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DMOG Previous studies from our lab looked at
2019-09-16
Previous studies from our lab looked at the effect of interfering with crossover helix interactions in TS-DHFR. One study utilized peptide mimetics of the crossover helix to inhibit wild-type TS-DHFR noncompetitively, and with an IC of 230 μM. A second study used a virtual screening approach to iden
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Dehydrogenation by a KSTD is also a
2019-09-16
— 1(2)-Dehydrogenation by a Δ1-KSTD is also a crucial step during 4-HQN mass degradation of the steroid core. Several Δ1-KSTDs were shown to be active under either aerobic or anaerobic conditions [27,29,47,50,66]. Furthermore, the last common intermediate of both aerobic and anaerobic steroid degrad
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Imidazo purine diones were another cluster of
2019-09-16
1-Imidazo[2,1-]purine-2,4(3,8)-diones were another cluster of compounds identified from the Chembridge screen (). A benzyl group at the R2 position was preferred over a phenyl or 2-phenylpropyl (. and ), and -substitution of the benzyl group increased potency to the nanomolar level ( IC=0.20μM . ).
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It has been reported that
2019-09-16
It has been reported that CysLT2 receptors negatively regulate CysLT1 receptor-mediated response in allergic airway inflammation in mice. Knockdown of CysLT2 receptors augmented CysLT1 receptor-mediated mast cell proliferation [31] and eosinophilic airway inflammation induced by antigen challenge in
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Enzyme mimics belong to a type of rising catalysts which
2019-09-12
Enzyme mimics belong to a type of rising catalysts which show the similar function with their corresponding natural enzymes [20], [21], [22], [23], [24], [25], [26], [27], although their structures are different from natural enzymes. In the area of prodrug activation, the widely-used enzyme mimics a
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flumethasone br Mechanisms of acquired resistance to st
2019-09-12
Mechanisms of acquired resistance to 1st and 2nd generation EGFR inhibitors After treatment with first or second generation EGFR TKIs, virtually all patients after approximately 12 months develop acquired resistance (AR). Different mechanisms of AR to EGFR TKIs have been reported to date and may
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Pharmacogenomics is the study of the
2019-09-12
Pharmacogenomics is the study of the role of the cantharidin in drug response. It was reported that the effectiveness of atorvastatin was affected by genetic factors.26, 27 In previous studies, there are many genetic polymorphisms related to the efficacy of atorvastatin. Cerda et al reported that S
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The quantification and monitoring of ChEs enzymatic
2019-09-12
The quantification and monitoring of ChEs enzymatic activities have traditionally been associated to environmental studies in order to diagnose the exposure of non-target organisms to specific anti-cholinesterasic agents (Nunes, 2011). The importance of these enzymes as biomarkers of environmental c
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br Materials and methods br Results br
2019-09-12
Materials and methods Results Discussion In this study, we confirmed the activation of Akt by udenafil in 3T3-L1 cells. To elucidate the underlying mechanism of udenafil, we focused on the mitochondria. Our findings demonstrated that udenafil improved mitochondrial function and expression o
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Grapiprant is a selective antagonist for prostaglandin
2019-09-12
Grapiprant () is a selective antagonist for prostaglandin E (PGE) receptor subtype 4 (EP4) identified as a clinical candidate for the treatment of inflammatory pain associated with osteoarthritis (OA). It is currently under development for use in humans and dogs. The projected dosing regimen of grap
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As illustrated in Table monocyclic acid analogs were synthes
2019-09-12
As illustrated in Table 3, monocyclic Protease Inhibitor Cocktail (EDTA-Free, 100X in DMSO) analogs were synthesized and evaluated. 2-Oxido-3H-1,2,3,5-oxathiadiazol analog 8 showed 15-fold less potent EP1 receptor affinity relative to 2b, while it showed 2.2-fold more potent antagonist activity. Ox
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br Methods br Discussion In a recent survey among high
2019-09-11
Methods Discussion In a recent survey among 2625 high risk patients on atorvastatin, 10.5% of patients achieved an LDL-target of Adenosine level for improvement of acceptance and adherence to effective lipid lowering therapy are warranted to maximize the benefits of standard treatment options
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In the previous study glutamyl endopeptidase of B intermediu
2019-09-11
In the previous study glutamyl endopeptidase of B. intermedius has been reported to be distributed in the (±)-Nutlin-3 and of B. intermedius as follows: 90% of synthesized enzyme has been detected in the culture liquid, 9.3% of glutamyl endopeptidase—in the fraction of membrane proteins [20]. The d
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The expression of EBI has been found to be dysregulated
2019-09-11
The expression of EBI2 has been found to be dysregulated in several types of B cell malignancies and is thus reduced in e.g. diffuse large B-cell lymphomas [12] and chronic lymphocytic leukemia [13] and increased in post-transplantation lymphoproliferative disorders (PTLDs) [14]. EBI2 is also highly
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Regardless of its effect on EBV infection the chemokine
2019-09-11
Regardless of its effect on EBV infection, the chemokine system has been found to be regulated in both nasopharyngeal cancer and Hodgkin lymphoma. As such, Hodgkin and Reed–Sternberg (HRS) cells from Hodgkin lymphoma and nasopharyngeal carcinoma cells have been shown to express CXCL8 and CCL17. Furt
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