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As a part of our continuing efforts
2021-10-29

As a part of our continuing efforts towards discovery of new class of compounds against different therapeutic areas and based on the literature reports, we designed a dual pharmacophore which possess a long aliphatic chain of free fatty acids and a phenyl propanoid part of known GPR40 agonists. Here
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br Acknowledgments br Introduction Postmenopausal osteoporos
2021-10-29

Acknowledgments Introduction Postmenopausal osteoporosis, which is primarily caused by nor-Binaltorphimine dihydrochloride deficiency, has been a worldwide health problem and threatens postmenopausal women of all races. An estimated 80% of osteoporosis patients in the United States are women,
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84 br Acknowledgments We would like to acknowledge Jenna
2021-10-29

Acknowledgments We would like to acknowledge Jenna Hall, Marita Rivir, Kathleen Smith, Joyce Sorrell, and Emily Yates for assistance with in vivo pharmacology studies. We would like to acknowledge Joe Chabenne and Steph Mowery for assistance with in vitro cell-based assays, and Patrick J. Knerr f
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br Conflicts of interest br Acknowledgments This work
2021-10-29

Conflicts of interest Acknowledgments This work was supported by the following funds: National Natural Science Foundation of China (81502222); Natural Science Foundation of Hubei Province (2013CFB370); Training program for Wuhan young and middle-aged medical backbone personnel (2017–51). In
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br Conclusion br Acknowledgements br Introduction
2021-10-29

Conclusion Acknowledgements Introduction γ- Aminobutyric CVT-313 receptor (GABA) is the main inhibitory neurotransmitter in the adult central nervous system. GABA receptors are divided into two classes, GABAA and GABAB. GABAA is an ionotropic receptor that mediates fast GABA responses by o
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In summary the SAR of a series of phenylpropanoic
2021-10-29

In summary, the SAR of a series of phenylpropanoic acid-free fatty Exendin-3 (9-39) amide receptor agonists is described which resulted in the identification of potent FFA4 agonists. The superior pharmacokinetic properties of compound led to its selection as an in vivo tool compound which afforded
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Corresponding to the different insulinotropic signaling
2021-10-29

Corresponding to the different insulinotropic signaling, the competitive radioligand-binding studies demonstrated at least 3 distinct kinetin on GPR40: orthosteric binding site for endogenous ligands, allosteric binding site for partial agonists and another allosteric binding site for full agonists
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Pharmacological inhibition of PKR seems to be an
2021-10-29

Pharmacological inhibition of PKR seems to be an interesting strategy for revealing the role of PKR in oxytosis and ferroptosis. The oxindole/imidazole derivative C16 was identified by screening a library of 26 different ATP-binding site-directed inhibitors of varying structure that is more selectiv
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Magtanong et al observed that caspase dependent apoptotic li
2021-10-29

Magtanong et al. (2019) observed that caspase-dependent apoptotic lipotoxicity of saturated fatty acids is suppressed by exogenous MUFAs. This may explain the ability of MUFAs to prevent atherosclerosis, in contrast to the pathogenicity of saturated fatty acids. Moreover, MUFAs may promote while PUF
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The Rho family of GTPases
2021-10-29

The Rho family of GTPases is composed of many small ubiquitous signaling G proteins that bind to guanosine triphosphate (GTP) and hydrolyze it to guanosine diphosphate (GDP). They act as switches: when binding to GTP, they are active and associate with a variety of target proteins that regulate intr
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Introduction Thrombotic disorders including ischemic heart
2021-10-29

Introduction Thrombotic disorders including ischemic heart disease, deep venous thrombosis, and ischemic stroke represent one of the most common causes of death in the world [1]. All these conditions relate to states accompanied by a shift of hemostasis balance into a coagulation side because of va
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br Experimental procedures br Results br Discussion The
2021-10-29

Experimental procedures Results Discussion The data herein confirm the well documented neuroinflammatory effect of TLR3 activation following systemic administration of the viral mimetic poly I:C and the associated acute sickness response which includes fever, reduced body weight and allodyn
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Previous studies have attributed the changes that occurs dur
2021-10-29

Previous studies have attributed the changes that occurs during the behvioral sensitization to many psychostimulants with neuroadaptation in dopaminergic cell bodies of the VTA (induction phase) along with alteration in dopamine axon terminal field transmission of NAc during the expression to sensit
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As a measure of ROS
2021-10-28

As a measure of ROS formation we measured the extent by which Cu(I) affected the production of hydrogen peroxide and, at the same time, to ensure that there would not be shortage of NADH substrate. Our results show that H2O2 production is increased over time by LPS stimulation but it is not when mic
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br Results br Discussion The twin cysteine motif is
2021-10-28

Results Discussion The twin-cysteine motif is an evolutionary conserved motif in all primate lentiviruses except HIV-1 and some strains of SIVcpz according to sequence analysis (Bohl et al., 2013). It is assumed that only those SIVcpz which have lost the twin-cysteines successfully evolved to
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