a Ca2+-dependent kinase with diverse cellular functions. With respect to synaptic transmission, CaMKII is recognized as a key synaptic protein that is required to modify the number of synaptic AMPARs in response to LTP and LTD stim

• azd9291 Polycyclic aromatic hydrocarbons PAHs are abundant e

  2023-05-15

  

  Polycyclic aromatic hydrocarbons (PAHs) are abundant environmental contaminants that are produced by the incomplete combustion of organic matter, combustion engines, residential heating, azd9291 burning, and industrial activities (Gelboin, 1980; Phillips, 1999, Phillips, 2002). Some PAHs have been

• Further evidence for ACh GABA

  2023-05-10

  

  Further evidence for ACh/GABA cotransmission had also been observed in the cortex. Extensive axonal arborization from cholinergic BF neurons exists throughout the cortical layers, allowing direct observation of cholinergic synaptic terminals. One study in the visual cortex of cat examined immunolabe

• br Increased blood ATX and LPA in liver

  2023-05-09

  

  Increased blood ATX and LPA in liver fibrosis Although previous in vitro findings have suggested a link between LPA and liver fibrosis in vivo, whether LPA plays a primary role in the pathogenesis of liver fibrosis has remained uncertain. No phenotypic changes in livers of LPA receptor-deficient

• Having taken a step back from affinity to gain better

  2023-05-09

  

  Having taken a step back from affinity to gain better exposure and solubility, we started work to replace the unstable oxazolinone, and address the selectivity over the hERG channel. Keeping in mind the binding mode of the series from crystal structures, triazole was identified as another mildly aci

• br Experimental section br Competing interests br Author

  2023-05-09

  

  Experimental section Competing interests Author's contributions Acknowledgement This research is partially supported by a seed fund for the Center for Drug Discovery and Translational Research (LS) and a research grant by Fujifilm (VPS and LS). The Sponsors played no roles in study desig

• br ACL Inhibition Lowering Blood LDL C to Reduce ASCVD

  2023-05-09

  

  ACL Inhibition: Lowering Blood LDL-C to Reduce ASCVD Risk Given its strategic position in the lipid biosynthesis pathway, ACL has been considered an attractive target for lipid-lowering even before statins and their effects on cholesterol homeostasis were elucidated (Box 2). Cells carefully maint

• Previous investigations have established that aromatase acti

  2023-05-09

  

  Previous investigations have established that aromatase activity is regulated via two different pathways in a tissue-specific manner. The first is a slower transcription regulatory pathway that involves an alteration in gene transcription and represents what is classically thought of as the way by w

• Autophagy is a self protecting cellular

  2023-05-09

  

  Autophagy is a self-protecting cellular catabolic pathway that degrades and recycles cytoplasmic contents for the maintenance of cellular homeostasis (Shao et al., 2016b). Macrophage autophagy plays an essential role in atherosclerosis by safeguarding sr1 against oxidative stress, reducing apoptosis

• Introduction Heterotrimeric G proteins mediate signal transd

  2023-05-08

  

  Introduction Heterotrimeric Gαβγ proteins mediate signal transduction through seven-transmembrane domain receptors. In response to neurotransmitters or hormones, activated receptors bind GTP via the Gα subunit leading to the dissociation of Gα from the Gβγ dimer. G proteins regulate the levels of s

• Introduction Increasing environmental pollution caused by

  2023-05-06

  

  Introduction Increasing environmental pollution caused by heavy metals, originating mainly from industrial processes and urban activities, as well as the widespread application of pesticides, fertilizers, manure and sewage sludge, has posed a serious problem for safe food production and become a po

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