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Several dehidropregnenolone derivatives functionalized at C
2023-12-11
Several 16-dehidropregnenolone derivatives functionalized at C3, C4, C5 and C6 (Fig. 7) were prepared and evaluated as 5α-reductase inhibitors bearing in mind that after the formation of an enzyme-steroid complex a nucleophilic portion of the enzyme attacks the double bond of the steroid through Mic
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On the other hand there were
2023-12-11
On the other hand, there were only a few cases that expressed DA2R in our study. Additionally, in the cases whose ACTH-secreting pituitary adenomas expressed DA2R, the ratio of positive staining Epinephrine HCl was very low. This suggests that dopamine agonists may be less effective in canine Cushi
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Arginase deficiency is a rare urea cycle disorder
2023-12-11
Arginase deficiency is a rare urea cycle disorder with hyperargininemia and profound neurological impairment as hallmark features. Arginase-1-deficient mouse models have been created, and they exhibit a profound lethal phenotype approximately 2 weeks after birth in the global knockout (KO) mice or a
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In addition to attracting immune cells to
2023-12-11
In addition to attracting immune cells to the site of injury, ROS also participate in proliferative responses during compensatory proliferation and regeneration. In Xenopus tadpoles, tail amputation induces sustained production of ROS over the span of regeneration, and decreasing ROS levels, especia
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br Concluding remarks and future perspectives While the
2023-12-11
Concluding remarks and future perspectives While the rational engineering of protein-based switches has yet to be fully developed, emerging empirical rules facilitate the construction of tailor-engineered artesunate with custom input and output parameters. Both in the context of molecular diagno
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br A and tau in
2023-12-11
Aβ and tau in Alzheimer's disease The two classical histopathological hallmarks of AD are extracellular insoluble Aβ deposits, known as Aβ plaques, and intracellular accumulations of insoluble microtubule-associated tau protein, known as neurofibrillary tangles [14]. Aβ peptides are produced as a
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Notably we have characterized the mechanism
2023-12-11
Notably, we have characterized the mechanism of action of ALK in the context of our current understanding of NLRP3 activation [5]. Non-priming macrophages, including BMDMs, exhibit no or minimal activation of NLRP3 in response to ATP. In contrast, LPS priming of macrophages makes them highly suscept
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HsALDH enzyme has been purified
2023-12-11
HsALDH enzyme has been purified for the first time in our laboratory from human saliva and has been kinetically characterized using different aromatic substrates [35]. Also, the effect of some common substances frequently encountered by the enzyme in the oral cavity (such as ethanol, hydrogen peroxi
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The numbers and types of
2023-12-11
The numbers and types of molecules needing to be transported across membranes are very large, and there is a corresponding very large and diverse number of transporters expressed throughout the body. Hundreds of proteins that have been assigned as having transporter function are broadly divided into
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br Author contributions br Acknowledgements We
2023-12-11
Author contributions Acknowledgements We thank Dr. Bob Hammer and the Transgenic Core Facility at UTSW for the generation of the transgenic lines, John Shelton and the Histology Core for assistance with histology and the UTSW Metabolic Core Unit for help in phenotyping. We acknowledge support
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sVRPs were more sensitive to ABT
2023-12-08
sVRPs were more sensitive to ABT-702 than MSRs. This result agrees with previous reports that the activation of A1 receptors more potently inhibits sVRPs than MSRs (Nakamura et al., 1997, Otsuguro et al., 2009). Importantly, sVRPs are thought to reflex C-fiber-evoked nociceptive transmission. Nocice
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Based on the improved characteristics of the mutant ECDs
2023-12-08
Based on the improved characteristics of the mutant ECDs we proceeded to crystallization trials, starting with the β1-BPloop as the most promising. We obtained rod shaped hexagonal crystals reproducibly, but with moderate diffraction ability (Fig. 5). Furthermore, the crystals were sensitive in moun
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Bioactive peptides contain amino acids
2023-12-08
Bioactive peptides contain 2–20 amino acids with possible bioactivities including antihypertensive, antioxidant, antimicrobial, anticancer, and opioid activity [9], [10], [11]. There has been a great interest in antihypertensive peptides for their efficiency in lowering blood pressure. The antihyper
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The first natural product described
2023-12-08
The first natural product described as 5-LO inhibitor was the polyphenol nordihydroguaiaretic MPTP hydrochloride from the Mexican dessert plant Larrea divaricata in 1981 (Bokoch and Reed, 1981), short after the initial identification of 5-LO in 1979 (Borgeat and Samuelsson, 1979). Long time before
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Docking studies were performed on the selected compounds to
2023-12-08
Docking studies were performed on the selected compounds to explore their binding patterns and to examine SAR in more detail. The co-crystal structure of ATX in complex with PF-8380 (PDB code: ) was selected for the docking studies due to structural similarity of the most potent compound with PF-83
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