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To investigate the potential link between G and
2025-01-21
To investigate the potential link between Gβγ and MT assembly in vivo, cultured NIH3T3 and PC12 cells were used. The role of Gβγ in MT assembly was demonstrated using nocodazole, a MT depolymerizing drug [14]. We found that Gβγ was preferentially bound to MTs in NIH3T3 and PC12 cells and treatment w
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NLX a k a F
2025-01-21
NLX-112 (a.k.a. F13640 or befiradol), exhibits nanomolar affinity at 5-HT1A receptors, and, in Biotin-PEG in nanoparticle formulation to the 5-HT1A receptor agonists listed above, it presents exceptional selectivity and high efficacy at these receptors (Colpaert et al., 2002, Newman-Tancredi et al.,
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Mechanisms implicated in antinociception by A R agonists in
2025-01-21
Mechanisms implicated in antinociception by A3R agonists in neuropathic pain are summarized in Box 3. Cellular transduction mechanisms for A3Rs include inhibition of cyclic AMP, PKA via Gαi, interactions with PLC/IP3/DAG and signaling via Gαi and Gαq, and interactions with PI3K/MEK/ERK via βγ subuni
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The gene SRD A encodes
2025-01-21
The gene SRD5A2 encodes the 5-α-reductase enzyme, which converts testosterone into dihydrotestosterone. Although dihydrotestosterone levels are considerably lower than testosterone, dihydrotestosterone has a five-fold stronger binding capacity to the androgen receptor and, thereby, a considerably mo
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br Introduction The principal pathways of adrenal
2025-01-21
Introduction The principal pathways of adrenal and gonadal steroidogenesis have been known for over 50 years (reviewed by Miller and Auchus, 2011). Cholesterol is first converted to pregnenolone via three reactions, 20-hydroxylation, 22-hydroxylation and scission of the 20,22 carbon–carbon bond,
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Regarding brain tumors AXL has been implicated
2025-01-21
Regarding Oxidative stress biomarker tumors, AXL has been implicated in gliomagenesis and chemoresistance [39]. Previous investigations found that AXL is constitutively phosphorylated in many glioma cell lines, murine xenograft tumors and primary patient tumor samples [40]. Immunohistochemical analy
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myo inositol benefits br Acknowledgements Authors wish to th
2025-01-21
Acknowledgements Authors wish to thank Sabanci University (Turkey), Tubitak (Cost Eu-Ros, 113Z463), and the University of Turin (Italy) for supporting this work. Beyza Vurusaner is supported by Sabanci University Post-doctoral research scholarship. Introduction Endometriosis is defined as the
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br Funding br Ethics br Conflict of
2025-01-21
Funding Ethics Conflict of interest Acknowledgements Introduction Hepatic fibrosis occurs in response to different etiologies of chronic liver injury, which is mainly accompanied by pathological salvinorin a receptor of excessive extracellular matrix (ECM) of the liver, as the common
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A high throughput screening campaign led to
2025-01-20
A high-throughput screening campaign led to the discovery of the first series of both potent and selective ATR kinase inhibitors by Vertex Pharmaceuticals (Charrier et al., 2011). One of these compounds, VE-821, was shown to be a potent ATP-competitive inhibitor of ATR with minimal cross-reactivity
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Receptor Subtypes and Their Function Critical
2025-01-20
Receptor Subtypes and Their Function – Critical Appraisal Largely unselective ligands of the benzodiazepine binding site, such as diazepam, are known to elicit a wide range of in vivo effects including hypnosis, sedation, anxiolysis, and muscle relaxation. Genetically modified mice were introduced
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Use of antibiotics would be
2025-01-20
Use of mRNA isolation magnetic beads would be expected to alter the maternal microbiome, thereby changing the infant's initial exposure is to the microbial environment, which could potentially lead to an abnormal succession of microbial colonization in the infant. Alterations in early microbial tra
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Akt phosphorylation activator br Material and methods br Res
2025-01-20
Material and methods Results Table 1 shows that in addition to Leu/CysAP and DPPIV, genes for AspAP, ArgAP, MetAP, APM and PSA are expressed in adipocytes. The kinetic parameters of these AP are also shown in Table 1, revealing that APM has the highest Vmax and catalytic efficiency (Kcat/Km),
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br Introduction Nonalcoholic fatty liver disease NAFLD is a
2025-01-20
Introduction Nonalcoholic fatty liver disease (NAFLD) is a clinicopathologic spectrum of liver pathologies associated with excessive accumulation of fat in the liver. This spectrum is continuous but can be graded based on pathological features; in increasing severity, these are: bland steatosis,
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In this study we designed and synthesized two
2025-01-20
In this study, we designed and synthesized two ALK PROTACs (degraders), 5 (MS4077) and 6 (MS4078), by linking ceritinib and pomalidomide [45] through two different linkers. Using human ALCL and NSCLC cells, we characterized both compounds in a battery of assays to demonstrate their effects on reduci
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The aldehyde reductase AKR A and aldose reductase AKR
2025-01-20
The aldehyde reductase (AKR1A1) and aldose reductase (AKR1B1) belong to aldo-ketoreductase (AKR) superfamily catalyzing the reduction of corresponding aldehydes and ketones involved. Both the closely related enzymes AKR1A1 and AKR1B1 have 65% structural similarity and differ only at the active site.