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Pharmacological inhibition of PKR seems to
2022-02-09
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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In fact most PIs are susceptible to
2022-02-09
In fact, most PIs are susceptible to substitutions at Asp168, which are often present in patients who fail therapy (Pawlotsky, 2016). Notably, the polymorphism Gln168 at this position underlies reduced efficacy of PIs against GT3 (Soumana et al., 2016a). Glecaprevir and voxilaprevir have improved re
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br NO GC pathway and implications for glaucoma Direct in
2022-02-09
NO-GC-1 pathway and implications for glaucoma Direct in vivo measurement of NO in the eye is not yet feasible. However, measurement of nitrate and nitrite levels are routinely used as markers for the activity of NOS and the production of NO radicals [98]. Several studies in human glaucoma patient
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Through the analysis of various synthetic GPR agonists as
2022-02-08
Through the analysis of various synthetic GPR40 agonists as reported in literature, we found that a number of these compounds contained a phenylpropanoic Carbidopa motif which was inspired from naturally occurring medium to long chain fatty acids. For instance, in the early period of discovering TA
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br Acknowledgments We would like to acknowledge Jenna Hall
2022-02-08
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 Results br Discussion Immune mediated chronic inflammator
2022-02-08
Results Discussion Immune-mediated chronic inflammatory diseases (e.g. rheumatoid arthritis, psoriasis, multiple sclerosis, and inflammatory bowel disease) are characterized by a dysregulated migration of leukocytes from blood vessels into inflamed tissues. To date, several new targets and inh
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Recent evidence indicates that prolonged vasoconstriction of
2022-02-08
Recent evidence indicates that prolonged vasoconstriction of conductance and resistance arteries involves VSMCs THZ1 Hydrochloride polymerization, through activation of small GTPases [4] and a subsequently transition to a more solid rheology [5]. Actin polymerization occurs in two steps, nucleation
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Recently they reported an enyne chemotype agonist
2022-02-08
Recently, they reported an enyne chemotype agonist (21, Fig. 13) with low lipophilicity, small polar surface area (PSA) and high potency (Clog P=3.8, tPSA=37 A2, EC50=20nM), further derived from TUG-424. The compound endowed fast oral meclofenamate (tmax=15min) and a decent pharmacokinetic profile,
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p53 tumor suppressor br Conclusions H K demethylases
2022-02-08
Conclusions H3K27 demethylases perform an important catalytic function in mediating change in gene expression, whether it is during cell differentiation or activation, because they remove repressive marks from histones which opens the chromatin and facilitates transcription. The number of publica
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Freinkel first reported in the late s that maternal hypertri
2022-02-08
Freinkel first reported in the late 1960s that maternal hypertriglyceridemia benefits the fetus during starvation by increasing maternal consumption of triglyceride for ketone body synthesis giving the basis for “accelerated starvation” theory [4,5]. This maternal metabolic reprogramming during peri
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Based on our results we propose three possible mechanisms
2022-02-08
Based on our results, we propose three possible mechanisms of HER2 loss after trastuzumab-based therapy (Fig. 3). The first possibility is a result of the differential effects of treatments on clonal subsets. In breast cancer, such selective pressure has been suggested to preferentially eradicate HE
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marizomib In this precancerous condition though cancer devel
2022-02-08
In this precancerous condition, though cancer develops from the epithelium, the subepithelial connective tissue also play crucial biological role in pathogenesis and progression to malignancy. In this context it may be noted that some recent reports addressed the problem of the mechanical interactio
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br Molecular mechanisms underpinning GSNOR function in the d
2022-02-08
Molecular mechanisms underpinning GSNOR1 function in the defence response Recently, Arabidopsis GSNOR1 has been shown to govern the extent of S-nitrosylation of two key regulatory proteins, Non-Expresser of Pathogenesis-Related Genes 1 (NPR1) and SA binding protein 3 (SABP3), which are integral t
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Curcumol As natural ligands of GPR
2022-02-08
As natural ligands of GPR120, several long chain polyunsaturated fatty acids (Lc-PUFAs) have been demonstrated to modulate the 3T3-L1 adipogenic differentiation. However, the effects of the Lc-PUFAs are inconclusive. DHA is shown to inhibit, promote or even not affect the differentiation of preadipo
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br Materials and methods br Results
2022-02-07
Materials and methods Results Discussion Heart hypertrophy is initially physiological to compensate for the loss of heart functions. However, sustained stresses lead to a pathological status, in which myocardium becomes stiffened by interstitial fibrosis and thereby diastolic dysfunction in
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