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br Results and discussion br Conclusions In
2024-04-29

Results and discussion Conclusions In this report we present the synthesis, structure determination, and the in vitro and in vivo evaluation of a series of new quinone analogues aiming to find novel lead structures for the development of 5-LO inhibitors. Our findings support that also the hydr
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Introduction hydroxytryptamine HT is found
2024-04-29

Introduction 5-hydroxytryptamine (5-HT) is found throughout the body and influences smooth muscle activity in various tissues including the intestine, vasculature and urinary M344 (Kim and Camilleri, 2000, Klarskov and Horby-Petersen, 1986, Mohammad-Zadeh et al., 2008). The current classification
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Later the same group designed
2024-04-29

Later, the same group designed and prepared several Δ16-steroidal C17 benzoazoles and pyrazines and evaluated their CYP17 and 5α-reductase inhibitory activities, binding to and transactivation of the AR, as well as their antiproliferative effects against two human PC cell lines (LNCaP and LAPC4) [1
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The consensus amino acid recognition sequence
2024-04-29

The consensus amino Hyper Assembly Cloning recognition sequence for p38α substrates is (Ser/Thr)Pro (Cuadrado and Nebreda, 2010), typically assisted by upstream docking motifs (Remenyi et al, 2005, Sharrocks et al, 2000). P450c17 has 32 Ser and 25 Thr residues, of which only Thr 341 and Ser 427 are
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Materials and methods br Results br Discussion
2024-04-29

Materials and methods Results Discussion ATX plays a significant role in initiating and sustaining tumor metastasis [43]. LPA stimulates cell proliferation, migration and survival by acting on its cognate G-protein-coupled receptors. Aberrant LPA production, receptor RQ-00203078 and signalin
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br Discussion In our current study
2024-04-29

Discussion In our current study, we demonstrated that both the metastatic and recurrent ovarian cancer tissues expressed lower levels of p62 when compared with the patient-matched primary tumor samples. High vomitoxin levels of p62 were associated with long progression-free survival of patients
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br Innate immune mechanisms that confront viral
2024-04-29

Innate immune mechanisms that confront viral infection Autophagy induction by virus sensing Antiviral xenophagy and virophagy The presence of viral particles within autophagosomal structures has been visualized in only rare instances. This is the case for HSV-1 when it is devoided of ICP34.
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Compound was docked into the active site of Aurora
2024-04-29

Compound was docked into the active site of Aurora B kinase using Tripos sybyl-X ver. 2.1.1. The crystal structure of human Aurora B kinase cocrystallized with its potent inhibitor VX-680 was used for the docking analysis (PDB ID: ). The most likely binding conformations were selected based on the
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The class C receptors also share a
2024-04-29

The class C receptors also share a common agonist-binding mode. In all cases, an agonist induces VFT closure by forming intermolecular bonds with surface residues in both the LB1 and LB2 domains (Geng et al., 2013, Geng et al., 2016, Kunishima et al., 2000, Muto et al., 2007, Nuemket et al., 2017, T
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AGI-5198 Several structural classes of ASK inhibitors mostly
2024-04-29

Several structural AGI-5198 of ASK1 inhibitors, mostly from industry but also from academia, have been identified over the last decade. In 2012, Terao et al. (Takeda) reported imidazo[1,2-α]pyridine () as a potent ASK1 inhibitor derived from structure-based drug design. GSK, Merck and Gilead reveale
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The first objective of the present study was
2024-04-29

The first objective of the present study was to investigate the impact of ageing on arginase activity in tissues which exhibit age-related impairments in their function. The second objective was to determine whether l-arginine supplementation modulated the effect of ageing on arginase activity. The
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On the other hand key enzymes also involved in
2024-04-29

On the other hand, key osmi also involved in NO metabolism are nNOS and eNOS. Apparently, during acute ischemia, eNOS activity and NO concentration surge for a short period of time (Schulz et al., 2004) but eventually the expression and activity of the synthase and consequently NO concentration decr
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Mechanistically it was soon realized that in
2024-04-28

Mechanistically, it was soon realized that in undead cells, Dronc promotes the activation of Jun-N-terminal kinase (JNK) signaling as the major inducer of AiP [25], [28] (Fig. 2B,C). However, it has been unknown for a long time how active Dronc promotes JNK signaling. Recently, it was reported that
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br Antibiotic drug discovery approaches Traditionally novel
2024-04-28

Antibiotic drug discovery approaches Traditionally, novel Pregnenolone Carbonitrile were largely discovered by phenotypic screening approaches of various sources of compounds, such as natural products isolated from extracts of soil microbes and semi-synthetic or fully synthetic compound libraries
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br Role of AMPK in inflammation signaling
2024-04-28

Role of AMPK in inflammation signaling Pro-inflammatory cytokines, such as interleukin (IL)-6 and tumor necrosis factor-α (TNF-α), activate Ikβ kinase (IKKβ), which phosphorylates IκBα, triggering the degradation of proteasomal IκB. This liberates active nuclear factor kB (NF-kB) to translocate i
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