• Previously we have shown that ghrelin

  2022-07-13

  

  Previously, we have shown that ghrelin and cannabinoids stimulate hypothalamic AMPK activity (Kola et al., 2005). In contrast, both the orexigenic compounds have inhibitory effects on AMPK activity in the liver and visceral fat (Kola et al., 2005). In this study, we were able to reproduce our previo

• Active compounds and were further tested and EC

  2022-07-12

  

  Active compounds , , and were further tested and EC and pEC values were determined as shown in . Compound showed EC of 0.97μM (pEC 6.01) with 84.5% maximal response, which suggests that introduction of alkyl chain on aromatic nucleus of , resulted in improved GPR40 agonistic activity than that of (E

• As a part of our continuing efforts towards discovery

  2022-07-12

  

  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

• Overall we partially confirmed our predictions

  2022-07-12

  

  Overall, we partially confirmed our predictions, and, when compared to the other existing dataset exploring the interaction among CRFR1, FAAH, and anxiety, our data are somewhat confirmatory. Demers and colleagues (Demers et al., 2016) found one (protective) CRFR1 minor allele (rs110402) and the (le

• gsk525762 Not only has the cortical actin

  2022-07-12

  

  Not only has the cortical gsk525762 network been found to influence plasma membrane properties but also to interact with exo- and endocytic vesicles (Gormal et al., 2015, Tomatis et al., 2013). The interplay between actin and membranes is integrally regulated by the phosphoinositide composition of

• br Methods br Results We have

  2022-07-12

  

  Methods Results We have previously used ß-hex assays in HeLa omadacycline to study the role of lysosomal exocytosis on transition metal clearance and the effects of transition metals on lysosomal exocytosis [26], [29], [40]. ß-hex is a lysosomal enzyme, the delivery of which to the extracellu

• Recently the toxicity of TBT was

  2022-07-12

  

  Recently, the toxicity of TBT was demonstrated at the vascular level in animal models (Nath, 2008), and the results obtained so far suggest that TBT may be a potential risk factor for cardiovascular diseases. TBT is capable to alter the coronary vascular reactivity to estradiol (dos Santos et al., 2

• The multiple regression analysis showed that testing during

  2022-07-12

  

  The multiple regression analysis showed that testing during summer and autumn was associated with higher histamine reactivity, which could be associated with the presence of pollen in the air. Gamboa et al. reported that more histamine was released during spring and autumn than during the other two

• Based on pharmacophore modeling a good HDAC inhibitor

  2022-07-12

  

  Based on pharmacophore modeling, a good HDAC inhibitor has at least three sides/regions: the attachment side of the Zn2+ cofactor/HDAC active site (Zn2+ binding group/ZBG), hydrophobic cap (CAP) and linker containing connecting unit (CU) with electronegative groups (Mohan et al., 2011, Rossi et al.,

• br Conclusion and future perspectives

  2022-07-12

  

  Conclusion and future perspectives The nicotinic PHA-680632 receptor receptor GPR109A and its close relatives GPR109B and GPR81 are primarily expressed in adipocytes and are coupled to Gi-type G proteins. Recently, the ketone body β-hydroxy-butyrate, the β-oxidation intermediate 3-hydroxy octano

• Although it is currently unknown why the longer splice varia

  2022-07-12

  

  Although it is currently unknown why the longer splice variant found in the human has not been found in any other species, similar results have been reported for other receptors, including the NSC 319726 receptor splice variant ERbeta2 identified in human and primate, but not other species (Sierens

• Our exploration of Domain focused on the role of the

  2022-07-11

  

  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

• AFB Fapy dG has been long recognized as a

  2022-07-11

  

  AFB1-Fapy-dG has been long recognized as a substrate for nucleotide excision repair [24,25]. However, we recently demonstrated that this lesion is removed by mecamylamine excision repair. We showed that DNA glycosylase NEIL1, a member of the Fpg/Nei glycosylase family, could excise AFB1-Fapy-dG fro

• An alternative to the chemoenzymatic preparation of

  2022-07-11

  

  An alternative to the chemoenzymatic preparation of glycoproteins is the production through total chemical synthesis or semi-synthesis [2,3,]. Many successful glycoprotein syntheses are based on native chemical ligation (NCL) [11], a reaction where unprotected peptides and glycopeptides of any lengt

• Crystal structures from soluble E

  2022-07-11

  

  Crystal structures from soluble E2 constructs (Khan et al., 2014; Kong et al., 2013) have revealed globular protein with no regular structure in spite of having eight disulphide bonds (Kong et al., 2013). Although 62% of the protein exists in loops or disordered structures, overall it was well-defin

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