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HOs can be found in
2021-12-10
HOs can be found in both plants and animals and they are evolutionarily conserved proteins [8]. There are two HO isoenzymes: inducible heme oxygenase-1 (HO-1) and constitutive heme oxygenase-2 (HO-2) encoded by different genes [9,10]. Biosynthesis of a stress-inducible HO-1 can be triggered by a var
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br Trifluoromethylketones This group of compounds was demons
2021-12-10
Trifluoromethylketones This group of compounds was demonstrated to bind the zinc Raloxifene HCl in the active site due to its easy hydration, forming the required chelating intermediate. Ontaria et al. [92] have proposed variations around the cap group of trifluoromethylthiophene as the core moti
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It is essential to maintain genome integrity and stability w
2021-12-10
It is essential to maintain genome integrity and stability which is assaulted by oxidative stress. To perform this function, all human cells have well developed repair systems. Base excision repair (BER) system is the most effective pathway responsible to revert back lesions caused by oxidative stre
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br Concluding remarks br Introduction The hair cells
2021-12-10
Concluding remarks Introduction The hair MCC950 sodium of vestibular organs detect linear and rotational head movements, providing sensory information that is essential for normal postural and visual reflexes. Most vestibular hair cells are produced during embryonic development, but they can
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Although NCT undergoes complex glycosylation processing for
2021-12-10
Although NCT undergoes complex glycosylation processing for maturation through trafficking from endoplasmic reticulum to Golgi or additional compartments, the effect of NCT glycosylation on γ-secretase activity and substrate specificity is still unknown. The present study focused on glycosylation st
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The GH family has potential applications in various industri
2021-12-10
The GH family has potential applications in various industries. A putative ORF encoding α-galactosidase, namely GalR, with a low identical match and e-value and high query coverage in the metagenome was selected because it demonstrated considerable activity. GalR shared 65% identity with the GH 27 p
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br Methods br Results It is well known
2021-12-10
Methods Results It is well known that during the onset of vasoconstriction there is an increase in intracellular Ca2+ which activates myosin light-chain kinase followed by cycling of actin-myosin cross-bridges in VSMCs. Recently, it has been recognized that aim products polymerization is also
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In conclusion a novel series
2021-12-10
In conclusion, a novel series of GPR40 agonists containing nitrogen heterocyclic rings derived from TAK-875 were designed and synthesized. The structural activity relationship studies indicated that the substituents on the nitrogen tgf beta receptor 1 had a remarkable effect on the GPR40 agonistic a
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Although exhibited high inhibitory activity was
2021-12-10
Although exhibited high inhibitory activity, was found to be metabolically unstable due to the hydrolysis of the phosphate group (data not shown), which prompted us to modify the phosphate moiety of . Comparison of the activities between three compounds bearing no or different spacer groups (, , a
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br Introduction More than structurally different isoprenoids
2021-12-10
Introduction More than 30,000 structurally different isoprenoids, such as steroids, carotenoids, prenyl side-chain of quinones, prenyl proteins, and natural rubber, exist in nature. In a biosynthetic pathway, linear prenyl diphosphates are common structures as a precursor of isoprenoids, as shown
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Chicoric acid CA is a di
2021-12-10
Chicoric gsk3 inhibitor (CA) is a di-acylated hydroxycinnamoyl tartaric acid ester [12] found in a variety of plant species, especially within the Astereceae family [13]. Of interest for this study, Sonchus oleraceus and Bidens pilosa plants, from Astereceae family, were used. Both S. oleraceus and
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Betahistine N methyl pyridyl ethylamine is a well known dual
2021-12-10
Betahistine (N-methyl-2-(2-pyridyl)ethylamine) is a well-known dual H1 CHIR-98014 agonist/H3 receptor antagonist with structural resemblance to histamine. Though it has been approved long before the discovery of H3R to treat disorders of vestibular function as Menières-Disease, the evidence for thi
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Given the overexpression of HO in some
2021-12-10
Given the overexpression of HO-1 in some tumors, such as CML, and its potential involvement in chemoresistance to classical chemotherapeutic agents, compounds 4 and 8f were tested in CML cell lines resistant to IM, a classical TK inhibitor used in CML. Compounds 4 and 8f, in combination with IM, sho
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PBI is an agonist of GPR and acts as an
2021-12-09
PBI-4050 is an agonist of GPR40 and acts as an antagonist or inverse agonist of GPR84. It cannot be excluded that other targets besides GPR40 and GPR84 could be implicated in the mechanism of action of PBI-4050 and could be explored in future studies. However, the present study, and in particular th
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The first described synthetic FFA active
2021-12-09
The first described synthetic FFA1 active agonist, GW9508 (4- [(3-phenoxyphenyl)methyl]amino benzenepropanoic acid), was immediately shown to also activate FFA4, although with some 100-fold lower potency [38]. Therefore, in the initial absence of FFA4-selective synthetic agonist ligands, GW9508 was
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