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Previous studies from our lab looked at the effect
2020-03-04

Previous studies from our lab looked at the effect of interfering with crossover helix interactions in TS-DHFR. One study utilized peptide mimetics of the crossover helix to inhibit wild-type TS-DHFR noncompetitively, and with an IC of 230 μM. A second study used a virtual screening approach to iden
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The folate pathway plays an essential
2020-03-04

The folate pathway plays an essential role in cell survival by generating 5, 10-methylene tetrahydrofolate as a one-carbon donor for the synthesis of deoxythymidine monophosphate (dTMP), purines, methionine and histidine. Disruption of this pathway leads to the critical deficiency of these key molec
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Interestingly some drugs have been
2020-03-04

Interestingly, some drugs have been shown to be effective in the regulation of cytokine production (such as IL-2, IL-10, IL-27, IL-35, IL-37 and transforming growth factor-β, TGF-β) and, therefore, having a key role in the management of certain inflammatory-based clinical conditions (Banchereau et a
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Compound was generated using a literature
2020-03-04

Compound was generated using a literature procedure and required two-step Dess–Martin-periodinane/Pinnick oxidation prior to the methylation of the sulfonamide. Compound () was obtained from the Suzuki coupling of the methyl ester intermediate (en route to NSC 87877 australia ). Hydrolysis of al
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Our structures also provide new
2020-03-04

Our structures also provide new insights into CRTH2 drug development. The ligand binding pocket revealed by our structures comprises many aromatic residues and a few polar residues at the distal end. Correspondingly, most CRTH2 antagonists share a similar structural feature characterized by an aceta
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Some of the psychoactive actions of nicotine are
2020-03-04

Some of the psychoactive actions of nicotine are mediated by the nigrostriatal and mesolimbic pathways (Di Chiara, 2000, Di Chiara et al., 2004). The nigrostriatal pathway originates in the dopaminergic neurons located in the substantia nigra and terminates in the putamen and nucleus caudatus which
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Identification of the drug to be used as
2020-03-04

Identification of the drug to be used as first-step antihypertensive treatment has always been, and remains, a matter of debate. The decision wihich drug (or drug combination) to choose as first-line therapy depend on many variables such as coexisting metabolic disorders, obesity, presence of subcli
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Introduction Hematopoietic stem cells HSCs in the adult bone
2020-03-04

Introduction Hematopoietic stem CBR-5884 receptor (HSCs) in the adult bone marrow (BM) provide all types of blood cells throughout life, while also self-renewing to maintain blood homeostasis. Blood/marrow stem cell transplantation is the most advanced method to cure patients suffering from hematol
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Several questions remain to be
2020-03-03

Several questions remain to be addressed. The hormones and metabolites that modulate expression of EERγ in the steps leading to maturation need to be identified to learn more about physiological and pathophysiological regulation of EERγ in β cells. Considering that ERRγ repressed cell cycle genes in
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br Concluding Remarks Recent studies have provided unprecede
2020-03-03

Concluding Remarks Recent studies have provided unprecedented details of APC/C structure and enzymology, which explain how the activity of this massive E3 ligase is controlled, and how ubiquitylation is achieved to temporally regulate cell division. Although one pervasive question has been why th
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The component E of PDHc PDHc E catalyzes
2020-03-03

The component E1 of PDHc (PDHc-E1) catalyzes the first step of multistep processes, using thiamine diphosphate (ThDP) and Mg2+ as cofactors.15, 16 Especially, this PDHc-E1 catalyzed process is a rate limiting step among multistep processes. Accordingly, the PDHc should be inactive by inhibiting the
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Experiments on the rat model of E coli pyelonephritis perfor
2020-03-03

Experiments on the rat model of E. coli pyelonephritis, performed to investigate the relationship between the acute inflammatory processes and the permanent kidney damage (Brooks et al., 1974), have demonstrated a positive correlation between the degree of free radical-mediated renal injury and the
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Finally our results suggest that R
2020-03-03

Finally, our results suggest that σ2R may, at least partially, mediate the hunger-suppressive action of amphetamine by interacting with orexigenic receptors in CRF2R-OX1R heteromer contexts. Despite extensive evidence supporting the formation of GPCR oligomers in heterologous systems, the lack of ap
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The binding pattern of was analysed by
2020-03-03

The binding pattern of 1 was analysed by flexible molecular docking. The Pioglitazone inserted into the narrow ATP binding site of CK2 (Fig. 2). As shown the aliphatic chain of 1 was located at the edge of the pocket and established van der Waals interactions with the side chains residues of Ile95,
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br Conflict of interest statement br
2020-03-03

Conflict of interest statement Acknowledgement The study was financially supported by the Ministry of Education, Youth and Sports of the Czech Republic – projects “CENAKVA” (No. CZ.1.05/2.1.00/01.0024) and “CENAKVA II” (No. LO1205 under the NPU I program), by the Grant Agency of the University
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