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br Regulation and pharmacology of mPGES mPGES kDa amino
2024-11-13
Regulation and pharmacology of mPGES-1 mPGES-1 (16 kDa, 152 amino acids) is a trimeric integral membrane protein of the endoplasmic reticulum with each monomer containing four transmembrane domains (Samuelsson et al., 2007; Sjogren et al., 2013). The three active site cavities are located at the
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The reaction of LOX with unlabeled
2024-11-13
The reaction of 5-LOX with unlabeled AA generated products from hydrogen abstraction at C7 (95% 5-HETE) with minor products derived from abstraction at C10 (5% 8-HETE). With 7,7--AA the selectivity remained skewed towards C7 hydrogen abstraction (59%) compared to C10 hydrogen abstraction products (4
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UMI-77 Compounds are representatives of an array of MBG
2024-11-13
Compounds – are representatives of an array of MBG targets (, ) related to imidazole standard that were synthesized and initially tested in a rat CYP17 lyase screening assay (). The inhibitors were synthesized as racemates by coupling of 6,7-dimethoxy-naphthalene-2-isopropyl ketone with the requisi
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br Clinical realities br Commentary
2024-11-13
Clinical realities Commentary on uses of selective 17,20 lyase inhibitors If continued monitoring of these same parameters along with tracking of circulating ACTH in human trials confirms these new drugs are the long sought after 17,20 lyase inhibitors, then we may for the first time be able t
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Having established the structural requirements for potency
2024-11-13
Having established the structural requirements for potency in both the biochemical and biomarker (CRA) assays, we evaluated key compounds in the metabolic stability assay. Disappointingly, we found that all compounds had high intrinsic clearances in mouse microsomes. To ascertain whether the in vitr
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However there are studies revealing the dark side of autopha
2024-11-13
However, there are studies revealing the “dark side” of autophagy at later stages in cancers, when oncogenes (mainly K-ras and B-raf) are activated and/or tumour suppressors such as PTEN and p53 are inactivated. These studies are based on the use of GEMM and deletions of essential autophagy genes (A
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Herbal medicines have been used
2024-11-13
Herbal medicines have been used to treat various types of diseases and disorders for thousands of years worldwide (Li and Brown, 2009). Natural products have been the remedy of cancer chemotherapy for the past several decades. Anisomeles indica (L.) Kuntze. (Labiatae), commonly known as 'yu-chen-tsa
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In addition to calpain I activity
2024-11-12
In addition to calpain I activity, cathepsin activities have been proven to be linked to apoptotic signaling. Cathepsin B and cathepsin D are two of the most abundant and well-investigated lysosome acid-dependent proteases that are involved in the apoptotic regulation (Ferri & Kroemer, 2001). Cathep
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glycoprotein iib iiia inhibitors br Conflicts of interest br
2024-11-12
Conflicts of interest Introduction When it comes to risk taking, surgeons and anesthesiologists show greater risk taking than other physicians. Surgical procedures carry several risks of which infection is one. Surgical site infections (SSI) are the most common hospital acquired infection and
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We provide here direct evidences that AT
2024-11-12
We provide here direct evidences that AT1 receptors are active in ADSCs since Ang II induces intracellular Ca mobilization in these cells. Data obtained during the observation of Ca influxes led us to the search for the ADSCs subpopulation constantly expressing AT1 receptor. ADSCs are necessary for
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Evidence from basic science studies suggests
2024-11-12
Evidence from basic science studies suggests that Cd may play a role in prostate cancer through disruption of the androgen receptor (AR). AR, a hormone-activated transcription factor, is the key driver of prostate cancer progression [6]. Ironically, the AR is also required for normal prostate growth
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Structural and functional imaging studies searching
2024-11-12
Structural and functional imaging studies searching for specific cortical areas related to each cognitive function domain have provided clues to the spreading patterns of cognitive dysfunction (Domoto-Reilly et al., 2012, Firbank et al., 2016, Li et al., 2012, Machulda et al., 2003, Mandal et al., 2
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A Venn diagram representing RNA seq data that
2024-11-12
A. Venn diagram representing RNA-seq data that show the number of gene overlaps in GFP and HepKO livers after chronic PF-06409577 dosing. B. Top canonical pathways that changed according to Ingenuity Pathway Analysis after chronic PF-06409577 dosing. C. Fibrosis-related genes that were altered in GF
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Although only Leu CysAP IRAP Herbest et al Keller
2024-11-12
Although only Leu/CysAP (IRAP) (Herbest et al., 1997, Keller, 2004) and DPPIV (Alponti and Silveira, 2010, Kirino et al., 2009) had been identified and studied in adipocytes, our kinetic analysis suggested the highest physiological significance for AspAP (highest affinity) and APM and PSA (highest e
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T-5224 When arachidonic acid is used as a
2024-11-12
When arachidonic T-5224 is used as a substrate, the platelet-type 12S-lipoxygenase produces predominantly the 12S-hydroperoxy derivative. In contrast, the leukocyte-type 12S-lipoxygenases generate substantial amounts of the 15-lipoxygenase product in addition to the 12S-hydroperoxy derivative. The r
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