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BMS-754807 br Transparency document br Introduction G protei
2024-05-09
Transparency document Introduction G protein-coupled receptors (GPCRs) comprise a diverse family of seven transmembrane domain-containing receptors represented by over 800 genes in humans. GPCRs respond to a range of stimuli, including peptides, hormones, growth factors, lipids, odorants, and
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In the late s Solvay Pharmaceuticals discontinued the
2024-05-09
In the late ‘90s, Solvay Pharmaceuticals discontinued the Phase 2 development of a promising potent and highly selective A1AR antagonist based on the pyrrolopyrimidine scaffold, SLV320 [43] (2, Chart 1, also named derenofylline; Ki hA1AR = 1 nM), for the treatment of acute heart failure [24]. In the
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Both subcutaneous s c and mucosal
2024-05-09
Both subcutaneous (s.c.) and mucosal administration of short synthetic peptide derivatives of AChR prevent the onset of EAMG, but do not treat ongoing EAMG [80], [81], [82], [83], [84], [85]. The selection of peptides for treatment is mainly based on the identification of immunodominant T- and B-cel
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br Conclusion In this brief Letter we report an easy
2024-05-09
Conclusion In this brief Letter, we report an easy method for the preparation of the antileukemic natural product 1. Using a biomimetic strategy,1, 8 in which the aromatic residues are attached to a lysine moiety prior to the reduction of the central carboxylate group, a step-economical synthesis
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br Dihydrotestosterone in adult fish
2024-05-09
Dihydrotestosterone in adult fish and frogs New perspectives and next directions Similar to other androgens, DHT can modulate reproductive endpoints in both fish and amphibians. However, predicting the effects of DHT can be challenging, as reproductive homeostasis is dependent upon the balance
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br Acknowledgement This work was
2024-05-09
Acknowledgement This work was funded by NIH/NINDS grant number NS080967 to C. Waites. Introduction Macro-autophagy also called autophagy is a conserved pathway for the lysosomal degradation and recycling of intracellular materials. It is instrumental for the homeostasis of cells and tissues a
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br Introduction In the past
2024-05-09
Introduction In the past two decades, graphene and graphene based nanomaterials with unique physicochemical properties have attracted great attentions in many fields including biomedicine and biotechnology. Graphene oxide (GO) and its derivatives have shown promising potential as biological and c
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In vascular endothelial cells L arginine produces nitric oxi
2024-05-09
In vascular endothelial cells, L-arginine produces nitric oxide (NO) under the action of nitric oxide synthase (NOS), and nitric oxide can activate guanylate cyclase to produce a large amount of cGMP, thereby relaxing vascular smooth muscle and expanding blood vessels. Numerous studies have confirme
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In previous years evidence emerged that inferred
2024-05-09
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 ci-1033 (7) and piceatannol (8) (Fig. 3b) on mammalian arginase with IC50s of 10
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AMP activated protein kinase AMPK is a key cellular
2024-05-08
AMP-activated protein kinase (AMPK) is a key cellular energy sensor that maintains energy homeostasis at the cellular and whole-organism level (Hardie et al., 2012). Functionally, the AMPK pathway sustains adenosine triphosphate (ATP) production through activation of fatty Exemestane oxidation and a
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Epidermal growth factor EGF has
2024-05-08
Epidermal growth factor (EGF) has been shown to increase the 12S-lipoxygenase mRNA level by about two-fold in human epidermoid carcinoma A431 cells [71]. This enzyme was shown to be of the platelet-type and associated with the microsomal fraction of the cells [71], [72]. A requirement for EGF recept
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The diversity of metabolic adaptations employed by cancer ce
2024-05-08
The diversity of metabolic adaptations employed by cancer cells in response to rapidly changing conditions, contributes to their biological aggressiveness and therapeutic resistance by enabling them to proliferate when nutrients are plentiful and to shift their resources to survival when nutrients a
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br Introduction There are greater than five million
2024-05-08
Introduction There are greater than five million Americans living with Alzheimer's dementia and more than 35 million people worldwide [1], and without a way to stop or slow the progression, there will be nearly a tripling of individuals affected by 2050 (13.8 million) [1]. The urgency to develop
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In summary we identified a novel
2024-05-08
In summary, we identified a novel MLPH-ALK fusion in AST with discordant results of ALK IHC. In order not to overlook ALK-rearranged AST with rare fusion partners on IHC screening, a sensitive IHC method is preferable. Introduction Lung cancer remains the leading cause of cancer related deaths w
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In conclusion phenolic hydroxyl was introduced not
2024-05-08
In conclusion, phenolic hydroxyl was introduced not only to C3 side chain but also to C6 or C7 position of the quinoxalinone core, resulting in a new group of ARIs candidates exhibiting antioxidant activity. Biological activity tests suggested that compounds were not only sufficient to inhibit ALR2
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