• br Conclusion br Conflict of interest br References

  2021-11-01

  

  Conclusion Conflict of interest References and recommended reading Papers of particular interest, published within the period of review, have been highlighted as: Acknowledgements Introduction Free fatty acids (FFAs) are essential nutrients that contribute to various cellular functio

• An alternative approach to improving pharmacokinetic profile

  2021-11-01

  

  An alternative approach to improving pharmacokinetic profile while retaining high GlyT1 potency was also pursued. Libraries were prepared in which potency enhancing piperidine C4 substituents were combined with clearance lowering truncated alkyl sulfonamides. The result was the discovery of (). Unl

• Previous studies have demonstrated that cannabinoid potentia

  2021-11-01

  

  Previous studies have demonstrated that cannabinoid potentiation of GlyR α3 subunits contributes to cannabinoid-induced analgesia. For instance, Dehydroxylcannabidiol (DH-CBD), a chemically modified cannabinoid, can alleviate acute pain and chronic inflammatory pain by targeting spinal α3 GlyRs (Xio

• Histamine functions as a key

  2021-11-01

  

  Histamine functions as a key neurotransmitter in multiple circuits to control various behaviors. In Drosophila photoreceptor, amyloid definition is produced de novo by histidine decarboxylase (Burg et al., 1993); meanwhile, maintaining normal histamine content also depends on the histamine recyclin

• br Experimental section br Introduction Fasting hyperglycaem

  2021-11-01

  

  Experimental section Introduction Fasting hyperglycaemia in all forms of diabetes mellitus occurs primarily as a result of upsurge in hepatic glucose synthesis (HGS) [1], [2]. Two specific enzymes, glucokinase (GK) and glucose-6 phosphatase (Glu-6-Pase) play crucial role in hepatic glucose pro

• We speculated modulation of redox balance in

  2021-11-01

  

  We speculated modulation of redox balance in brain, by activation of GIP receptor pathway. QA is known to mediate production of ROS, lipid peroxidation by its interactions with Fe2+ and formation of QA-Fe2+ complex (Braidy et al., 2010, Rios and Santamaria, 1991, Stipek et al., 1997). QA induces NOS

• According to the aforementioned preclinical

  2021-11-01

  

  According to the aforementioned preclinical and clinical data, GHS-R1a blockade appears to be a potential pharmacological approach to treat AUD. Given that GHS-R1a has high constitutive (ligand-independent) activity, inverse agonism of the receptor may exert more potent and desirable effects than pu

• Introduction G quadruplexes are therapeutically important

  2021-11-01

  

  Introduction G-quadruplexes are therapeutically important non-canonical nucleic pak1 structures that are formed by a planar assembly of four guanines, termed G-tetrads (Fig. 1), in the guanine rich regions of genome [[1], [2], [3]]. As it is getting increasingly established, several life forms inc

• This hypothesis is in line with

  2021-11-01

  

  This hypothesis is in line with our phylogenetic analysis of FBPase sequences which revealed that vertebrate FBP2 evolved significantly faster than FBP1 (Fig. 2). An average distance between FBP2 and ancestral vertebrate FBPase was higher than that for FBP1. Moreover, preliminary study on amphibia

• To evaluate the role of increased FPPS expression in

  2021-11-01

  

  To evaluate the role of increased FPPS expression in paclitaxel-treated cells, we investigated the effects of FPPS on hiv fusion inhibitors progression. DNA content analysis showed that the number of cells accumulating in the G/M phase increased in a dose-dependent manner in paclitaxel-treated cell

• Furthermore a direct thiol protective role

  2021-10-29

  

  Furthermore, a direct thiol protective role of S-nitrosylation has been reported in animals [66]. Here, formation of higher order irreversible oxidative modifications, such as sulfinic and sulfonic acids were prevented by S-nitrosylation. All these observations underline the important role of ROS in

• In summary through medicinal chemistry

  2021-10-29

  

  In summary, through medicinal chemistry design and computer-assisted conformational modeling, the initial lead was evolved into a series of dihydrobenzofuran derivatives, , as potent GPR119 agonists. Optimization of general structure at various regions of the molecule, including the substituent on

• The global spread and ever

  2021-10-29

  

  The global spread and ever-increasing incidence of metabolic syndrome over the past few decades has not only categorized it as an ‘epidemic’ but has also dramatically increased the risk of cardiovascular diseases and diabetes. The increase in prevalence of diabetes in the United States alone has bee

• br Concluding Remarks br Outstanding Questions br Acknowledg

  2021-10-29

  

  Concluding Remarks Outstanding Questions Acknowledgments Research on DNA glycosylases in our laboratory is supported by the National Science Foundation (MCB-1517695). A.A.R. and N.P.B. are supported by the National Science Foundation Graduate Research Fellowship Program (DGE-1445197). In

• The fine interplay among post translational

  2021-10-29

  

  The fine interplay among post-translational modifications and intersection with other pathways, such as PI3K–AKT, has a crucial role in the regulation of GLI activity and in the generation of their repressor forms 40, 41, 42. In addition to β-TrCP, for example, other E3 ligases belonging to the real

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