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The benzimidazole group seems to be
2024-03-12
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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Here we show that the co activation
2024-03-12
Here, we show that the co-activation of RTKs and non-RTKs is a common trait in treatment-naïve EGFR-mutation-positive NSCLC Sodium 4-Aminosalicylate and patients, with AXL and CDCP1 being commonly over-expressed. The combination of gefitinib or osimertinib with the Src/FAK/Janus kinase 2 (JAK2) inhi
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Having demonstrated that Gq coupled mGluR a was necessary
2024-03-12
Having demonstrated that Gq-coupled mGluR1a was necessary for estradiol-induced enhancement of CREB phosphorylation, we hypothesized that activation of a separate G-protein signaling pathway could explain the effect of estradiol on L-type calcium channel signaling (Boulware et al., 2005). Indeed, in
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Because R gene is positively regulated by
2024-03-12
Because 5α-R2 gene is positively regulated by T and in the prostate gland (Torres et al., 2003), and our BPA-treated rats showed decreased circulating T and probably intraprostatic androgen levels, it might be responsible for the decrease of 5α-R2 expression. However, in a previous work using castra
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br ROS in AiP and regeneration Tissue wounding and
2024-03-12
ROS in AiP and regeneration Tissue wounding and inflammation are associated with production of ROS, and recent studies show that generation of ROS, especially during the initial stages of wounding and regeneration are essential for an efficient wound healing response. ROS, in particular H2O2 func
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Most human diseases e g cancer diabetes
2024-03-12
Most human diseases (e.g., cancer, diabetes, and neurodegenerative diseases) are complex and multifactorial. Several investigations in the literature focused on new multi-target drug development, which implies active pharmacophores incorporation in one scaffold (Meunier, 2008, Lazar et al., 2004, Te
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The RE compartment has been shown to be critical for
2024-03-12
The RE compartment has been shown to be critical for supplying AMPAR during LTP (Hanley, 2010; Park et al., 2004), but whether they also supply AMPAR for synaptic scaling has been less clear (Gainey et al., 2015; Tan et al., 2015). Interestingly, although an increase in μ3A is necessary for scaling,
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br MHCI peptide editing N
2024-03-12
MHCI peptide editing, N-terminal extensions and the peptide loading complex Conventionally, peptide-MHCI binding is thought to require both amino- and carboxyl-termini for stable interaction (Madden, 1995; Bouvier and Wiley, 1994). Peptides with longer than optimal length (10–13 residues) have be
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In the MT SGL two regularization parameters need to
2024-03-12
In the MT-SGL, two regularization parameters need to be specified: λ1 and λ2. Using recent results on norm regularization (Banerjee et al., 2014), it is possible to express both parameters via a single parameter as follows: and (Meier et al., 2008, Banerjee et al., 2014), where and are computed
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Adiponectin also works on AdipoR inducing extracellular Ca i
2024-03-11
Adiponectin also works on AdipoR1, inducing extracellular Ca2+ influx necessary for activation of Ca2+/calmodulin-dependent protein kinase kinase (CaMKK)β, AMPK (Fig. 1). This step is then followed by activation of SirT1 and increased expression and decreased acetylation of PPARγ coactivator (PGC)-1
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The cellular mechanism underlying the CGS mediated inhibitio
2024-03-11
The cellular mechanism underlying the CGS12066-mediated inhibition of glutamate release from hippocampal nerve terminals through presynaptic 5-HT1B receptors remains to be elucidated. 5-HT1B receptors are coupled to PTX-sensitive G proteins (Gi or Go) that have been shown to inhibit AC activity as w
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The difference in the mean values of serum ADA in
2024-03-11
The difference in the mean values of serum ADA in sputum positive PTB and controls was found to be highly significant (P Discussion Tuberculosis is a major health problem in India, and out of all its forms PTB is the commonest. A definite diagnosis of PTB can be made with the presence of trichosta
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The bovine Ack is called
2024-03-11
The bovine Ack is called Ack2 (bAck2) and has been suggested to act as a clathrin-assembly protein regulated by the small GTPase Cdc42 [17]. bAck2 lacks some of the C-terminal parts when compared to hAck1 and mAck1. Both Ack1 and Ack2 have been demonstrated to interact with sorting nexin 9 (SNX9 or
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The bovine Ack is called
2024-03-11
The bovine Ack is called Ack2 (bAck2) and has been suggested to act as a clathrin-assembly protein regulated by the small GTPase Cdc42 [17]. bAck2 lacks some of the C-terminal parts when compared to hAck1 and mAck1. Both Ack1 and Ack2 have been demonstrated to interact with sorting nexin 9 (SNX9 or
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br Conclusions Triptans are HT
2024-03-11
Conclusions Triptans are 5-HT1B/1D/(1F) receptors agonists and are considered as the gold standard for acute migraine treatment that have been proven effective. Unfortunately, they are contraindicated in patients with cardiovascular diseases due to their vasoconstrictor (side) effects (MaassenVan
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