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In the past few years DNA templated fluorescent
2020-10-22

In the past few years, DNA-templated fluorescent metal nanoparticles have been developed as ideal alternatives to organic dyes due to their facile synthetic process, outstanding optical properties, ultrafine size, and fine biological compatibility. Since the first successful demonstration of DNA-tem
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Classical DHFR inhibitors such as methotrexate MTX bind tigh
2020-10-22

Classical DHFR inhibitors such as methotrexate (MTX) bind tightly to the enzyme and possess adequate clinical pharmacokinetics. MTX bind to the DHFR binding site through the formation of hydrogen bonds with Asn64, Lys68, Arg28, Arg70, Val115 and Ile7 amino Pridinol Methanesulfonate residues as well
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Although DAPK has been implicated in neuronal
2020-10-22

Although DAPK has been implicated in neuronal death in ischemic stroke and neurodegenerative diseases, such as Alzheimer’s disease (Shamloo et al., 2005, Duan et al., 2013), the mechanisms about how DAPK regulates cell death are still elusive. In the present study, we investigated the signal transdu
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In cancer interactions between the transformed cancer
2020-10-22

In cancer, interactions between the transformed cancer Conoidin A and other cell types recruited to the tumor are important. Tumor associated macrophages provide cancer cells with a suitable low-grade inflammatory milieu including growth promoting factors. Our results suggest a novel pro-tumorigenic
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Since PTKs are involved in numerous aspects
2020-10-22

Since PTKs are involved in numerous aspects of cell function, their regulation is critical for cell survival and function. The carboxyl-terminal tyrosine of Src-family PTKs is a key site of regulation. Phosphorylation on this carboxyl-terminal tyrosine contributes to the induction of a conformationa
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Acknowledgments The authors thank Dr Vladimir Poltoratsky
2020-10-22

Acknowledgments The authors thank Dr. Vladimir Poltoratsky and Zhihui Xiao for their help with the in vitro FRET assay. Support for this research was provided by Saint John’s University. Introduction We predicted the existence of endothelium-derived contractile factors (EDCFs) in 1982 [1]. In 1
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acetylcholinesterase inhibitor Fusion genes are formed as th
2020-10-22

Fusion genes are formed as the result of either structural chromosomal rearrangement including, primarily, translocation, inversion, amplification and deletion, or non-structural aberrations caused by cis- and trans-splicing or transcriptional read-through. Such events are known to play important ro
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It has been observed in our results
2020-10-22

It has been observed in our results that patients carrying risk allele “a” are at the greater risk of developing psoriasis. Same results have been presented by Coto-Segura et al., 2011, in a study conducted on Spanish population where they reported association of VNTR polymorphism among the patients
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Introduction Obesity constitutes a global healthcare problem
2020-10-22

Introduction Obesity constitutes a global healthcare problem and has many adverse effects on the cardiovascular function [1,2]. Recently, the perivascular adipose tissue (PVAT) has emerged as a relevant fat depot for cardiovascular risk and as a potential trigger in vascular dysfunction. Indeed, PV
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In the current study cocaine did not
2020-10-22

In the current study, cocaine did not significantly increase negative subjective effects and nepicastat did not increase these responses. This outcome is somewhat surprising given that the most commonly reported effect to date has been to increase the aversive properties of cocaine such as anxiety,
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Like compound substitution on compound contains amino and ca
2020-10-22

Like compound substitution on compound () contains amino and carboxamide groups attached to adjacent ring positions. These groups have similar interactions as compound with the protein backbone and Glu114. The triazole core is coordinated with Lys291. The triazole ring core π-stacks with Tyr226. Th
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The ribosomal synthesis of D
2020-10-22

The ribosomal synthesis of D-proteins is not currently feasible; the best effort undertaken so far was limited to the translational incorporation of two D-amino acids into the nascent protein chain by means of modified ribosomes (Dedkova et al., 2006). We therefore apply solid-phase peptide synthesi
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Several research groups have disclosed potent
2020-10-22

Several research groups have disclosed potent and selective DGAT-1 inhibitors from several chemically-distinct series. Pre-clinical studies with these compounds have confirmed that small molecule DGAT-1 inhibitors can elicit metabolic outcomes comparable to those observed in DGAT-1−/− mice.19, 20, 2
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Our recent discovery M P H R
2020-10-22

Our recent discovery (M.P., H.R., A.S.) of a highly selective and in vivo active DDR1 small-molecule inhibitor provides evidence that DDR1 is a druggable pharmaceutical target, and some details of our efforts are provided below. To avoid the repurposing of known kinase inhibitor structural motifs, w
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A variety of fused membered ring chemotypes have arisen
2020-10-21

A variety of fused 6–5-membered ring chemotypes have arisen such as 7-azaindole acetic acids, benzimidazolyl acetic acids, spiro-indolinone acetic acids, and indolizine acetic acids, however, to the best of our knowledge, fused 5,5-membered ring systems have not been reported. Prostaglandin D (PG
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