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In prostate cancer PCa glucose metabolism plays
2022-03-12
In prostate cancer (PCa), glucose metabolism plays a major role in progression [14]. Androgens can activate the metabolic regulator AMP-activated kinase (AMPK), promoting oxidative phosphorylation (OXPHOS) [15]. Besides, androgens increase GLUT1 [16], which overproduction has been described in the m
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Compound C pHi regulation in astrocytes has been examined pr
2022-03-12
pHi regulation in astrocytes has been examined primarily in cell culture rather than in situ. Two HCO3−-dependent transporters, NBC and Na+-driven Cl-HCO3 exchange (NDCBE), have been described [10,16], in addition to Cl-HCO3 anion exchange (AE) [96]. Culture studies indicate that NHE is the principa
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Various strategies have been pursued
2022-03-12
Various strategies have been pursued in the search for GIPR antagonists. Antibodies raised against both GIP(1–42) [14], [15] or the GIPR [16], [17], a small molecule antagonist [18], amino transcription factors substitutions of GIP(1–42) [19], and various GIP(1–42) truncations and modifications such
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br Conflict of interest br Transparency
2022-03-12
Conflict of interest Transparency document Acknowledgements We acknowledge our funding sources from the American Heart Association (13EIA4480016) and the National Institute of Health/National Heart, Lung, and Blood Institute (RO1 HL094414). We are very grateful to Dr. Shaohua Xiao and Dr. S
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As a part of our continuing efforts
2022-03-12
As a part of our continuing efforts towards discovery of new class of compounds against different therapeutic areas and based on the literature reports, we designed a dual pharmacophore which possess a long aliphatic chain of free fatty acids and a phenyl propanoid part of known GPR40 agonists. Here
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More specific quantitative assays for DiXaIs are based on th
2022-03-12
More specific quantitative assays for DiXaIs are based on the inhibition of chromogenic or clotting activity of Factor Xa. During drug development, Kubitza developed an endogenous Anti-Factor Xa assay [45], which is very sensitive to Rivaroxaban drug concentration. This assay was based on Factor Xa
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br Acknowledgments R Dalmann has obtained a bourse
2022-03-12
Acknowledgments R. Dalmann has obtained a “bourse Cifre” (grant 304/2011) from the ‘Association Nationale de la Recherche Technique’ and Bristol-Myers-Squibb. Introduction Endocannabinoids, their molecular targets (receptors), their synthetic and degrading enzymes and proteins that transport
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ANP (1-11), rat sale Some SNPs have been identified
2022-03-11
Some SNPs have been identified for HRH in cancer (Table 4). Looking into breast cancer research, H4 receptor polymorphisms have been recently associated with the malignancy of the disease. This was evidenced upon the analysis of genotypes and haplotypes of a Chinese Han population; this study showed
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pilocarpine hydrochloride br Mechanisms of HDAC inhibition
2022-03-11
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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Mapping PPI networks is challenging as it is
2022-03-11
Mapping PPI networks is challenging, as it is difficult to express and purify large variaties of InstaBlue Protein Stain Solution synthesis in sufficient quantities to allow the study of interactions between them. Membrane-bound proteins are particularly difficult to purify in functional form due to
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Our results show that deletion of the first loop
2022-03-11
Our results show that deletion of the first loop of Obg does not abolish the augmentation of the GTPase activity of CgtAvc, revealing that the first loop is mainly responsible for the anchoring of the protein in the 50S and the transient interaction with ribosome is enough for augmentation of GTPase
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Tamoxifen is still the most frequently
2022-03-11
Tamoxifen is still the most frequently used selective estrogen receptor mediator (SERM) in premenopausal women suffering from estrogen receptor positive (ER+) breast carcinomas [15]. Although this therapy has been proven very successful, about 20–30% of ER+ breast tumors will not respond, or acquire
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br Introduction Atherothrombosis is associated with the pres
2022-03-11
Introduction Atherothrombosis is associated with the presence of a low-grade, subclinical smoldering inflammatory response [1]. Several inflammatory markers, among them high-sensitive C-reactive protein (hs-CRP) [2], the erythrocyte sedimentation rate (ESR) [3], fibrinogen concentrations [4], int
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Homoharringtonine sale In the latent inhibition model a con
2022-03-11
In the latent inhibition model, a conditioned stimulus (CS) is pre-exposed alone without any consequences (i.e., unconditioned stimulus [US]) in the pre-exposure phase. The CS is then associated with a US to form a CS-US association. The strength of the CS-induced response in the pre-exposure group
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br Results and discussion br Conclusions TZDs represent a
2022-03-11
Results and discussion Conclusions TZDs represent a well-studied group of antidiabetic agents. Based on previous observations of the ability of some TZDs to activate FFAR1, we designed five scaffolds consisting of the TZD head, a linker, and a carefully selected privileged structure. For the p
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