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Consistent with the observation that mutations
2023-01-13
Consistent with the observation that mutations in the redox-partner binding site of P450c17 that reverse charge from basic to acidic (R347H, R358Q) cause 17,20-lyase deficiency (Geller et al, 1997, Geller et al, 1999), at least one POR mutation that changes a residue in the FMN domain from neutral t
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The Type A series contains
2023-01-13
The Type-A series contains 6 of the 11 confirmed hits, making it a highly attractive lead template. Seven (7) out of 8 Type-A series of 3-substituted-2-furoic acids are highly active (84–100% inhibition) at the high concentration of 100μM. We could deduce some interesting, albeit preliminary structu
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In HepG cells compound showed inhibition of total lipid synt
2023-01-13
In HepG2 cells, mp 1 synthesis showed inhibition of total lipid syntheses with an IC of 8μM. A cell based Alamar Blue cytotoxicity assay was used in parallel to differentiate the effect on the inhibition of lipid synthesis versus potential cytotoxicity. Under identical incubation conditions, compo
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We wanted to investigate the influence of substituents on
2023-01-13
We wanted to investigate the influence of substituents on the pyrazole ring on the activity, but only a few substituted pyrazole-3-carboxylic acids/esters were commercially available in useful amounts at a reasonable price, for example, 4- and 5-nitro-pyrazole-3-carboxylic acid. The preparation of 4
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br Conflict of interest statement br Introduction
2023-01-10
Conflict of interest statement Introduction Currently, adenocarcinoma is the most common histological subtype of lung cancer. Activating mutations and translocations with a potential for targeted therapy are reported predominantly in non-smokers. ALK rearrangement is found in less than 5% of u
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br Hypothesis The hypothesis is that AhR in
2023-01-10
Hypothesis The hypothesis is that AhR in skin diseases could be an objective of study for future dermatological therapies. Both stimulation and inhibition of the receptor might have significant influences on neoplastic or inflammatory skin diseases. However, at present the functions of AhR are un
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br Material and methods br
2023-01-10
Material and methods Results Discussion To develop a novel regenerative and/or neuroprotective therapy for optic neuropathy, including glaucoma, numerous studies have tested new candidates favorable to RGC survival and axon regeneration. Among the many candidate drugs, AdoR modulators are o
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Compounds were profiled for their inhibitory activity agains
2023-01-10
Compounds – were profiled for their inhibitory activity against dipeptidyl peptidase-IV Activity and/or Structure Homologues (DASH) [e.g. DPP2, DPP8 and DPP9] and non-DASH [eg. post-proline cleaving enzyme (PPCE), neutral endopeptidase (NEP), aminopeptidase P (APP), aminopeptidase N (APN)] enzymes.
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br Author contributions br Competing interests
2023-01-10
Author contributions Competing interests Transparency document Acknowledgments This research was funded by a TOP ZonMW grant (40-00812-98-10054) to R.O.E., a DFG grant (KR4391/1-1) and IZKF Erlangen grant (J36) to A.K. and supported in part by Centro de Investigación Biomédica en Red de
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br Materials and methods br Results br Discussion
2023-01-10
Materials and methods Results Discussion CUs, which have been used as traditional medicine for thousands of years in East Asian countries, have the potential to be used for cancer chemoprevention and chemotherapy [17], [18], [19], [20]. CuB is one of the most promising agents as it is repor
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The LO has so far only been found in
2023-01-10
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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Coincident with APJ receptor several cell types
2023-01-10
Coincident with APJ receptor, several cell types in the body can synthesize apelin protein. For example, the highest apelin concentrations in the body have been found in the rat central nervous system, pituitary gland, lungs, cardiac muscle, gastrointestinal tract and mammary glands, with lower valu
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Bran is a byproduct of
2023-01-10
Bran is a byproduct of flour milling, typically utilized as a valuable component of animal feeds. Because of its attractive technological and health-promoting properties, it INK 128 has also been increasingly used in food manufacturing as a source of dietary fiber. Indeed, with the growing interest
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A strain previously reported as
2023-01-10
A strain previously reported as demonstrating strong antifungal activity and suitability for food applications is Lactobacillus reuteri R29 (Axel et al., 2016, Oliveira et al., 2015). Oliveira et al. (2015) demonstrated that the cell-free supernatant (cfs) of medium fermented for 48 h with this stra
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In the largest postmortem study of autopsied individuals alm
2023-01-10
In the largest postmortem study of 3618 autopsied individuals, almost 75% of the individuals without Aβ pathology already harbored cortical NFT pathology mostly confined to the medial temporal regions (Murray et al., 2015). In Braak's study of 2366 autopsied individuals (Braak and Del Tredici, 2014)
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