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Among all the compounds the novel L derivative d
2024-08-21
Among all the compounds, the novel L-748,337 derivative (23d) showed the potent human β3-AR antagonist activity and high lipolysis inhibitory activity in vitro. The Erteberel synthesis 23d displayed 23-fold more potent β3-AR antagonist activity (EC50 = 0.5117 nM) than that of L-748,337 (EC50 = 11.91
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Diabetes or inflammation is associated with up regulation of
2024-08-21
Diabetes or inflammation is associated with up-regulation of A2AAR (Pang et al., 2010). High levels of A2AARs are found in macrophages and microglial cells that are poised, on activation, to abrogate the immune response (Trincavelli et al., 2008). In addition, hyperglycemia is associated with increa
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br ACK inhibitors Since ACK activation is correlated with po
2024-08-21
ACK1 inhibitors Since ACK1 activation is correlated with poor prognosis in various cancers, strong efforts are being directed by multiple groups towards developing highly potent and specific small molecule inhibitors targeting the ACK1 kinase. At least eight small molecule kinase inhibitors have
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Fig A shows a schematic
2024-08-21
Fig. 2A shows a schematic representation of histological results according to the Franklin and Paxinos Mouse Brain Atlas (2001). The black circles represent the sites of drug infusion that were on-target within the amygdala. Gray circles represent the animals that had infusion locations outside the
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br Studies in zebrafish vascular and
2024-08-21
Studies in zebrafish: vascular and neural development and the regulation of left–right asymmetry Zebrafish embryos represent an excellent model system to examine vertebrate vascular development. Major advantages of the zebrafish system include its genetic tractability, small size, external fertil
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Fig summarizes the oxidative metabolism of arachidonic
2024-08-21
Fig. 1 summarizes the oxidative metabolism of arachidonic p-Cresyl sulfate by lipoxygenases cyclooxygenases and cytochrome P450. Lipoxygenases in humans are expressed in a tissue-specific fashion: 5-LOX is mainly expressed in leukocytes, 12-LOX in platelets, and 15-LOX-1 in reticulocytes, eosinoph
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br Conflicts of interest br Financial support This work was
2024-08-20
Conflicts of interest Financial support This work was supported by grants from the Fondazione Cariplo [Grant number 2011-0463] (Carini); and by Funds for Original Research of the Università del Piemonte Orientale (2016, Project: Carini-Boldorini). The sponsors had no involvement in study desig
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In previous years evidence emerged that inferred
2024-08-20
In previous years, evidence emerged that inferred secondary metabolites in plants might exhibit a potential arginase inhibition [36]. In a recent study, Pham and co-workers showed the inhibitory activity of chlorogenic 7915 (7) and piceatannol (8) (Fig. 3b) on mammalian arginase with IC50s of 10.6
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br The role of apelin in hepatic diseases The
2024-08-20
The role of apelin in hepatic diseases The involvement of the apelin/APJ system in liver physiology and pathology has been proven in numerous studies (Table 6). For instance, in the experiment of Emam et al. [63] on rats suffering from hepatic injury, apelin decreased the levels of ALT, AST and L
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The crucial role of AP in establishing and
2024-08-20
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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br MADS box proteins in plants a
2024-08-20
MADS box proteins in plants, a flourishing family In contrast to animals, homeotic genes in plants do not code for homeodomain-containing proteins, but rather, in almost all cases, for MADS domain proteins. The sequencing of the genome of Arabidopsis thaliana revealed more than 100 putative MADS
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Introduction Cardiovascular disease is the principal cause o
2024-08-20
Introduction Cardiovascular disease is the principal cause of morbidity and mortality in patients with Danoprevir (1). Comprehensive management of these patients includes not only adequate glycemic control but also attention to additional recognized risk factors. Hypertension is a cardiovascular r
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br Conflict of interest statement br
2024-08-20
Conflict of interest statement Introduction Tanshinone IIA (Tan IIA) is a major active component of Salvia miltiorrhiza (S. miltiorrhiza), a well-known Chinese traditional medicine that is used for the treatment of cardiovascular and cerebrovascular diseases [1]. Tan IIA exhibits diverse pharm
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In another study Yerra and Kumar used streptozotocin
2024-08-20
In another study, Yerra and Kumar (2016) used streptozotocin to induce diabetic neuropathy in rats. Mechanical/thermal hyperalgesia, motor/sensory nerve conduction velocities (MNCV and SNCV) and sciatic nerve blood flow (NBF) were evaluated. In vitro studies of Neuro2a (N2A) cell culture were perfor
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br Conflict of interest statement br
2024-08-20
Conflict of interest statement Acknowledgement Introduction Lipoxygenases (LOs) are enzymes catalyzing the positional as well as stereo-specific introduction of molecular oxygen into 1,4-pentadiene structures found in unsaturated fatty acids such as arachidonic beta-lactamase or linoleic a
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