• BHQ Introduction G quadruplexes are therapeutically importan

  2022-02-03

  

  Introduction G-quadruplexes are therapeutically important non-canonical nucleic BHQ 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 incl

• br Experimental br Acknowledgments br Human

  2022-02-03

  

  Experimental Acknowledgments Human immunodeficiency virus-1 (HIV-1) is the causative agent of acquired immunodeficiency syndrome (AIDS), and without treatment results in a debilitating disease that cripples the immune system of the patient, increasing susceptibility to opportunistic diseases

• br To explore further the functional impact

  2022-02-01

  

  To explore further the functional impact of the similarity of the UTY and KDM6A proteins, the FANTOM5 human dataset was analysed to determine whether or not the genes were expressed at the same time in the same tissues (which would suggest that they are controlled by the same regulators) or with o

• The neurotransmitter histamine plays a key

  2022-02-01

  

  The neurotransmitter histamine plays a key role in the sleep-wake cycle and in learning and memory. Alterations in gap 27 histamine levels are closely connected with central nervous system dysfunction, and are thought to contribute to neurological disorders, including Alzheimer's disease and depress

• In addition to lifestyle factors

  2022-02-01

  

  In addition to lifestyle factors, genetic factors may also influence the efficacy of antineoplastic drugs in breast cancer patients.16, 17 The HER2 gene contains several single nucleotide polymorphisms (SNPs). Two of the most investigated HER2 SNPs are Ile655Val (rs1136201) and Ala1170Pro (rs1058808

• In contrast to sGC stimulators sGC activators

  2022-02-01

  

  In contrast to sGC stimulators, sGC activators promote enzymatic activity of sGC containing oxidized heme iron (Fe3+) or missing the heme group. A-350619 is one of the oldest activators of sGC to be discovered. A-350619 increased sGC activation in a non-additive manner with respect to YC-1, leading

• Selected GSNOR inhibitors were assessed

  2022-02-01

  

  Selected GSNOR inhibitors were assessed for potential off-target activity with a panel of 54 transmembrane and soluble receptors, ion channels, and monoamine transporters. Off-target effects were estimated from the percent inhibition of receptor radio-ligand binding in the presence of 10μM of test c

• br Conclusions br Acknowledgements The

  2022-02-01

  

  Conclusions Acknowledgements The authors thank Matt JM Wood and colleagues (AstraZeneca, UK) for permission to use logD and protein binding data presented in Sup. Table S2. Introduction The number of people suffering from type 2 diabetes mellitus (T2DM) has escalated worldwide as a consequ

• GPR is a member of

  2022-02-01

  

  GPR119 is a member of the G protein-coupled receptor family, and is highly expressed in pancreatic β-cells and intestinal endocrine cells. It has been proposed that GPR119 agonists modulate glucose homeostasis by indirectly stimulating glucose-dependent insulin release through enhancing pancreatic c

• Both GPR A and GPR are located on chromosome q

  2022-02-01

  

  Both GPR109A and GPR81 are located on chromosome 12q24 [3] and mediate anti-lipolytic effects through coupling to Gi-type G proteins [17]. It is important to note that with the recent deorphanization of these receptors, there has been a recommendation to the International Union of Basic and Clinical

• br Inclusion exclusion criteria br Quality assessment All st

  2022-02-01

  

  Inclusion/exclusion criteria Quality assessment All studies included in the qualitative synthesis were evaluated using the Quality Assessment Tool for Quantitative Studies (QATQS), which allows to determine their methodological quality. QATQS assesses 8 sections: selection bias, study design,

• br Introduction Cherry tomato Solanum lycopersicum L is a

  2022-02-01

  

  Introduction Cherry tomato (Solanum lycopersicum L.) is a commonly consumed fruit on a worldwide scale due to its characteristic flavor and high nutrition (Wei et al., 2016, Yu et al., 2014). Tomato is low in fat and calories, and is a rich natural source of nutrition and bioactive antioxidant co

• br Genetic manipulation variation of

  2022-01-31

  

  Genetic manipulation/variation of the ghrelin system and alcohol-related outcomes Genetic manipulation of the ghrelin system (either the peptide or the receptor gene) via knockout rodent models has provided further insight into the role of this system in alcohol seeking and consummatory behaviors

• Some aspects of intercellular Ca wave spread are similar

  2022-01-31

  

  Some aspects of intercellular Ca2+ wave spread are similar to the phenomenon of spreading depression and associated with migraine headache [57]. These depolarization waves, followed by electrical inhibition, are evoked by transient hypoxia and other types of middle-aged injury and spread slowly acr

• One effective approach to fine tuning the lipophilicity

  2022-01-31

  

  One effective approach to fine-tuning the lipophilicity profile of FFA1 agonists is to ‘decorate’ the 3-phenylpropahoic ghrelin receptor scaffold with polar heterocyclic moieties. Alternatively, this scaffold could be replaced with heterocyclic isosteres (as in Takeda’s compounds 1,2 and 3 as well

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