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Fatostatin A CPG a metalloenzyme derived from
2021-01-23
CPG2, a metalloenzyme derived from sp., was the elected enzyme for the first pilot-scale clinical trial of ADEPT. This enzyme has no mammalian homologue and activates glutamic Fatostatin A prodrug derivatives of several nitrogen mustards alkylating agents., , , , , A bond cleavable by CPG2 is ess
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Interestingly Carver Johnson and Kim investigated
2021-01-23
Interestingly, Carver, Johnson, and Kim (2016) investigated a polymorphism in the OPRM1 μ-opioid receptor gene for its role in sensitivity to social contexts. The G allele of this polymorphism was associated with higher levels of sensitivity. The authors found significant interactions, e.g. the nega
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To investigate the mechanism of action of trisubstituted azo
2021-01-23
To investigate the mechanism of action of 2,4,5-trisubstituted azoles, we profiled selected 2,4,5-trisubstituted azoles against a panel of 97 kinases to identify potential targets that could be involved in cardiogenesis. We narrowed down the identified targets to the casein kinase 1 (CK1) family due
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It has been reported that Eph Ephrin are
2021-01-23
It has been reported that Eph/Ephrin are involved in the regulation of the tumor angiogenesis [10], [11], [12]. The distinct and specific involvement of MDV 3100 and veins in tumor angiogenesis is unclear. EphrinB2 is expressed in arteries and its receptor EphB4 is expressed in veins; these molecul
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br Materials and methods br Results br Discussion
2021-01-23
Materials and methods Results Discussion Fluoride has multiple effects that contribute to caries prevention. S. mutans is 20- to 40-fold more sensitive to NaF than Lactobacillus casei and seven-fold more sensitive than some species of Actinomyces[10]. There are some specific metabolic effec
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br RING dimerization RING type domains are found in
2021-01-23
RING dimerization RING-type domains are found in many different structural contexts. While many exist as single-chain TASIN-1 (Fig. 3A), a notable feature of RING-type E3s is their tendency to form homodimers and heterodimers (Fig. 3C–F). Homodimeric RING-type E3s include cIAP, RNF4, BIRC7 (shown
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Acknowledgments br Introduction Diabetes mellitus DM is
2021-01-23
Acknowledgments Introduction Diabetes mellitus (DM) is a multifactorial disease [1] associated with serious comorbidities. This condition has recently reached epidemic proportions, as its occurrence has exponentially increased in the general population. Over 400 million people worldwide were est
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A range of inhibitors were therefore synthesized containing
2021-01-22
A range of inhibitors were therefore synthesized containing either carboxylic ARCA or ester functionality at the ‘tail’ group as well as variations in the ‘head.’ These were assayed in vitro using the DCIP assay for binding affinity against and human DHODH at 50μM, respectively (). Analysis of th
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br Materials and Methods br Acknowledgements br
2021-01-22
Materials and Methods Acknowledgements Introduction Collagen fibrillogenesis, the assembly of collagen fibers, is a critical process in the development, maturation, and repair of mammalian tissue. Alterations in the structure and amount of deposited collagen fibers can greatly alter the int
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To better understand Wolbachia s dependence on these enzymes
2021-01-22
To better understand Wolbachia’s dependence on these enzymes, RNAi experiments targeting these transcripts will be required to examine the consequences of their down-regulation on Wolbachia in the different tissues of the parasite. Initial studies have shown that decreases in Bm-cpl-3 and Bm-cpl-6 t
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PR171 br Introduction Sphingolipids are ubiquitous membrane
2021-01-22
Introduction Sphingolipids are ubiquitous membrane components of all eukaryotic cells belonging to a group of complex lipids. The basic structure of sphingolipids is composed of a sphingoid long chain base (LCB) linked to a fatty PR171 via an amide bond to form a ceramide [1]. In animals, sphingo
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We next considered the mechanism of the hepatospecific decre
2021-01-22
We next considered the mechanism of the hepatospecific decrease in CYP3A exerted by EGCG. We examined the possibility that orally administered EGCG was absorbed from the intestine and directly decreased the CYP3A expression level in the liver. Although the Aprotinin rate of orally administered EGCG
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Phenylbenzofurans are a very important molecule skeleton due
2021-01-22
Phenylbenzofurans are a very important molecule skeleton due to their synthetic versatility and their proved pharmacological properties [2]. They are synthetic compounds in which an additional phenyl ring is present in any position of the benzofuran nucleus. This could be easily obtained possible by
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The inhibition of CYP activity by NOR
2021-01-22
The inhibition of CYP11β activity by NOR was 11- and 2.5-fold higher than those reported for the antifungal agents ketoconazole (IC50: 4.4μM) and clotrimozole (IC50: 1.0μM) (Fernandes and Porte, 2013). Furthermore, NOR was able to inhibit P450 aromatase activity in carp ovaries, although at a rather
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The HEV vaccine developed based
2021-01-22
The HEV vaccine, developed based on p239 particles, is of good efficacy, immunogenicity and safety, and was licensed in China in 2012. p239 (aa 368–606) and E2 (aa 394–606) share a common region of ORF2, referred to as E2s (aa 459–606), which harbors the major antigenic determinants of the HEV vacci
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