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From an historical perspective ligands for GPCRs
2022-12-13

From an historical perspective, ligands for GPCRs (adrenaline, serotonin, capreomycin or morphine, to name a few) have been identified before their receptor counterparts, at a time when the concept of receptor itself was controversial [15]. Although many cognate receptors for endogenous ligands wer
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On the other hand key enzymes also involved in
2022-12-13

On the other hand, key plk1 inhibitor 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 concent
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In addition to calpain I activity cathepsin
2022-12-13

In addition to calpain I activity, cathepsin activities have been proven to be linked to apoptotic signaling. Cathepsin B and cathepsin D are two of the most abundant and well-investigated lysosome acid-dependent proteases that are involved in the apoptotic regulation (Ferri & Kroemer, 2001). Cathep
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The putative residue apelin proprotein proapelin or apelin i
2022-12-13

The putative 55-residue apelin proprotein (proapelin or apelin-55) is processed from a 77-residue preproprotein through removal of a 22-residue signal peptide (Table 1). Apelin-55 is further processed into bioactive isoforms of 36, 17, or 13 residues, likely through protease-mediated mechanisms. To
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br Disclosures br Author contributions br Grants This
2022-12-13

Disclosures Author contributions Grants This work was supported by National Institutes of Health/National Heart, Lung, and Blood Institute MERIT Award R37 HL040696 to J.A.F. Acknowledgments Introduction The AGC kinases, named after the protein A, G and C kinases, are an evolutionaril
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Metformin s pluripotent roles are alluded to in terms of
2022-12-12

Metformin's pluripotent roles are alluded to in terms of its antitumorigenic, glucose-lowering, and cardioprotective effects, which are due in part to its upregulation of AMPK activity [39,40]. Metformin's glucose-lowering effect is a result of reduced hepatic gluconeogenesis, whereas improved insul
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br Results br Discussion The actin cytoskeleton is
2022-12-12

Results Discussion The aa dutp receptor cytoskeleton is a highly attractive target for many bacterial toxins, owing to its role in activation and locomotion of immune cells, secretion of humoral response factors, and maintenance of protective barriers at the cellular (sub-membrane cytoskeleton
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br Materials and methods br Results The
2022-12-12

Materials and methods Results The determination of the intrinsic inhibitory potential of the oximes HI-6 and MMB-4 with human and guinea pig AChE revealed marked differences between both oximes (Table 1). MMB-4 had an only marginal effect on both AChE species, calculated IC50 of >1000μM, while
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Based on the observation that antipsychotic drugs increase
2022-12-12

Based on the observation that antipsychotic drugs increase 5-HT1A–D2 heteromerization level (Łukasiewicz et al., 2016), we set out to compare the effect of paroxetine to that of risperidone. Paroxetine, a potent SSRI, is very effective in the treatment of depression and anxiety disorders, e.g., gene
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HCC aetiology is multifactorial and the disease is often
2022-12-12

HCC aetiology is multifactorial and the disease is often preceded by other conditions including liver fibrosis and cirrhosis that are associated with HCV, HBV, alcoholic and non-alcoholic hepatitis. The discovery of new therapeutic targets will require a greater understanding of the pathogenic mecha
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br Materials and methods br Results
2022-12-12

Materials and methods Results Discussion Despite the relative complexity of immunotherapy, such treatment may have an important role, in conjunction with other therapies in the treatment of cancer refractory to conventional treatments alone. Clinical studies have recently shown that adding
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Functional enhancers are often composed of binding motifs
2022-12-12

Functional enhancers are often composed of binding motifs of multiple key transcription factors to confer spatial and temporal regulation of genes in a certain context. In the uterus, the difference between the number of genes that have associated PGR occupancy and that of progesterone responsive ge
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A third motif involves the toggle switch and consists of
2022-12-12

A third motif involves the toggle switch and consists of the conserved FxxCWxP sequence in TM6 of class A GPCRs (Hofmann et al., 2009, Rosenbaum et al., 2009). Rotamerization of Trp in combination with a kink caused by Pro facilitates the outward movement of TM6 upon activation (Hofmann et al., 2009
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br Discussion Arginase and Arginase are homologous
2022-12-12

Discussion Arginase 1 and Arginase 2 are homologous enzymes that consume l-arginine to produce l-ornithine and urea [14], [15]. These enzymes compete with NO synthases for the same substrate [14], [15], [30], and therefore may reduce NO production [21], [24], [30]. The colocalization of arginases
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This study evaluated the anti tumor influences of LA
2022-12-12

This study evaluated the anti-tumor influences of LA against HepG2 Vicriviroc Malate in vivro, and investigated the molecular mechanisms of inducing apoptosis. Overall, our studies suggested that LA is a promising anti-cancer drug and a possible novel therapeutic agent directed toward the mitochond
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