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The fact that the BPloopAsn regains its Btx binding with
2023-10-30

The fact that the α1-BPloopAsn141 regains its α-Btx binding with a Kd similar to that of the wild type α1 ECD [18], suggests that the AChBP Cys-loop does not interfere with the correct conformation of the mutant ECD. Data from analogous mutants of the human neuronal α7 subunit ECD showed improved li
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The benzimidazole group seems to be
2023-10-30

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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Aurora A or B selective and pan aurora inhibitors
2023-10-30

Aurora -A or -B selective and pan-aurora inhibitors have demonstrated different preclinical and clinical therapeutic efficacies [2,[19], [20], [21], [22], [23]]. For example, clinical trials for a pan-Aurora inhibitor VX-680 (developed by Vertex) were halted at phase II for toxicity reasons (one cas
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Among the most important Ca regulatory mechanisms
2023-10-30

Among the most important Ca regulatory mechanisms are the Plasma Membrane Calcium ATPase (PMCA) and Sarcoplasmic Reticulum Calcium ATPase (SERCA). These pumps belong to the family of P-ATPases, which share the formation of an acid-stable phosphorylated intermediate as part of their reaction cycle. P
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br Conclusion br Acknowledgement This
2023-10-30

Conclusion Acknowledgement This study was supported by NIH/NINDSR01 NS036812-16. Introduction Stroke is the leading cause of disability and the fifth leading cause of death in the United States (Writing Group et al., 2016). On average, every 4 min a human dies of stroke (Lackland et al., 2
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Our results clearly demonstrate that inhibition of ATM pathw
2023-10-30

Our results clearly demonstrate that inhibition of ATM pathway activation results in resistance to Vγ2Vδ2 T cell-mediated cell death. Therefore, enhancing ATM activation along with Vγ2Vδ2 T cell treatment would promote the cytotoxicity of resistant ovarian cancer cells. To our knowledge, this is the
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Somatostatin analogs also bind to somatostatin receptors It
2023-10-30

Somatostatin analogs also bind to somatostatin receptors. It has been reported that octreotide has a high affinity for hSSTR2, moderate affinity for hSSTR3 and hSSTR5, and does not bind to hSSTR1 or hSSTR4 (Ben-Shlomo and Melmed 2008). Compared to octreotide, pasireotide displays 40-, 30-, and 5-fol
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br Genetic analysis of polarity complexes Model
2023-10-30

Genetic analysis of polarity complexes Model organisms such as Caenorhabditis elegans and Drosophila melanogaster provide useful means of describing basic biological processes. They lend themselves particularly well to addressing some of the questions arising in this field because of their struct
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br Antifungal resistance what is in
2023-10-30

Antifungal resistance, what is in a name? Antifungal resistance is an emerging and hot topic in the field of medical mycology. Microbiological resistance is identified by determining minimal inhibitory concentrations (MICs) in vitro for a given antifungal and interpreting this value according to
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Although little is known about the etiopathogenesis of preec
2023-10-27

Although little is known about the etiopathogenesis of preeclampsia, this syndrome has a major impact on maternal and fetal health worldwide, since it is responsible for 10–15% of maternal deaths [16], [17], preterm births, intrauterine growth restriction (IUGR), and fetal deaths [2]. In developing
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br Introduction Increased renin angiotensin system RAS
2023-10-27

Introduction Increased renin-angiotensin system (RAS) activity and inflammation in cardiovascular-related regions of the central nervous system contribute to the overactivity of neurohumoral systems that promote volume retention, cardiac remodeling and serious cardiac arrhythmias in systolic hear
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In addition unconventional mechanisms of internalization can
2023-10-27

In addition, unconventional mechanisms of internalization cannot be ignored. It is generally believed that the conventional homologous internalization of a GPCR depends on the activation of G proteins, since GRK activation requires the pre-activation of G proteins (Fig. 2). Feng et al. demonstrated
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br Experimental section br Abbreviations PSA
2023-10-27

Experimental section Abbreviations PSA, puromycin–sensitive aminopeptidase; APN, aminopeptidase N; AML, acute myeloid Leukemia; ALL, acute lymphoblastic leukemia; AADR, amino 8-Bromo-cGMP, sodium salt deprivation response; PAN, puromycin aminonucleoside; DCC, dicyclohexyl carbodiimide; NHS, N
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In glaucoma the primary retinal defect
2023-10-27

In glaucoma, the primary retinal defect appears in the GCL, whereas the other retinal layers appear normal (Kendell et al., 1995). In the current work, chronic elevation of IOP induced RGC apoptosis, especially in the GCL, and α2 adrenergic treatment reduced RGC apoptosis. Various studies have repor
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br Concluding remarks Following the disappointing
2023-10-27

Concluding remarks Following the disappointing outcomes of Aβ immunotherapy trials for AD [62], the current prevailing concept is that disease-modifying therapy must be initiated from the presymptomatic stage of the disease because of the presumed incurability of chronic diseases once they become
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