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The structure of LO is divided in
2024-01-29

The structure of 5-LO is divided in two domains, the catalytic C-terminal domain and the N-terminal regulatory C2-like domain (C2ld) [59,60]. The C2ld spans the Rottlerin 1-114 and is responsible for translocation and binding of calcium and membranes [61–63]. The catalytic domain is primarily an α-
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Steroidal CYP inhibitors can further be classified
2024-01-29

Steroidal CYP17 inhibitors can further be classified based on their mode of action, namely as mechanism-based inhibitors and type I and type II competitive inhibitors [129]. Recent studies investigated other biological targets than CYP17, and some new compounds have shown interesting dual activity a
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Since innate immune responses represent the
2024-01-29

Since innate immune responses represent the first defense against incoming infectious microorganisms, they are particularly engaged during the early stages of viral infections. Many innate defense mechanisms rely on the engagement of pattern recognition receptors (PRRs) which are conserved, germ lin
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The transcription factor activator protein AP is
2024-01-29

The transcription factor activator protein-1 (AP-1) is a redox-sensitive transcription factor whose activity is controlled by agents that perturb intracellular thiol concentrations [10,11]. AP-1 is mainly composed of Jun, Fos, and ATF protein dimers [12,13]. AP-1 mediates the regulation of numerous
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br Results Four HT esters butyrate caprylate laurate and ste
2024-01-29

Results Four HT esters (butyrate, caprylate, laurate and stearate esters) were chosen as representative compounds of increasing lipophilicity (Fig. 1). We will refer to them as C4HT, C8HT, C12HT and C18HT, respectively. They have been synthesized, purified and characterized according to our previ
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In addition a substantial knowledge has been
2024-01-29

In addition, a substantial knowledge has been gained about the main properties of AT1R, such as ligand preference, signaling, regulation, and trafficking. However, it is less known how AT1R and other plasma membrane receptors affect each other’s function, and how these crosstalk mechanisms can be ut
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In the present study a
2024-01-29

In the present study, a splice acceptor site mutation (c.1769-1G > C) was identified in AR gene from patients with CAIS. The c.1769-1G > C mutation results in replacement of the normal sequence (CAG/G) with a new sequence (CAC/G) at the splice acceptor site of intron 2. In the splice acceptor site r
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Pyrimethamine synthesis We find that the interaction of NSF
2024-01-29

We find that the interaction of NSF and SNAP is critically involved in NMDAR-induced PICK1 unclustering. The binding of SNAP to NSF increases the ATPase activity of NSF, which is known to be essential for the unbinding of PICK1 from GluR2 (Hanley et al., 2002). Disruption of the association between
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An issue related to research without biomarkers is
2024-01-27

An issue related to research without biomarkers is that many studies will ascertain some but not all biomarker groups in study participants. Because tau PET is relatively new, incomplete biomarker information will occur in studies that use imaging for amyloid and neurodegenerative biomarker characte
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In this study we designed and
2024-01-27

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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br Materials and methods br Results br Discussion
2024-01-27

Materials and methods Results Discussion Knowledge of the molecular basis of an inherited genetic disease is crucial for understanding the disease pathology and, ultimately, for therapeutic design. Several recent reports have stressed the need for physical characterization of disease-associ
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Aberrant or a sustained activation of AhR
2024-01-27

Aberrant or a sustained activation of AhR signaling pathway, triggered by exogenous toxic ligands such as dioxins, PAHs or polychlorinated biphenyls (PCBs), is a well-described biological process engaged during tumor initiation and/or promotion in various tissues (e.g. liver, lung, skin)(reviewed in
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br Introduction Psychostimulant abuse and addiction remain a
2024-01-27

Introduction Psychostimulant abuse and addiction remain a societal problem in the United States. The latest statistics from the National Survey on Drug Use and Health indicate that slightly less than one million people over the age of 12 report having a cocaine use disorder (NSDUH, 2016). Additio
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Bioactive peptides contain amino acids with possible bioacti
2024-01-27

Bioactive peptides contain 2–20 amino acids with possible bioactivities including antihypertensive, antioxidant, antimicrobial, anticancer, and opioid activity [9], [10], [11]. There has been a great interest in antihypertensive peptides for their efficiency in lowering blood pressure. The antihyper
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Additional evidence for a putative
2024-01-27

Additional evidence for a putative role of COXs and 5-LOX in AD derives from pharmacological studies using inhibitors of these enzymes (for review, see Firuzi and Praticò, 2006). In addition to helping delineate the pathobiological mechanisms of AD, these results raise hope for discovering novel the
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