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For the TSH receptor signaling at the Golgi trans Golgi
2024-05-15

For the TSH receptor, signaling at the Golgi/trans-Golgi network appears required for both rapid effects of TSH − such as metabolic enzymes depolymerization, which is implicated in thyroglobulin reuptake and, thus, thyroid hormone release − and late ones, such as those on gene transcription. Continu
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TLX may promote survival and prevent
2024-05-15

TLX may promote survival and prevent apoptosis in NB SF1670 [12]. Here, we ask whether the survival-promoting effects of TLX are mediated by Apoptosis Signal-regulating Kinase-1 (ASK1, MAP3K5). ASK1 is a member of the Mitogen-Activated Protein (MAP) kinase family and it preferentially activates the
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Limitations of this study include the use
2024-05-15

Limitations of this study include the use of HL-1 cardiomyocytes, which show different characteristics than primary cardiomyocytes [56]. Furthermore, sustained TAC in Ampkα1-deficient mice did not favorably influence cardiac function [33]. It must be kept in mind that global Ampkα1-deficiency may af
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Most human diseases e g
2024-05-15

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 lack of benefit in terms
2024-05-15

The lack of benefit in terms of overall survival for antiangiogenic treatment was similar when antiangiogenic drug was used both as first and second-line therapy, and both in association with cytotoxic treatment or alone. Noteworthy, a trend for an inferior outcome was observed in the group of patie
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br Introduction The development and plasticity of synapses
2024-05-15

Introduction The development and plasticity of synapses involve the timely recruitment of a plethora of proteins on both pre- and postsynaptic sides through ill-defined mechanisms. At excitatory synapses, two of the major proteins that are dynamically recruited postsynaptically are the Ca2+/calmo
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This chemistry paved way for multi gram synthesis of
2024-05-14

This chemistry paved way for multi-gram synthesis of which was utilized for extensive piperazine benzamide SAR exploration. Depicted in , the two-step operation towards final targets involved standard amide coupling conditions with EDC or HATU followed by Boc deprotection under acidic conditions.
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The synthetic route to M developed by
2024-05-14

The synthetic route to M100907 developed by Rice was utilized, however, the chiral resolution was carried out at an earlier stage to provide the possibility of introducing different substituents onto the piperidinyl group. The conditions for this resolution were different from previously reported.
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In order to get a better understanding of this
2024-05-14

In order to get a better understanding of this synergy, we tested the effect of preliminary incubation of BAY 87-2243 with non-stimulating concentrations of gonadotropins or FSK before subsequent stimulation by FSK or gonadotropins alone, also at sub-stimulating concentrations. We observed that hum
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A selected set of these new
2024-05-14

A selected set of these new derivatives was then used for functional assays at the human A1AR showing, as expected, an antagonist profile with IC50 values at nanomolar level. The same molecules showed also to be efficacious as nanomolar antagonists in a functional assay aimed at analyzing their abil
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Among the enzymes involved in adenosine metabolism
2024-05-14

Among the enzymes involved in adenosine metabolism, adenosine kinase plays an important role in regulating formation and release of endogenous adenosine in cardiomyocytes as well as vascular endothelial cells Decking et al., 1997, Kowaluk et al., 1998, Smolenski et al., 1994. Inhibition of adenosine
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In summary this study reveals that the stability
2024-05-14

In summary, this study reveals that the stability of rapsyn is critically dependent on HSP90β, highlighting a novel function of HSP90β in NMJ formation and maintenance. It also identifies a mechanism in agrin signaling for AChR clustering, i.e., by upregulating the interaction between HSP90β and rap
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angiotensin receptor blockers Several reports of single case
2024-05-14

Several reports of single cases of MG patients treated with Rituximab have claimed a favourable response (Baek et al., 2007, Gajra et al., 2004, Hain et al., 2006, Thakre et al., 2007, Wylam et al., 2003, Zaja et al., 2000). We report our experience with Rituximab in 6 patients with severe MG, 3 pa
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Renal Cell Carcinoma RCC is
2024-05-14

Renal Cell Carcinoma (RCC) is a lethal cancer with bad prognosis due to development of chemoresistance and recurrence of an aggressive tumor with increased tumor-angiogenesis and metastasis [7]. We have found Axl and Gas6 to be differentially presented in RCC subtypes, and Axl to correlate to tumor
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In PMCA Mg favors the conversion E P E P
2024-05-14

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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