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br Acknowledgement This research was supported by Basic Scie
2022-01-05
Acknowledgement This research was supported by Basic Science Research Program through the National Research Foundation of Korea funded by the Ministry of Education, Science and Technology (NRF-2016R1A2B4012818). Oral Sephin1 is the most popular administration route due to good patients’ compl
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Histamine H and H receptors are considered as
2022-01-05
Histamine H1 and H2 receptors are considered as low affinity receptors (pKi of 4.2 and 4.3 respectively), whereas histamine H3 and H4 receptors as a high affinity receptors (pKi of 8 and 8.2 respectively) (Schreeb et al., 2013). Therefore it might well be that other histamine receptors might be invo
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Multi targeting agents are of major interest in modern
2022-01-05
Multi-targeting agents are of major interest in modern drug design and discovery. Design of such compounds can be applied to H3R antagonists for the purpose of achieving optimum efficiency as performed for some preclinical candidates such as recently for contilisant (Bautista-Aguilera et al., 2017;
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In our previous study we designed and synthesized
2022-01-04
In our previous study, we designed and synthesized compounds of A series from the starting material 4-hydroxy-3-methoxycinnamic bazedoxifene australia (ferulic acid). These compounds with R group being amino acid residues, fatty acyl group and sulfuryl group showed moderate HDAC inhibition and in vi
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br Role of dynamin in
2022-01-04
Role of dynamin in NPRA endocytosis In recent studies using 125I-ANP binding assay and confocal microscopy, we have examined the role of dynamin in the internalization and trafficking of NPRA in a stably transfected HEK-293 Cholesterol [69]. Our findings indicated that ANP treatment of high-dens
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br Disclosure statement br Acknowledgements We
2022-01-04
Disclosure statement Acknowledgements We thank Dr. Rona Carroll for her contribution to the preparation of the manuscript and Dr. Iosif Pediaditakis for his contribution to the preparation of the figures. This work was supported by NIHR01 HD019938 to U.B.K. Introduction The mammalian hypot
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Despite potent biological actions the
2022-01-04
Despite potent biological actions, the native hormone undergoes degradation by the enzyme dipeptidylpeptidase-IV (DPP-IV) [17] and is rapidly cleared from the bloodstream by renal filtration [18]. One such approach to prolong the biological half-life of GIP is through conjugation with a polyethylene
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Knowing that our strongest phenotypic differences between th
2022-01-04
Knowing that our strongest phenotypic differences between the genotypes involved feeding behavior in various contexts, we decided to examine the case of restricted feeding and food anticipatory activity. Animals faced with a restricted schedule of food availability develop a series of anticipatory b
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Based upon the present findings it is tempting to imagine
2022-01-04
Based upon the present findings, it is tempting to imagine that selective, and especially stable blood–brain barrier (BBB) penetrating GalR1 antagonists might be useful as drugs for acute suppression of appetite. While this may be possible, previous studies using nonspecific galanin antagonists yiel
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To date types of glucose transport protein have been
2022-01-04
To date, 14 types of glucose transport protein have been discovered, each having its own specific functions with different distributions [33]. Among these, GLUT4 is particularly important for maintaining glucose metabolism homeostasis and insulin sensitivity, since it is involved in glucose transpor
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Much is known about FPPS structure and function with
2022-01-04
Much is known about FPPS structure and function, with over 120 FPPS crystal structures being currently available. This wealth of information is largely the consequence of human FPPS serving as a drug target for the treatment and/or prevention of pathologies such as osteoporosis, hypercalcemia and Pa
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Tourette s syndrome TS is a neurobehavioral
2022-01-03
Tourette's syndrome (TS) is a neurobehavioral disorder characterized by chronic motor and vocal tics. The histaminergic system appears to be implicated in the pathophysiology of TS because H3R up-regulation has been observed in the striatum of HDC knock-out animal models (Rapanelli et al., 2017; Rap
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Finally our work showed that HAART resulted in
2022-01-03
Finally, our work showed that HAART resulted in significant inter-individual variability among DEGs, which reflected the Nogo-66 (1-40) in HIV-affected human gene expressions (Fig. 1, Fig. 2, Fig. 3, Fig. 4). These observations also highlighted the importance of determining common as well as person
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Our exploration of Domain focused on the role
2022-01-03
Our exploration of Domain 1 focused on the role of the carbonyl linker in (). We found that replacement of this group by a methylene unit as in or direct attachment of the thiophene ring to the central aromatic core as in did not significantly impact potency. The thiophene ring in could be repla
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L-Cysteinesulfinic acid mg br Results and discussion A diver
2022-01-03
Results and discussion A diverse set of compounds were synthesized to improve the PK and physicochemical properties of 2. Compounds' agonist effects on hGPR40 were assessed by calcium mobilization assay using hGPR40-HEK293 cell line which stably expressed human GPR40. Preliminary explorations fo
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