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PGE exerts its functions by binding
2021-07-02
PGE2 exerts its functions by binding to different receptors. Four different subtypes of PGE2 receptors are found in mammals and are designated as EP1-4. These are G-protein coupled receptors that belong to a family of seven rhodopsin-like transmembrane spanning receptors. They are structurally diffe
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br Conflict of interest statement br References
2021-07-02
Conflict of interest statement References and recommended reading Papers of particular interest, published within the period of review, have been highlighted as: Acknowledgements We acknowledge financial support by the Swiss State Secretariat for Education, Research and Innovation (Federal
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Information on the mechanism by
2021-07-02
Information on the mechanism by which parasite infections promote ECM degradation is limited (McKerrow et al., 1983; Andrade, 1994; Lu and Lai, 2013; Thibeaux et al., 2014). The interaction of plasminogen-plasmin with proteins of microorganisms, including bacteria, has been suggested to play a key r
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Using HPLC and an amino acid sequencer the site of
2021-07-02
Using HPLC and an amino GSK180 sale sequencer, the site of cleavage into the fluorogenic substrate AbzFRQEDDnp, determined as specific to the endopeptidase STH2, was analyzed and identified as being R2-Q3, and into substrate AbzFGQEDDnp, determined as specific to SH1, it was G2-Q3 (Fig. 5, Fig. 6).
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We have reported previously that aminoacrylate
2021-06-29
We have reported previously that β-aminoacrylate derivatives of the general structure () are inhibitors of DHODH. In particular, tricyclic derivatives and displayed sub-micromolar IC values against DHODH, and in the case of there was a 1000-fold greater potency compared to the human enzyme (DHODH).
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br Concluding remarks A crucial step
2021-06-29
Concluding remarks A crucial step in the microbial degradation of steroids is the 1(2)-dehydrogenation of the steroid nucleus by FAD-dependent Δ1-KSTDs. This step is required to initiate the opening of the steroid nucleus under both aerobic and anaerobic conditions. A large variety of steroid-deg
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Previous studies showed that many
2021-06-29
Previous studies showed that many steroidogenic enzymes act when the enzyme binds to the cofactor first [30]. In the present study, we showed that HPTE inhibited both AKR1C14 and RDH2 in a mixed mode when cofactor was used. This indicates that HPTE interferes with cofactor-binding residues although
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br Chagas disease and HAT drug R D Drug R
2021-06-29
Chagas disease and HAT drug R&D Drug R&D for Chagas disease and HAT has historically relied on serendipitous findings achieved using low-technology approaches. The absence of biotechnology tools associated and the very limited understanding of the biomolecular processes of the parasites are among
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Dexamethasone DEX a potent synthetic glucocorticoid drug
2021-06-29
Dexamethasone (DEX), a potent synthetic glucocorticoid drug, is effective for treatment of a range of inflammatory and autoimmune conditions as well as the reduction of side effects associated with chemotherapy. On the Czech Republic pharmaceutical market, DEX is incorporated into eighteen drugs use
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Compounds and were outliers for this equation being
2021-06-29
Compounds and were outliers for this equation being the two most reactive compounds. The presence of outliers implies that other factors or specific mechanisms are involved in their chemical hydrolysis. Generally urea derivatives prove to be highly stable in aqueous solutions in vitro. Additional
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CPI-203 The substitution of serine by an
2021-06-28
The substitution of serine 185 by an alanine led to an increase of EGF-R stabilization along with a better binding of PRK1, a RhoB effector described to be involved in EGF-R intracellular traffic. Overall these data indicated that the phosphate group on serine 185 impaired its binding to the effecto
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The CLC proteins in Arabidopsis have been studied in
2021-06-28
The CLC proteins in Arabidopsis have been studied in some detail, and a total of seven genes (named AtCLCa-AtCLCg) have been identified (Lv et al., 2009). It is interesting that AtCLCa-AtCLCd and AtCLCg define a distinct phylogenetic branch that is closely related to eukaryotic CLCs, while the othe
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The small intestine in addition to its primary role
2021-06-28
The small intestine, in addition to its primary role of absorption, has the ability to metabolize drugs and other xenobiotics through phase 1 and phase 11 metabolisms [25] since almost all the cytochrome P450 ANP (1-11), rat synthesis present in the liver are also present in the small intestine alth
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br Conclusions br Acknowledgment br Introduction The role of
2021-06-28
Conclusions Acknowledgment Introduction The role of cholesterol metabolism during multiple sclerosis (MS) is debated and the underlying physiopathology largely unknown. Dyslipidaemia is associated with worsening inflammatory activity and MS disease progression [1], [2], [3]. In the mouse m
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br Conflicts of interest br Acknowledgements br Introduction
2021-06-28
Conflicts of interest Acknowledgements Introduction Atherosclerosis is the number one cause of death in the United States and among the leading causes of morbidity and mortality globally [1]. Inflammation is critical in all stages of atherosclerosis from the formation of a plaque in the ves
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