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EVP4593 Recently AFF was used to convert an FN based binder
2024-06-21
Recently, AFF was used to convert an FN3-based binder specific to the Src homology 2 (SH2) domain of cAbl kinase into an allosterically regulated, intermolecular fluorescent switch (Figure 2D). Binding to cAbl kinase co-operatively stabilized the assembly of the FN3-based binder from two partial fra
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The reproducibility of the IC measurements in
2024-06-21
The reproducibility of the IC50 measurements in the Pf-dhfr yeast was far better than comparable measurements in P. falciparum in vitro [1]. This is probably due to the extremely low level of folate and para-aminobenzoic Cyclo(RGDyK) mg in the yeast growth medium. This is in contrast to culture of
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Introduction Plant pathogenic fungi are major pathogens in a
2024-06-21
Introduction Plant pathogenic fungi are major pathogens in agricultural diseases and the cause of large crop losses worldwide. There are many kinds of plant pathogenic fungi, with various modes of action. For example, Botrytis cinerea (B. cinerea) is the disease pathogen in the economically importa
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Anti angiogenic activity of natural products in ocular
2024-06-21
Anti-angiogenic activity of natural products in ocular neovascularization A number of molecules, obtained from the natural source, have been evaluated for ocular neovascularization [14], [15]. As these compounds exhibit antioxidant effects, these were also tried for their therapeutic efficacy in in
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br Animal models of NAFLD Human research has greatly shaped
2024-06-20
Animal models of NAFLD Human research has greatly shaped our understanding of non-alcoholic fatty liver disease, but several limitations exist in studying the disease processes in humans, such as variations in environmental exposure, pre-existing genetic risk factors, racial and ethnic difference
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An ALK rearrangement was found in all
2024-06-20
An ALK rearrangement was found in all the analyzable ‘truly positive’ IHC+/FISH+ samples, and the proportion of the various transcripts was in accordance with the literature [[26], [46], [47], [48]]. In these samples, the RNA-seq technique was therefore 100% sensitive and specific. Additional non-ta
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Cancers that responded to immune
2024-06-20
Cancers that responded to immune checkpoint inhibitors were shown to present a type I interferon (IFN) signature in the TME 33, 34. Type I IFNs positively regulate the expression of tumor antigens and their crosspresentation by DCs to tumoricidal CTLs. Furthermore, CD8+ T cell develops full effector
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As we previously observed in the NSFT
2024-06-20
As we previously observed in the NSFT (Fukumoto et al., 2014), the effect of LY341495 in the FST was also inhibited by a 5-HT1A receptor antagonist, indicating the role of the 5-HT1A receptor in the actions of LY341495. Among the 5-HT1A receptors, which exist both presynaptically and postsynapticall
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The activation of the A BR subtype triggers
2024-06-20
The activation of the A2BR subtype triggers different intracellular metabolic pathways, often linked to the activation of adenylyl cyclase and increased levels of intracellular cAMP (Lynge et al., 2003, Bernareggi et al., 2015). The nAChR-channel Exendin-3 (9-39) amide receptor mediated by the cAMP
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br Discussion One binding site MB Fig is located
2024-06-20
Discussion One binding site, MB327-1 (Fig. 4) is located in the extracellular domain between the γ and α subunits. MB327 adopts an extended conformation in the MB327-1 site and is oriented parallel to the channel. The second putative binding site, MB327-2 (Fig. 4) is situated deep inside the chan
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MC1568 It is already established in the
2024-06-20
It is already established in the literature that products synthesized by 5-LO, such as lipoxin A4, can activate PPARγ in a setting of experimental stroke [43]. Interestingly, experiments using 5-LO knockout mice in an endotoxemia model to mimic septic conditions, demonstrated reduced multiple organ
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Direct inhibition of LO activity by BRP is clearly evident
2024-06-20
Direct inhibition of 5-LO activity by BRP-187 is clearly evident in cell-free assays using PMNL homogenates and isolated human recombinant 5-LO as enzyme source. In such assays, pure FLAP inhibitors like MK886 are inactive [9], [10], [29], [44]. Wash-out experiments and studies using the nonionic de
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Numerous studies have reported high glutamate levels in the
2024-06-20
Numerous studies have reported high glutamate levels in the brains of patients with depression, indicating that the glutamate system plays a crucial role in depression (Sanacora et al., 2004; Kendell et al., 2005; Hashimoto et al., 2007). Furthermore, several clinically effective antidepressant drug
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For the NSCLC patients with
2024-06-20
For the NSCLC patients with EGFR-activating mutations, EGFR-TKIs (gefitinib and erlotinib) are effective clinical therapies [21], [22]. However, approximately 10% of patients harboring EGFR-sensitizing mutations exhibit intrinsic resistance, and up to 40% do not attain a major response to treatment
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br Epidemiology br Genetics The dominantly inherited
2024-06-19
Epidemiology Genetics The dominantly inherited PrP cerebral amyloidoses are genetically transmitted with a penetrance of almost 100%. Early linkage analysis studies helped to established the relationship between GSS and mutations in the PRNP gene. PRNP is located on the short arm of chromosome
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