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In the present study we set
2021-11-22

In the present study we set out to discover new non-steroidal SEGRA and to analyse their mechanism of function. Towards this goal we initiated a virtual screening (VS) approach, utilizing structure-based pharmacophore modeling, in silico docking and molecular dynamics (MD) simulations. Our pharmacop
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Inhibitors of the G rdos
2021-11-22

Inhibitors of the Gárdos effect include the Ca2+-channel blocker nitrendipine with an IC50 of ∼103nM (Ellory et al., 1992, Ellory et al., 1992); its mode of action is likely to be from direct blockage of K+ flux through the Gárdos channel (Ellory et al., 1992, Ellory et al., 1992), and the peptidic
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In the course of our ongoing attempts to
2021-11-22

In the course of our ongoing attempts to photolabel allosteric binding sites of γ-aminobutyric rapamycin price synthesis type A (GABAA) receptors, we were met with the need for relatively large (near mg) quantities of recombinant protein. Rather than establishing a stable cell line we sought to opt
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Recently there are only a spot of
2021-11-22

Recently, there are only a spot of FFA4 agonists reported in the literature (Fig. 1),13, 14, 15 and there is no selective FFA4 agonists have reached clinical trial for the treatment of T2DM. TUG-891, the first potent and selective FFA4 agonist, was developed in University of Southern Denmark as a wi
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Of the cases identified herein three known and
2021-11-22

Of the 52 cases identified herein, three known and 11 novel FGFR fusion partners were identified. Notably, an oligomerization domain, including coiled-coil dimerization domains similar to that seen in echinoderm microtubule associated protein like 4 gene (EML4), which is the most common ALK partner
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Following these discoveries the term ferroptosis was
2021-11-22

Following these discoveries, the term ferroptosis was coined in 2012 [25], to describe this iron-dependent, non-apoptotic form cell death induced by erastin and RSL3. This discovery was accompanied by the development of the first small molecule ferroptosis inhibitor, termed ferrostatin-1, and the de
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A compound structurally similar to PF has been developed by
2021-11-20

A Zanamivir structurally similar to PF-03654746 has been developed by Pfizer (PF-03654764), with a minor change in the substituent attached to the cyclobutanecarboxamide moiety (Wager et al., 2011). This compound, with the chemical name trans-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl]-N-(
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Maillard reaction also known as
2021-11-20

Maillard reaction, also known as non-enzymatic browning reaction, is a complex chemical reaction between carbonyl groups of reducing sugars and free amino groups of amino acids, peptides, proteins or some other nitrogen containing compounds. Maillard reaction plays an important role in food industry
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Fig C presents the secondary structure arrangement
2021-11-20

Fig. 1(C) presents the secondary structure arrangement of the PAS-A and PAS-B domains in both HIF-2α and ARNT. The common scaffold of the PAS domains is a β sheet with numerous flanking α helixes. The PAS-A domains of both HIF-2α and ARNT have A’α, Aβ, Bβ, Cα, Dα, Eα, Fα, Gβ, Hβ, and Iβ from the N t
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Here we report the genomic
2021-11-20

Here we report the genomic structure and the phylogenetic analysis of testis-specific Ser/Thr kinase haspin gene. Materials and methods Results Discussion The isolation and analysis of haspin genomic DNA showed that haspin was an intron-less gene and localized in an intron of integrin αM2
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br Rho protein networks in malignancy It
2021-11-20

Rho protein networks in malignancy It has long been recognized that Rho activity and expression are frequently elevated in tumors (Fritz et al., 1999, Orgaz et al., 2014). In this chapter we will introduce the most prominent Rho proteins, their regulators and effectors and provide an overview of
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br GSNOR activity and functions The identification of
2021-11-20

GSNOR activity and functions The identification of the enzyme responsible for GSNO decomposition dates back to 1998, when Jensen and colleagues described an NAD(P)H-dependent GSNO catabolizing activity in cytosolic fractions obtained from rat liver [16]. Upon purification, they identified this en
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br Experimental br Acknowledgments This research was support
2021-11-20

Experimental Acknowledgments This research was supported by the Korea Research Foundation (2013R1A1A2007509). The authors thank to Dr. Moon Ho Son (Dong-A Pharm. Co. Ltd) for hGPR119 agonist activity assay. We also thank to Pharmacal Research Institute and Central Laboratory of Kangwon Nationa
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Over expression of Glo can suppress
2021-11-20

Over-expression of Glo-1 can suppress inflammatory responses. Methylglyoxal mediates vascular inflammation in human endothelial (R,S)-Anatabine [33], indicating that Glo-1 may attenuate inflammation via eliminating methylglyoxal. Glo-1 knockdown mediated methylglyoxal accumulation provokes collagen
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br Results br Discussion br Materials
2021-11-20

Results Discussion Materials and Methods Introduction Deoxyribonucleic ML-291 (DNA) is among the most important biopolymers in living organisms alongside carbohydrates and proteins. DNA is a linear polymer consisting of four types of nucleobases, deoxyribose, and phosphate. The backbone
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