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GSK has also been used
2022-04-29
GSK-189254 has also been used as PET radiotracer (in the form of [11C]-GSK-189254, also used as [11C]-AZ12807110 by Jucaite et al. (Jucaite et al., 2013)) to assess H3R occupancy (Ashworth et al., 2010), and is currently used in an image-based phase I clinical trial study for investigating GSK-23951
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br Conflict of interest br Introduction Endometriosis
2022-04-29
Conflict of interest Introduction Endometriosis is defined as the presence of endometrial glands and stroma outside the uterus, most often in the pelvic peritoneum and ovaries. This disorder affects an estimated 10% of women in the reproductive age group and is basically an estrogen-dependent
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2188 synthesis Under increased drug pressure more protease v
2022-04-29
Under increased drug pressure, more protease variants with more than one substitution will likely become clinically relevant. The accumulation of additional substitutions can allow RAS variants to emerge that alone are not viable, but in combination can rescue the viral fitness. We previously demons
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br Structural studies of GCAP Recoverin was
2022-04-29
Structural studies of GCAP Recoverin was the first member of this subfamily of Ca2+-binding L002 to be investigated by structural methods [27], [54], [55], [56], [57], [58]. These proteins have four EF-hands arranged in pairs that give rise to amino- and carboxyl-terminal domains. The crystal st
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Annexin A ANXA a member
2022-04-29
Annexin A7 (ANXA7), a member of annexin superfamily, is a Ca2+- and phospholipid-binding protein and possesses GTPase activity [5,6]. The ANXA7 gene is located on human chromosome 10q21, where multiple potential tumor suppressor genes exist. Homozygous ANXA7 (−/−) knockout mice showed a lethal pheno
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Introduction CD T cell recovery after initiation of combinat
2022-04-26
Introduction CD4+ T cell recovery after initiation of combination antiretroviral therapy (cART) is essential for restoring immune function in HIV-positive individuals [1]. However, CD4 recovery is variable and is affected by factors such as biological sex [2], [3], race [4], BMI [5], geographic reg
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The dramatic increase in the
2022-04-26
The dramatic increase in the development of EAAT inhibitors and substrates over the last several years can likely be attributed to a number of experimental advances. Firstly, the isolation of the individual EAAT clones allowed each subtype to be selectively examined in well-characterized expression
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br Introduction The alternative splicing of pre mRNA is esse
2022-04-25
Introduction The alternative splicing of pre-mRNA is essential for generating multiple matured mRNAs from a single gene by selectively removing introns. Neural Phenformin show many examples of regulated alternative splicing events, which produce structural changes in proteins important for the de
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br Introduction Glucokinase GCK hexokinase IV is a monomeric
2022-04-25
Introduction Glucokinase (GCK, hexokinase IV) is a monomeric enzyme that catalyzes the ATP-dependent conversion of glucose to glucose 6-phosphate, the first and rate-limiting step of glycolysis in the liver and pancreas [1,2]. GCK was first discovered in the early 1960's, and shortly thereafter i
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Although in in vitro analyses GANT sensitized Daoy cells
2022-04-25
Although in in vitro analyses GANT61 sensitized Daoy Tideglusib to RITA treatment, this was not fully reflected in the in vivo xenograft studies in nude mice, as the combinatorial treatment elicited a comparable reduction of tumor growth. However, the dual drug administration reduced within-group va
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br Materials and methods br Results br Discussion Ghrelin
2022-04-25
Materials and methods Results Discussion Ghrelin is reported to regulate a number of processes related to cancer progression including tumor cell proliferation, apoptosis and metastasis [3,7,[15], [16], [17], [18], [19], [20], [21], [22]]. In the present study, we examined the potential eff
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br Presenilins and Wnt catenin
2022-04-25
Presenilins and Wnt/β-catenin signalling Several groups have provided substantial data indicating that PS1 acts as a negative modulator of the transcriptional activity of the β-catenin/Tcf-4 complex (Fig. 4) [120], [121], [122]. β-Catenin is a multifunctional protein that was first described as a
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In order to address the Cyp inhibition
2022-04-25
In order to address the Cyp inhibition issue, we tested the possibility of further changes in the heterocycle combined with reducing the electron density in the ring system by swapping the central aniline nitrogen atom for a ketone. details the synthesis of these analogs, which started with 7-bromo
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NCSs are helical proteins containing four EF hand
2022-04-22
NCSs are α-helical proteins containing four EF-hand motifs with EF1 being incapable of Ca-binding throughout the family (atomic-resolution structure was firstly resolved for recoverin [5]; for review on NCS structure, see [6]). Some of the NCS proteins (i.e. recoverin and KChIP3) have two while oth
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The Rab to Rab switch on endosomes co occurs
2022-04-22
The Rab5 to Rab7 switch on endosomes co-occurs with the release of the Rab5 GEF Rabex5 from endosomes, which prevents further Rab5 activation [5]. In addition, the Rab5 GAP is recruited to inactivate remaining Rab5 [67]. Recent data suggest that another GAP, TBC1D5, which binds the retromer complex,
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