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Extensive pharmacological and structural analysis shows GCGR
2022-08-22

Extensive pharmacological and structural analysis shows GCGR antibody REMD-477 competitively blocks GLC binding to the GCGR with 30-pM binding affinity, and can fully inhibit the receptor activity at low nanomolar concentrations in ANA 12 14, 17, 20. Functionally identical to REMD-477, REMD2.59 is a
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We tested formyl MYVKWPWYVWL which we had
2022-08-19

We tested formyl-MYVKWPWYVWL, which we had previously shown to have essentially identical Kis for W190/N192, R190/K192 and R190/N190 [8] of 130 nM, for its ability to downregulate surface receptor (Fig. 5A). R190/K192 exhibited the lowest EC50 of 44±4 nM about 3 fold below the observed Ki and a maxi
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br Introduction In addition to glucose which is the foremost
2022-08-19

Introduction In addition to glucose, which is the foremost stimulator of insulin secretion in beta-cells, other nutrients such as free fatty acids (also called non-esterified fatty acids, NEFA) contribute to glucose-stimulated insulin secretion (GSIS). Glucose triggers the processes leading to in
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4-Aminobutyric acid Combination inhibitors of FAAH TRPV and
2022-08-19

Combination inhibitors of FAAH, TRPV1, and/or COX2 may have the advantage of effective pain relief with a high therapeutic index. For example, arachidonoyl serotonin (AA-5-HT) inhibits both FAAH (IC=1–12μM) and TRPV1 (IC=37–270nM against 100nM capsaicin in HEK-293 cells)., In mice, AA-5-HT had great
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Our observation of LPS induced increase in the sensitivity
2022-08-19

Our observation of LPS-induced increase in the sensitivity of cultured endothelium-intact coronary ARM1 towards stimulation with selective ETB receptor agonist (S6c) could be explained by activation of TLRs receptors located on the endothelium of rat coronary arteries. However, the possible recruit
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br The HDC knockout mouse as a pathophysiological model of
2022-08-19

The HDC knockout mouse as a pathophysiological model of TS The implication of a hypomorphic allele of the Hdc gene as a rare cause of TS (Ercan-Sencicek et al., 2010) created a rare opportunity for the generation of a pathophysiologically grounded model of the disorder. Modeling pathophysiology o
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br Although there are growing bodies of research dealing
2022-08-19

Although there are growing bodies of research dealing with diverse non-imidazole based compounds, they are not free from obstacles in their development pipeline and hence the design of these compounds is complicated by various factors briefly discussed below. One of the problems in designing H3R a
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Successful immune escape will be then followed
2022-08-19

Successful immune escape will be then followed by cancer development, along with which immunocytes infiltration occurs. While some immunocytes are born to sweep away the malignancy, others aim to neutralize the lethality and sustain immune anergy and tolerance [59,60]. And the latter one is well rep
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The inhibition of HDAC increases the level of
2022-08-19

The inhibition of HDAC increases the level of histone acetylation and consequently turns the chromatin to be loose and active, allowing multiple transcription factors to access to promoters of diverse genes including tumor suppressor genes []. As compound possessed potent HDAC inhibitory activity a
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br Introduction Although effective hepatitis B
2022-08-19

Introduction Although effective hepatitis B virus (HBV) vaccines are in use worldwide, HBV-related liver diseases are still a major public health concern, causing considerable morbidity and mortality. Approximately 257 million people are currently suffering from chronic hepatitis B and 887,000 de
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Cells undergoing EMT display a downregulation of E cadherin
2022-08-19

Cells undergoing EMT display a downregulation of E-cadherin and dissociation of their junctional complexes that associates cell-cell contacts with the AEE788 receptor cytoskeleton, known as the adherens junction (Berx and van Roy, 2009, Birchmeier and Behrens, 1994). Adherens junctions are speciali
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We also examined possible involvement of the NF B signaling
2022-08-19

We also examined possible involvement of the NF-κB signaling pathway in GSK-3 inhibitor-induced suppression of PGE2 production, whereas GSK-3 inhibitors did not have a significant effect on IκB phosphorylation/degradation or NF-κB nuclear translocation. These results are consistent with a previous p
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A few methods have been developed to separate
2022-08-19

A few methods have been developed to separate and prepare compounds from L. chinensis, such as silica gel column chromatography [5,6] and high-performance liquid chromatography (HPLC) [7]. Silica gel column chromatography is still used for its simple equipment and low cost. However, this method is o
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Little is known about the endocrinological control of reprod
2022-08-18

Little is known about the endocrinological control of reproduction in polychaetes. In vertebrates, gonadal maturation is regulated by the hypothalamo-pituitary-gonadal axis. GnRH, GTHs, and steroid hormones are involved in this axis (see Okubo and Nagahama, 2008). In two polychaete species, Perinere
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Therefore we investigated the acute and delayed response of
2022-08-18

Therefore, we investigated the acute and delayed response of 92 human mono- and dizygous twins to an acute shift from low fat to high fat diet with respect to serum levels of VEGF and the expression of SLC2A1 in subcutaneous adipose tissue (AT). By comparing the degree of concordance of basal and di
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