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keap1 nrf2 br Polymorphic variation ERAP is polymorphic and
2024-11-15
Polymorphic variation ERAP1 is polymorphic and several single nucleotide polymorphisms (SNPs) in its gene that encode amino keap1 nrf2 changes have been associated with predisposition to a variety of diseases, ranging from viral infections to cancer and autoimmunity (Alvarez-Navarro and Lopez de
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Aldicarb Some of the mechanisms that involve LOX
2024-11-15
Some of the mechanisms that involve 12-LOX as a potential pathogenic enzyme are illustrated in Fig. 2. Direct β cell effects associated with the stimulation of 12-LOX activity include the activation of second messengers c-Jun N-terminal kinase and p38 MAPK, both of which show increased phosphorylati
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The lactam emerged as lead candidate due to its
2024-11-15
The lactam (6) emerged as lead candidate due to its high selectivity, outstanding potency (against ALK or in clinically known ALK mutants), low in vitro clearance, and low efflux potential. The lactam (6) was selected for further profiling against the resistant ALK mutants. Preclinical rat pharmacok
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It thus appeared reasonable that AR needed to be
2024-11-15
It thus appeared reasonable that AR needed to be inhibited and great experimental efforts began which are still on-going [6]. Indeed, hundreds of ARIs have been characterized but no significant drug development has followed. The case of Sorbinil, which did not pass clinical trials is emblematic [7]
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Ginsenosides are the major bioactive constituents of the Pan
2024-11-15
Ginsenosides are the major bioactive constituents of the Panax ginseng root, which contain many types of ginsenosides including Rb1, Rg1, Rc, and Rg3. The ginsenoside Rb1 appears to be the most abundant of the bioactive ginsenosides [15]. Rb1 exhibits antiinflammatory, anticarcinogenic, and antioxid
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The rank order of agonist potency in turkey
2024-11-15
The rank order of agonist potency in turkey cardiac chambers demonstrated the predominant presence of the β-adrenergic receptor subtype, in line with the receptor classification by . However, a previous radioligand binding study in the left ventricles of 7-week old turkeys reported the existence of
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Lipotoxicity is the accumulation of excess lipids
2024-11-15
Lipotoxicity is the accumulation of excess lipids in non-adipose tissues that leads to cell dysfunction or cell death. It may play an important role in the pathogenesis of diabetes, and contributes to the rate of progression of CKD [7,8]. Emerging evidence indicates that renal lipid dysregulation is
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Etomoxir The second evidence comes from
2024-11-15
The second evidence comes from the results obtained by patch-clamp recordings carried out at the endplate region of isolated mouse FDB fibers, where adenosine and the P1R agonist NECA significantly affected the NPo, the open frequency and the time constant τ of the adult nAChR channels. It is genera
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In the olfactory bulb expression was
2024-11-15
In the olfactory bulb, expression was especially prominent in the mitral cell layer from embryonic stages to adult tissues (Figs. 1D–G). By E14–E16, Ack1 signal was remarkably intense in the proliferative ventricular zone (Fig. 1D). From E18 to adult, expression was also observed in glomerular and g
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Kif15-IN-2 br Funding br Introduction The interest in the ef
2024-11-14
Funding Introduction The interest in the effects of endocrine disrupting chemicals (EDCs) in the aquatic environment continues to increase over the past decade, specifically those that act on steroidogenic pathways. EDCs that include synthetic androgenic and estrogenic compounds can severely
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Song et al reported series of triazolylsalicylamide
2024-11-14
Song et al. reported series of 1,2,3-triazolylsalicylamide derivatives and screened over kinase panel and found compound 31 as most potent which inhibited Aurora-A, specifically with IC50 of 0.37 μM. Compound 31 was about 10-fold more active for Aurora-A than for Aurora-B (IC50 = 3.58 μM reported se
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b catenin inhibitor V ATPase is a complex enzyme that
2024-11-14
V-ATPase is a complex enzyme that is composed of several subunits, which are assembled into two domains: trans-membrane (V0) and cytosolic (V1) domains [3,5]. Epididymal epithelial b catenin inhibitor of rats has been reported to contain V-ATPase which is distributed at the apical pole of the narrow
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The LO has so far only been found
2024-11-14
The 15-LO-1 has so far only been found in humans and rabbit reticulocytes [3], [20] and the rabbit 15-LO-1 protein demonstrate 81% identity to the human 15-LO-1. However, rabbit monocytes express an enzyme with mainly 12-LO activity [20], [21]. The high degree of sequence conservation between these
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BMS354825 To further investigate the role of cholesterol in
2024-11-14
To further investigate the role of cholesterol in the Rh2-induced cytotoxicity, we then focused on the U937 cell line, which is cholesterol auxotroph and considered as a valuable model to study the importance of cholesterol in membrane structure and function (Billheimer et al., 1987), and used the e
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br STAR Methods br Author
2024-11-14
STAR★Methods Author Contributions Acknowledgments We thank Craig D. Wenger and Neva C. Durand for helpful advice, guidance, and discussions. D.H.P. is supported by the NIH National Human Genome Research Institute (NHGRI) (grant R00HG008662) and the Damon Runyon Cancer Research Foundation (D
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