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br Galanin in depression A
2021-12-17

Galanin in depression A major impediment in depression research is the lack of validated animals´ models. Animals not only lack consciousness of self, self-reflection and consideration of others but also hallmarks of the disorder such as depressed mood, low self-esteem or suicidal intent are hard
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On the other hand histone deacetylase inhibitors can acceler
2021-12-17

On the other hand, histone deacetylase inhibitors can accelerate inflammation resolution by promoting the externalization of AnxA1, a main ALX/FPR2 agonist, with concomitant inhibition of cytokine gene expression in mouse macrophages [30]. Thus, our present results provide an additional mechanism, i
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Zalcitabine br Materials and methods br Acknowledgments We a
2021-12-17

Materials and methods Acknowledgments We are grateful for financial support from the National Natural Science Foundation of China (Grants No. 81661148046 and 81773762, China) and the “Personalized Medicines—Molecular Signature-based Drug Discovery and Development”, Strategic Priority Research
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br Author contributions br Acknowledgements The work was
2021-12-17

Author contributions Acknowledgements The work was supported in part by Natural Science Foundation of China (31601995, 31501028) and an internal research grant of Jianghan University (14042). The authors thank HY of Jingchu University of technology for revising the manuscript. Introduction
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A second H R antagonist
2021-12-17

A second H3R antagonist with benzamide-based structure from Johnson & Johnson is JNJ-31001074, known as Bavisant and under chemical IUPAC name of (4-cyclopropylpiperazin-1-yl)-[4-(morpholin-4-ylmethyl)phenyl]methanone. It is a compound with molecular weight 329.44, HBA four, and MLogP 1.52 encompass
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br Conflict of interest br Acknowledgements br
2021-12-17

Conflict of interest Acknowledgements A Class of Unconventional, Dimerization-Activated GTPases GTP-binding proteins, or GTPases, are a superfamily of proteins that regulate numerous cellular pathways 1, 2, 3, 4. Pioneering work on the extended Ras subfamily of GTPases, exemplified by Ras,
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br Family A Receptors as Promiscuous
2021-12-17

Family A Receptors as Promiscuous Sensors for Peptone and Free Fatty Acids (FFAs) In addition to the family C 7TM receptors, several family A 7TM receptors are promiscuous in their ligand preferences, and several respond to organic nutrients from food, notably protein degradation products and FFA
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Optimization of the tetrahydroindazole series led
2021-12-17

Optimization of the tetrahydroindazole series led to the discovery of two moderately potent γ-secretase modulators, 2-cyclobutane and 2-hydroxy-2-methylpropane which were subsequently evaluated in a kinetic aqueous solubility assay. Unfortunately, neither analog demonstrated improved solubility ()
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br Factor Xa an enzyme in the coagulation cascade has
2021-12-16

Factor Xa, an enzyme in the coagulation cascade, has recently been identified as having a role in inflammation, generating interest in factor Xa inhibitors as anti-inflammatory agents beyond their established use as anticoagulants [, , , ]. We report sustained clinical and electrophysiologic impro
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Following the discovery of diketo compounds
2021-12-16

Following the discovery of β-diketo compounds S-1360 [31] and L-731988 [32] as anti-HIV integrase inhibitors, a group of researchers discovered a potent triphosphate based derivative (1) as the inhibitor of HIV integrase functioning at the 3′-processing and strand transfer steps of HIV integrase. Bi
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We reveal that the four well known vertebrate families
2021-12-16

We reveal that the four well known vertebrate families of KAT enzymes (GNAT, MYST, P300/CBP, Basal transcription factor/nuclear receptor co-activator) seem to be conserved (Karmodiya et al., 2014; Roth et al., 2001; Sheikh & Akhtar, 2018) in the mangrove rivulus, together with Camello, a potential n
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am580 Multi targeting agents are of major interest in
2021-12-16

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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br Material and methods br
2021-12-16

Material and methods Result Discussion The female with well-differentiated endometrial cancer, especially those in the reproductive age have a strong desire to preserve fertility. Therefore, conservative medical treatment with progestin is widely used in the clinic. However, up to 30% of pa
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The bioconversion of inositol from glucose was
2021-12-16

The bioconversion of inositol from glucose was anticipated nearly a century ago and later confirmed by isotope tracing methods [[22], [23]]. This biosynthesis of inositol involves three sequentially acting enzymes: Firstly, ATP-dependent glucokinase converts glucose to glucose-6-phosphate (G-6P) [[2
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Some but not all GSIs inhibit signal peptide peptidases as
2021-12-16

Some, but not all, GSIs inhibit signal peptide peptidases as well, though this has not been systemically studied [36], [41]. When considering biological activities of various GSIs this is an important and understudied caveat that could influence both biological response as well as potential toxiciti
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