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From an historical perspective ligands for GPCRs adrenaline
2024-01-16

From an historical perspective, ligands for GPCRs (adrenaline, serotonin, Ryuvidine 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 were
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Intriguingly androgens may also have
2024-01-16

Intriguingly androgens may also have an indirect effect on AR gene expression through inhibition of the GATA2 transcription factor gene (He et al., 2014) (Table 1). Using ChIP-seq, GATA2 was found to bind to a regulatory element 5.5 kb upstream of the TSS of the AR gene and enhanced transcription, w
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ATI-2341 Fig shows a possible scheme
2024-01-16

Fig. 8 shows a possible scheme of the generation of AP(+)-exosomes based on this study. In response to inflammatory stimuli, ERAP1 is secreted from ER into the extracellular milieu through the conventional secretion pathway. On the other hand, exosomes are derived from the endosomal pathway, and are
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These mutations induce the gene auto activation in
2024-01-15

These mutations induce the gene auto-activation in 10–40% of adenocarcinomas, triggering the EGFR-signaling pathway in the absence of ligand. That leads to an uncontrolled acceleration of cell proliferation, survival and anti-apoptotic signals (Couraud et al., 2012). The frequency of these mutations
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The cavity volume of the binding pocket may differ not
2024-01-15

The cavity volume of the binding pocket may differ not only between species but also among various AhR/ARNT isoforms within a single species. It is noteworthy that even a single amino glutamate transporter substitution within a binding pocket may result in a change in the cavity volume. This, in tur
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The study by Lo http
2024-01-15

The study by Lowry et al. (2001) pointed toward functionally uncharacterized DA- and 5-HT-accumulating neurons within the DMH as a potential target for rapid nongenomic effects of CORT. Similar DA- and 5-HT-accumulating systems are distributed throughout the central and peripheral nervous systems, s
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br Conflict of interest br
2024-01-15

Conflict of interest Acknowledgements The authors would like to thank Mrs. Amparo Pacheco from CMPL, PUC, for her technical and secretarial assistance. This work was supported by the Fondo Nacional de Desarrollo Científico y Tecnológico (FONDECYT 1150344, 1050377, 11150083), and the Direccioń
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The gene SRD A encodes the reductase enzyme
2024-01-15

The gene SRD5A2 encodes the 5-α-reductase enzyme, which converts testosterone into dihydrotestosterone. Although dihydrotestosterone levels are considerably lower than testosterone, dihydrotestosterone has a five-fold stronger binding capacity to the androgen receptor and, thereby, a considerably mo
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On another hand pyrazoles are widely found as the core
2024-01-15

On another hand, pyrazoles, are widely found as the core structure in a large variety of compounds of great biological and pharmaceutical value exhibiting anti-HCV [11], antitumor [12], cytotoxic[13], and antioxidant activities [14]. Finally, 1,2,3-triazoles have attracted the interest of medicinal
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It involves complementary and inflammatory system
2024-01-15

It involves complementary and inflammatory system proteins, mast cells, eosinophils, basophils, macrophages, natural killer (NK) cells and cytokines [1]. Innate immunity, not only include cells, but also barriers that defend the organism to the penetration of pathogenic agents [2]. Important mediat
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gamma-Glu-Cys br Introduction Breast cancer is the second
2024-01-15

Introduction Breast cancer is the second most lethal cancer among women, accounting for approximately 40,000 deaths in the United States in 2015 [1]. The prognosis of breast cancer has improved significantly with the identification of immunohistochemical subtypes that predict response to therapy
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br Competing interests br Acknowledgments This
2024-01-13

Competing interests Acknowledgments This research was supported by Basic Science Research Program through the National Research Foundation of Korea (NRF) funded by the Ministry of Science and ICT (NRF-2014R1A4A1071040). Introduction Mitochondria occupy an important position as mediators o
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Our research group has been
2024-01-13

Our research group has been involved by many years in the synthesis of new 2,3-benzodiazepin-4-ones (e.g. 1, Fig. 1) and in the characterization of their mechanism of action.15, 16, 17 Within the development of these compounds, we demonstrated that an improvement of AMPAR antagonism by 2,3-benzodiaz
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Although only Leu CysAP IRAP Herbest et
2024-01-13

Although only Leu/CysAP (IRAP) (Herbest et al., 1997, Keller, 2004) and DPPIV (Alponti and Silveira, 2010, Kirino et al., 2009) had been identified and studied in adipocytes, our kinetic analysis suggested the highest physiological significance for AspAP (highest affinity) and APM and PSA (highest e
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br Methods br Results br Discussion First
2024-01-13

Methods Results Discussion First, the RO4987655 isolated from non-PD TA tissue and PD plaque tissue were characterized. The results showed that both cell groups were positive for vimentin and negative for desmin suggesting that these cells were fibroblasts. It was also observed that treatm
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