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Thrilled by these promising results our
2021-12-22
Thrilled by these promising results, our quest for discovering new PPAR-γ/FFAR1 co-agonists was directed towards exploring the other two new scaffolds. So, in this proposed manuscript, we will describe our efforts regarding the synthesis, biological evaluation and molecular docking studies of the be
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br Results br Discussion Our studies highlight MUFAs as key
2021-12-22
Results Discussion Our studies highlight MUFAs as key lipid modulators of both non-apoptotic and apoptotic cell death. Recent studies show that a more mesenchymal phenotype, de-differentiation, and acquired resistance to targeted inhibitors, can all promote a ferroptosis-sensitive cell state (
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Focal adhesion kinase Fakir et al also known
2021-12-21
Focal adhesion kinase (Fakir et al., 2006), also known as non-receptor tyrosine kinase (PTK2), is a 125-kDa protein that regulates cell migration, adhesion, proliferation, and survival (Tavora et al., 2014; Yang et al., 2016; Tian et al., 2017). Many studies have observed FAK overexpression and/or h
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br Mechanisms of HDAC inhibition dependent
2021-12-21
Mechanisms of HDAC inhibition-dependent cardioprotection Multiple preclinical studies have demonstrated potent cardioprotective benefits of HDAC inhibition in murine models of myocardial stress, including I/R [19,25,29,30]. TSA reduces myocardial infarct size by up to 50% [19,25]. In addition, tr
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For the study described herein analogues
2021-12-21
For the study described herein, analogues of CID1792197 (2) were selected for exploration. There are a variety of reasons for this decision. First, the synthetic approach, described hereafter, is modular in nature to rapidly enable the independent modification of either end of the molecule. Second,
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T L cells can be induced
2021-12-21
3T3-L1 cells can be induced to differentiate into adipocytes by the appropriate hormonal treatment and they offer a useful in vitro model system for adipogenesis. GPR120 mRNA was detected in differentiated mature adipocytes but not in confluent preadipocytes (Fig. 3A). The level of GPR120 mRNA incre
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Milligan et al demonstrated the important role of TNF
2021-12-21
Milligan et al. [31] demonstrated the important role of TNF-α, IL-6 and IL-1β in the development of mechanical hyperalgesia induced by intrathecal injection of gp120. Because of this work, we decide to produce and purify gp120 to develop biological systems to study pain and behavior in rodents. Intr
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LbGlcK and the HsHxKIV d glucose complex PDB entry IDH
2021-12-21
LbGlcK and the HsHxKIV-d-glucose complex (PDB entry 3IDH) [17] were superimposed from individual subunits. The active site regions revealed the key AZ 10417808 binding residues to be present for LbGlcK; also, the superposition showed that HsHxKIV had residues that were absent in LbGlcK, such as K16
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Growth hormone secretagogue receptor GHSR is a member of G
2021-12-21
Growth hormone secretagogue receptor (GHSR) is a member of G-protein-coupled receptor family [3]. GHSR is predominantly expressed in human pituitary, rhypothalamus and hippocampus [4]. GHSR is also expressed in peripheral tissues including lungs, liver, kidney, and adrenal gland. In cardiovascular s
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Following an endoproteolytic cleavage of
2021-12-21
Following an endoproteolytic cleavage of C99, γ-secretase trims the remaining fragment Aβ49 or Aβ48 in successive, mostly three-residue steps. Aβ49 typically gives rise to Aβ46, Aβ43, and Aβ40; whereas Aβ48 usually yields Aβ45 and Aβ42 [59]. The physical basis for this characteristic cleavage patter
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The chemical structure of BAs consists
2021-12-21
The chemical structure of BAs consists of a steroid nucleus with an acidic side chain. They are amphipatic molecules characterized by a hydrophilic α-face and a hydrophobic β-face. The hydrophobic pocket of the FXR LBD interacts with BAs largely through the β-face. The α-face contains several hydrox
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br Acknowledgments This study was supported by a Conquer
2021-12-21
Acknowledgments This study was supported by a Conquer Cancer Foundation (American Society for Clinical Oncology) Drug Development Research Professorship Grant (AAA). Introduction Gastric cancer (GC) is one of difficult cancers to treat in terms of its poor prognosis and limited applicability
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dacomitinib The normal function of the FBPase enzyme is to
2021-12-21
The normal function of the FBPase enzyme is to catalyze the hydrolysis of F1,6BP to F6P. This activity is induced by diabetes and starvation and is increased in diabetic rats. The level of FBPase can be normalized by insulin, however, similar information is not available from diabetic patients. FBPa
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Genome wide binding and transcriptome
2021-12-20
Genome-wide binding and transcriptome analyses demonstrate that Fbxl10 directly binds the Areg, Mdk, Lmnb1, Thbs1, Mgp and Cxcl12 locus and thereby might influences the expression of these migration associated genes. The expression of epidermal growth factor (EGF)-like molecule Amphiregulin (Areg)
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GPR shares a amino acid sequence identity
2021-12-20
GPR81 shares a 52% amino ACP-196 sequence identity in humans to GPR109A [1], [2], [3]. In addition, GPR81 is localized more specifically to the adipose tissue [3]. In 2008, lactate was discovered to be the endogenous ligand for GPR81 [9], [10]. Plasma lactate levels reach concentrations capable of
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