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Experimentally the ECD spectrum of showed three ECD bands
2024-03-07
Experimentally, the ECD spectrum of 1 showed three ECD bands: positive ones at 260 and 200nm, and a negative one at 230nm (Fig. 4). Meanwhile, there is only one broad positive ECD band starting from 300nm in the ECD spectrum of 2. ECD spectra of 1 and its derivatives attracted great interest because
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Insulin is the central hormone involved in
2024-03-07
Insulin is the central hormone involved in the control of glucose and lipid metabolism. Other nonmetabolic effects of insulin are intensively studied as well. Activation of insulin receptor not only promotes glucose uptake, protein synthesis, and inhibits lipid metabolism, but also is crucial for re
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br Acknowledgments br Introduction Amyloid deposit formation
2024-03-07
Acknowledgments Introduction Amyloid deposit formation is defined by the aggregation of β-sheeted forms of proteins that appear as starch-like amorphous material [1], [2]. Using a Kongo red stain, amyloids show birefringence behavior and an apple-green to reddish multicolor emission. Extracere
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Recently a Phase III study demonstrated that alectinib
2024-03-07
Recently, a Phase III study demonstrated that alectinib, the second-generation ALK inhibitor, might have a better response to ALK-rearrangement patients than crizotinib [10]. Should alectinib replace crizotinib as the frontline treatment for ALK-rearranged patients? Or should those patients be treat
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The fact that the BPloopAsn
2024-03-07
The fact that the α1-BPloopAsn141 regains its α-Btx binding with a Kd similar to that of the wild type α1 ECD [18], suggests that the AChBP Cys-loop does not interfere with the correct conformation of the mutant ECD. Data from analogous mutants of the human neuronal α7 subunit ECD showed improved li
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Compounds were profiled for their inhibitory activity
2024-03-07
Compounds – were profiled for their inhibitory activity against dipeptidyl peptidase-IV Activity and/or Structure Homologues (DASH) [e.g. DPP2, DPP8 and DPP9] and non-DASH [eg. post-proline cleaving enzyme (PPCE), neutral endopeptidase (NEP), aminopeptidase P (APP), aminopeptidase N (APN)] enzymes.
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In this report the natural compound deguelin potently
2024-03-07
In this report, the natural compound deguelin potently and dose-dependently suppressed Aurora B kinase activity in vitro, indicating that this compound is an effective Aurora B inhibitor. The docking study indicated that deguelin was docked into the ATP-binding pocket of Aurora B and formed hydropho
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In Rainey et al published the results of
2024-03-06
In 2008, Rainey et al. published the results of a targeted compound library screen for potential inhibitors of the ATM kinase. In this study, the compound CP466722 was identified as a highly selective and rapidly reversible ATM inhibitor, which did not inhibit PI3K or related PIKK family members. Mo
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From an historical perspective ligands for GPCRs
2024-03-06
From an historical perspective, ligands for GPCRs (adrenaline, serotonin, Alrestatin synthesis 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 li
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br Introduction Humans have consumed mushrooms for centuries
2024-03-06
Introduction Humans have consumed mushrooms for centuries because of their high nutrient content and low lipid content, as well as their excellent flavor and texture [1]. Edible mushrooms possess notable medicinal properties and bioactivities, including antitumor, antiviral, antidiabetic, and ant
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br Future directions outlook Peptide
2024-03-06
Future directions-outlook Peptide-based macrocycles are among the privileged scaffolds in antibiotic drug discovery. Many compounds were discovered by natural product screening and developed unchanged, or as semi-synthetic derivatizations. Since the golden age of antibiotic discovery (1940s-mid 1
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In this report we introduce
2024-03-06
In this report, we introduce a new method for identifying aminopeptidases. Because single substrates can be insufficient for enzyme identification, we used an entire library of substrates to obtain more information about enzyme activity and to directly detect aminopeptidases. Moreover, substrates ca
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3254 synthesis The preferential expression of ALOX B in huma
2024-03-06
The preferential expression of ALOX15B in human macrophages may explain why human genetic studies investigating the association of ALOX15 with cardiovascular disease did not show consistent results. Two rare functional polymorphisms have been characterized in the ALOX15 gene, which leads to increase
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AhR was proven to participate in carcinogenesis Its high exp
2024-03-06
AhR was proven to participate in carcinogenesis. Its high expression was demonstrated in a variety of tumors, i.e. pancreatic, prostate, urinary tract, lung and papillary thyroid carcinoma (Safe et al., 2013, Mian et al., 2014). However, cell line studies showed variable AhR levels/responses. AhR kn
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br Hyperadiponectinemia in disease conditions Other evidence
2024-03-06
Hyperadiponectinemia in disease conditions Other evidence indicates that hyperadiponectinemia does not necessarily always imply a healthy outcome. Indeed, a recent study suggested that hyperadiponectinemia occurs in various diseases. Given that the risk for AD and vascular dementia is increased i
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