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Until now five muscarinic receptor M genes
2024-10-18

Until now, five muscarinic receptor (M1-5) genes have been cloned, but, M1-3 receptors are functionally recognized in the lungs. Smooth muscle contraction is mainly mediated by M3. M2 may also participate in the contraction via Gi protein which leads to a decrease in cAMP. On the other hand, M2 is l
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Previously we reported that EL
2024-10-18

Previously, we reported that EL-Kras mice-fed diets rich in omega-6 FAs demonstrated increased pancreatic mast cell infiltration [16]. Significantly, increased infiltration of mast cells into the tumor microenvironment correlates with a poor prognosis [15]. Soucek et al.[25] demonstrated that mast c
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Numerous studies have reported high glutamate levels in
2024-10-18

Numerous studies have reported high glutamate levels in the brains of patients with depression, indicating that the glutamate system plays a crucial role in depression (Sanacora et al., 2004; Kendell et al., 2005; Hashimoto et al., 2007). Furthermore, several clinically effective antidepressant drug
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Application of the broad acting HTR antagonist methiothepin
2024-10-18

Application of the broad-acting 5-HTR antagonist methiothepin (Bard et al., 1996, Hoyer et al., 1994, Peroutka, 1990) converted the TBS-induced response of both thalamocortical and intracortical A1 synapses from LTP to LTD, an effect that was mimicked by the selective 5-HT2R antagonist ketanserin (L
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Thirty six of the analogs
2024-10-17

Thirty-six of the analogs synthesized showed ATX inhibition greater than 50% at 10μM with FS-3, twelve of which had improved potency over the lead (Fig. 5). Of these, 22 was sub-micromolar (IC50 670nM). The 3,5-dichlorophenoxy ring of 22 is reminiscent of the 3,5-dichlorophenylthiourea ring in Hoegl
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Consistent with a damaging role for increased LOX
2024-10-17

Consistent with a damaging role for increased 12/15-LOX activity in stroke, systemic administration of the 12/15-LOX inhibitor, LB1, 2 h after permanent focal cerebral ischemia significantly reduced infarct size 24 h after the ischemia, and the treatment group demonstrated improved behavioral and he
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br Conflict of interest statement br Acknowledgments
2024-10-17

Conflict of interest statement Acknowledgments Introduction Cellular responses to genotoxic stress in eukaryotic cells are coordinated by members of the phosphoinositide kinase related protein kinase (PIKK) family. Two members of this family, Ataxia–Telangiectasia mutated (ATM) and ATM and
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br Conflict of interest statement br Funding br Acknowledgme
2024-10-17

Conflict of interest statement Funding Acknowledgments We thank the team at Medical and Collider-Accelerator Departments at BNL and for their support at NSRL. We thank Dr. Janice Pluth and Professor Peter O’Neill for useful discussions related to our work. Introduction The DNA damage re
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The crucial role of AP in establishing and
2024-10-17

The crucial role of AP-1 in establishing and maintaining cell type-specific gene expression programs and cell identity is further apparent during reprogramming of mouse embryo fibroblasts (MEFs) into iPSCs with either Oct4/Sox2/Klf4/cMyc (OSKM ) factors , or chemicals . Using ATAC-seq to profile ch
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Over expression of the inflammatory cytokines MMPs and COX
2024-10-17

Over expression of the inflammatory cytokines, MMPs and COX-2 act as an important inducer of chronic inflammation. COX-2 catalyzes the biosynthesis of prostaglandins (PGs), and induced expression was observed in rna helicase stimulated with pro-inflammatory cytokines or bacterial lipopolysaccharide
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The AT hook motif is
2024-10-17

The AT-hook motif is highly conserved in evolution from bacteria to humans and is found in one or more copies in a large number of other, non-HMGA, proteins, many of which are transcription factors or are involved in chromatin remodeling [8]. For example, AT-hook peptide motifs are essential compone
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Another hypothesis is angiogenesis inhibition Angiogenesis i
2024-10-17

Another hypothesis is angiogenesis inhibition. Angiogenesis is a process that involves the growth, migration and differentiation of endothelial PSB 0777 ammonium salt to form new blood vessels. Angiogenesis favorably influences tumor growth and also influences tumor invasion of vessels, resulting in
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br Materials and methods br Results
2024-10-17

Materials and methods Results and discussion First, we examined whether hypothalamic Akt-mediated signaling pathways are regulated postprandially in chickens. Refeeding significantly (P diltiazem hydrochloride receptor concentrations significantly increased in chicks after 1 h of refeeding (9
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APPL is highly expressed in pancreatic cells
2024-10-16

APPL1 is highly expressed in pancreatic β cells, but its levels are significantly decreased in several mouse models of obesity and diabetes, including HFD-induced obese mice and db/db mice [6], [73], suggesting that the dysregulation of APPL1 may be associated with malfunction of the pancreas in obe
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Encouraged by this observation a systematic SAR
2024-10-16

Encouraged by this observation, a systematic SAR study on the A ring -alkoxy was conducted as summarized in . The A ring methoxy-containing KRCA-0008 was proven an optimal substituent in terms of potency after all and its bigger size derivatives were detrimental in both biochemical and H3122 cellula
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