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The fact that the BPloopAsn regains its Btx binding
2024-12-25
The fact that the α1-BPloopAsn141 regains its α-Btx binding with a Kd similar to that of the wild type α1 ECD [18], suggests that the AChBP Cys-loop does not interfere with the correct conformation of the mutant ECD. Data from analogous mutants of the human neuronal α7 subunit ECD showed improved li
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Several in vivo and in vitro studies have
2024-12-24
Several in vivo and in vitro studies have demonstrated changes in bioactive lipid profiles under hyperglycemic conditions and have linked these changes with increased leukocyte adhesion and vascular dysfunction during diabetes. This input has originated partly from lipidomic studies that showed elev
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The class C receptors also share a
2024-12-24
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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It is now well established that the cumulative exposure
2024-12-24
It is now well established that the cumulative exposure to endogenous estrogens throughout a woman's life, mainly due to her reproductive history, has an impact on the risk of hormone-dependent breast cancer (Lambertini et al., 2016). Prolonged exposure to estrogens in the case of early age at menar
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br Apelin The APJ receptor ligand apelin
2024-12-24
Apelin The APJ receptor ligand apelin firstly in 1998 was segregated from bovine stomach tissue. Human preproapelin gene located on chromosome Xq25–26.1. The apelin preproproteins consist of 77 amino choline fenofibrate residues that are cleaved into biologically active C-terminal fragments of va
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colony stimulating factor 1 receptor Although mature fibrils
2024-12-24
Although mature fibrils formed from Aβ colony stimulating factor 1 receptor have long been thought to be the main neurodegenerative agents in AD, recent evidence suggests that soluble multimers of these pathogenic proteins, referred to here as “oligomers,” may initiate the synaptic and neuronal dys
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First investigation of numerous membered ether linked macroc
2024-12-24
First, investigation of numerous 12-14-membered ether-linked macrocycles revealed that smaller motifs were most lipophilic efficient. Compound (3) (12-membered macrocycle) exhibited good cellular potencies (ALK IC50 = 1.0 nM; ALK-L1196 M IC50 = 20 nM) and the highest LipE (4.4) with picomolar bindin
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Aldose reductase inhibitor Furthermore stress hormones can i
2024-12-24
Furthermore, stress hormones can indirectly induce DNA damage, for example by altering DNA repair and transcriptional regulation of the cell cycle. It has been found that stress hormones induce the up-regulation of checkpoint kinase 1 (Chk1) and checkpoint kinase 2 (Chk2) and proto-oncogene cell div
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While A Rs communicate mainly with the D R
2024-12-24
While A1Rs communicate mainly with the D1R subtype [36], A2AR and D2R interaction occurs mainly in basal ganglia. D2Rs colocalizes with A2ARs in this pd184352 area where they are preferentially localized postsynaptically in the soma and dendrites of GABAergic striatopallidal neurons [69]. This inte
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Children with ADA SCID commonly suffer from a
2024-12-23
Children with ADA-SCID commonly suffer from a variety of opportunistic infections, including viral, fungal, and mycobacterial infections. Due to defects in Xevinapant and IG production, they are also susceptible to infection with encapsulated bacteria such as Haemophilus influenzae, Streptococcus p
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p38 inhibitors br Discussion The clinical course of our pati
2024-12-23
Discussion The clinical course of our patient until May 2012 was rather typical of early onset AChR-MG. Later on, the pattern of the disease was more typical of MuSK-MG, as evidenced by the distribution of myasthenic weakness and the unprovoked exacerbations. The p38 inhibitors of MuSK-MG appears
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The theoretical calculations of ADME parameters molecular we
2024-12-23
The theoretical calculations of ADME parameters (molecular weight (MW), log P, topological polar surface are (tPSA), number of hydrogen donors (nON) and acceptors (nOHNH), and volume) and DLS are presented in along with the violations of Lipinski’s rule. According to these data, all compounds (–) c
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Osteocytes the most abundant cells in an adult skeleton are
2024-12-23
Osteocytes, the most abundant cells in an adult skeleton, are essentially mature osteoblasts that are surrounded by the products they secreted (Noble and Reeve, 2000). Osteocytes serve as mechanosensors that direct bone remodeling and that regulate the activities of osteoblasts and osteoclasts (Bone
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enolase GABAB receptor is associated with brain and behavior
2024-12-23
GABAB receptor is associated with enolase and behavioral diseases, including epilepsy, spasticity, anxiety and neuropathic pain (Bettler et al., 2004, Bowery et al., 2002, Froestl, 2010). Baclofen, a clinical drug and selective GABAB receptor agonist, is used to treat muscle spasticity in patients
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Apelin APJ triggers a variety of cellular
2024-12-23
Apelin/APJ triggers a variety of cellular signaling pathways (Fig. 1). Recent studies from our laboratory showed that apelin-13 induces vascular smooth muscle cell (VSMC) proliferation by the upregulation of Cyclin D1 expression, which is involved in an ERK-dependent activation of Jagged-1/Notch3 si
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