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Much is known about FPPS
2022-06-09

Much is known about FPPS structure and function, with over 120 FPPS crystal structures being currently available. This wealth of information is largely the consequence of human FPPS serving as a drug target for the treatment and/or prevention of pathologies such as osteoporosis, hypercalcemia and Pa
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In the Medicines for Malaria Venture MMV distributed the Ope
2022-06-09

In 2011 the Medicines for Malaria Venture (MMV) distributed the Open-Access Malaria Box to accelerate antimalarial drug discovery (Spangenberg et al., 2013). The Malaria Box consists of 400 structurally diverse compounds, curated from >20,000 hits generated from large-scale screens, that inhibit the
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Studies have demonstrated the paradoxical role of HO in tumo
2022-06-08

Studies have demonstrated the paradoxical role of HO-1 in tumorigenesis. At initial stages of carcinogenesis, it protects DNA by lowering the ROS-mediated mutational rate, but later, HO-1 promotes cancer cell survival and proliferation. One PDAC therapeutic strategy is to increase ROS production and
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More recently Vismodegib was administered in
2022-06-08

More recently, Vismodegib was administered in combination with Gemcitabine in a pilot clinical trial that enrolled 23 patients affected by metastatic pancreatic adenocarcinoma. This type of malignancy is the most frequent form of pancreas cancer and is ranked in fourth place for cancer mortality in
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The Hardy Weinberg equilibrium was verified in
2022-06-08

The Hardy-Weinberg equilibrium was verified in all groups using the chi-square test. Using WINPEPI 11.65, the number of carriers and non-carriers of the Δ32 allele was compared between the groups through the Pearson's chi-square test with Yates's correction. Two-tailed Fisher's test was used when ap
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Toxoplasma gondii is an exceptionally tractable apicomplexan
2022-06-08

Toxoplasma gondii is an exceptionally tractable apicomplexan parasite that expresses a limited yet representative subset of apicomplexan cyclase orthologs, making it an ideal model for investigating cyclic nucleotide signaling in Apicomplexa. Of the five putative nucleotide cyclases, only TgACα1 and
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br Membrane Fusion Requires Rab
2022-06-08

Membrane Fusion Requires Rab-GTPases, Tethers, and SNAREs Regulation and Function of Rab5 Following endocytosis in metazoan cells, the Rab5-specific GEF Rabex5 binds to ubiquitinated cargo proteins, such as cell surface receptors or metabolite transporters, and subsequently activates Rab5 on e
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Urinary hydroxypyrene OHP is a
2022-06-08

Urinary 1-hydroxypyrene (1-OHP) is a widely used biological marker of exposure to PAHs and indicator for internal dose of activated PAHs (Jongeneelen, 1987, Adonis et al., 2003). PAH metabolites may be excreted either as free or as conjugated compounds. When 1-OHP is measured after treating the urin
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Having identified initial leads and
2022-06-08

Having identified initial leads and (), further lead optimization was initiated on B- and C-rings to afford compounds with improved potency. Initial set of substituted imidazole-biphenyl-carboxylic Thiorphan receptor derivatives – and () were evaluated for GSNOR potency. Among this, fluoro, methyl,
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br Conclusion In conclusion we
2022-06-08

Conclusion In conclusion, we showed that apoptosis is involved in etoposide-induced pancreatic β-cell cytotoxicity. More importantly, as shown in Fig. 6, the results of this study demonstrated that etoposide induces pancreatic β-cell death via the JNK/ERK activation-mediated GSK-3 downstream-trig
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We previously evaluated the immuno modulatory efficacy of GS
2022-06-08

We previously evaluated the immuno-modulatory efficacy of GSNO in different EAE models and reported prophylactic and therapeutic efficacy of GSNO against the clinical disease of EAE [22], [36]. GSNO inhibited the IL-6-induced STAT3 activation (Tyr705 phosphorylation) by S-nitrosylation of the STAT3
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Introduction Substantial body of evidence supports the notio
2022-06-08

Introduction Substantial body of evidence supports the notion that GABA, the dominant inhibitory neurotransmitter in the hypothalamus of mammals, affects GnRH release by two classes of membrane receptors: GABAA (GABAAR) [1] and GABAB (GABAB R) [2]. Studies in rodents and sheep have documented that
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We also explored various nitrogen
2022-06-08

We also explored various nitrogen substituents with an aim toward modulating sterics and basicity within the ABH series. No glycine uptake inhibition was detected with non-basic bicycles (data not shown). Isopropyl was the best compromise between desired on-target effect and clearance, however, eff
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br Methods br Results and discussion
2022-06-08

Methods Results and discussion Protein analysis of commonly used cell lines (C6, D54-MG, U87, U251 and STTG1) reveals high Tipifarnib of SXC (Cho and Bannai, 1990, Ye et al., 1999, de Groot et al., 2005, Lyons et al., 2007, Savaskan et al., 2008). Since protein expression can be altered over
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Regarding the causative diseases of ES patients with unknown
2022-06-08

Regarding the causative diseases of ES, patients with unknown cause and those with encephalitis had significantly higher CSF levels of MK-8776 against GluN2B-NT2 and GluN2B-CT than the disease controls, but patients with genetic disorder and those with cortical dysplasia showed no significant diffe
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