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br Structure of USP Schematic representation of the
2021-01-04

Structure of USP7 Schematic representation of the USP7 domain architecture is shown in Fig. 3B. USP7 is a 135 kDa protein that consists of seven domains, including the N-terminal TRAF-like (Tumor necrosis factor Receptor–Associated Factor) domain, followed by the catalytic core domain and the fiv
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It has previously been established that
2021-01-04

It has previously been established that DDRs play an important role in collagen regulation in at least two distinct ways: (1) activation of DDRs by collagen results in up-regulation of the matrix metalloproteinases, which results in cleavage and degradation of the ECM20., 21., [22] and (2) daunorubi
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Our knowledge of DDR induced signaling pathways
2021-01-04

Our knowledge of DDR-induced signaling pathways is still fragmentary. In particular, we do not know which signaling effectors interact with the phosphorylated receptors and how different effectors are linked to the control of specific cellular functions. The DDRs are at the interface between RTKs an
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At the therapeutic level the logical approach to
2021-01-04

At the therapeutic level, the logical approach to address the cooperation between FGFR4 and EGFR was the combined inhibition of both receptors. To explore the potential efficacy and specificity of this approach, we tested the effect of FGFR and EGFR inhibitors in monotherapy or in combination in syn
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Approximately of the etamicastat dose was recovered
2020-12-31

Approximately 50% of the etamicastat dose was recovered in urine, 30% in the form of etamicastat and 20% in the form of BIA 5-961. These data agree with those from a study with [14C]-labeled etamicastat in healthy subjects, which showed that approximately 95% of the administered radioactivity had be
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CYP A is involved in the metabolism of
2020-12-31

CYP3A is involved in the metabolism of approximately 50% of all drugs that are currently prescribed to patients [1], [15], [16]. Marked interindividual variabilitity of the catalytic function for metabolizing CYP3A substrates has been demonstrated with variability exceeding 20-fold [1]. Levonorgestr
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A comparison between tinnitus and controls subjects
2020-12-31

A comparison between tinnitus and controls subjects showed increased activity in the left AUD and PHC for the gamma frequency band. The link between gamma band activity in the AUD and tinnitus has been identified using both EEG (van der Loo et al., 2009) and MEG (Weisz et al., 2005, 2007). This is s
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The present study sought to determine if
2020-12-31

The present study sought to determine if chlorodifluoroacetophenones, such as 3 and 4, were amenable to a radiolabelling methodology to generate potential 18F imaging agents with high cholinesterase affinity. A number of procedures have been reported for the synthesis of trifluoromethyl ketones, inc
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Kshirsagar et al previously reported an
2020-12-31

Kshirsagar et al. previously reported an association between CHK2thr68 expression and the presence of the chromatin remodeling factor Rsf-1 in solid HGSC specimens [22]. Rsf-1 expression was previously analyzed in our effusion series and was found to be related to poor survival [23]. Analysis of the
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Our finding that activating DDR variants are a
2020-12-30

Our finding that activating DDR2 variants are a cause of this disease suggested that the ABL inhibitor dasatinib, a leukemia drug that also inhibits DDR2, could be used for treatment of affected individuals.10, 11 To examine the effect of dasatinib on p.Leu610Pro- and p.Tyr740Cys-induced autophospho
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Introduction Myclobutanil MCL RS chlorophenyl H triazol ylme
2020-12-30

Introduction Myclobutanil (MCL), (RS)-2-(4-chlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)hexanenitrile (Fig. 1), is a broad-spectrum systemic triazole fungicide with protective, eradicative, and curative action (University of Hertfordshire, 2018). It is employed to control pests such as powdery mild
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The structure of the HOIP RBR LDD module bound to
2020-12-30

The structure of the HOIP RBR–LDD module bound to UbcH5~Ub reveals insights into an activated HOIP component [47]. Contacts between the E2~Ub and the non-cognate RBR module in the crystal suggest how a structure in which the active sites of the E2 and the E3 are in close proximity might look. In th
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br A brief history of RBR E s RBR
2020-12-30

A brief history of RBR E3s RBR E3s were originally defined based on sequence alignments that predicted a tripartite motif of three zinc (Zn)-binding domains: two RING domains (RING1 and RING2) connected via an in-between-RING (IBR) domain [28], [29]. The prediction together with initial observati
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Given the link between E s autoimmunity and antitumor immuni
2020-12-30

Given the link between E3s, autoimmunity, and antitumor immunity, it tankyrase is reasonable to assume that, similar to other ICBs, IRAEs may limit the clinical use of E3-targeting therapies – further stressing the need to better understand the underlying mechanisms of these unwanted effects. Despi
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Although the implication of DA and glutamate signaling cross
2020-12-30

Although the implication of DA and glutamate signaling crosstalk in drug-evoked neuronal adaptations is well acknowledged, targeting the cognate receptors to alleviate symptoms is associated with a loss of efficacy over time and the appearance of severe sides effects, likely due to the involvement o
 
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