• Aurora A or B selective and pan aurora

  2024-10-23

  

  Aurora -A or -B selective and pan-aurora inhibitors have demonstrated different preclinical and clinical therapeutic efficacies [2,[19], [20], [21], [22], [23]]. For example, clinical trials for a pan-Aurora inhibitor VX-680 (developed by Vertex) were halted at phase II for toxicity reasons (one cas

• br Colorectal carcinoma The growth rate of

  2024-10-23

  

  Colorectal carcinoma The growth rate of murine colon adenocarcinoma tumors decreased upon inhibition of 5-LOX, an enzyme that harbors counteracting properties to 15-LOX [28]. It is not clear whether 15-LOX was associated with this phenomenon, but its expression is induced in the colon carcinoma c

• Introduction Cytochrome P CYP aromatase catalyzes the conver

  2024-10-22

  

  Introduction Cytochrome P450 19 (CYP19; aromatase) catalyzes the conversion of androgens to estrogens in a three-reaction sequence, where each step depends on NADPH and O2 [[1], [2], [3]]. The first two steps are accepted to be hydroxylations of the steroid C19 methyl group, whereas the final step

• TUNEL assay Apoptotic DNA fragmentation in cells was

  2024-10-22

  

  TUNEL assay. Apoptotic DNA fragmentation in UCF 101 was measured using a commercially available TUNEL assay kit (Thermo Fisher). Frozen cells were fixed with 10% paraformaldehyde/PBS. Apoptosis was determined by staining the 3′-OH ends of fragmented DNA with biotin-dNTP using DNA I klenow fragment a

• TLRs play a key role in pathogen recognition

  2024-10-22

  

  TLRs play a key role in pathogen recognition and early response. In our study, we showed an increase of TLR2 mRNA and protein expression after BMECs were stimulated by S. aureus, as seen for BMECs in a previous study [25]. Although most studies describe TLR4 as a primary receptor for Gram-negative b

• Over the years measures of total

  2024-10-22

  

  Over the years, measures of total antioxidant status (TAS) have been developed to capture the collective effect of antioxidant defense capacity, including enzymatic and nonenzymatic systems (Fraga et al., 2014, Franco et al., 2007). Multiple antioxidant enzymes, as well as antioxidant vitamins and m

• Thiazole heterocycles constitute an interesting

  2024-10-22

  

  Thiazole heterocycles constitute an interesting class of molecules, which exhibit a broad spectrum of biological activity, including antifungal properties [[16], [17], [18], [19]]. Encouraged by our previous study that describes the activity of hydrazine-thiazole derivatives against C. gattii and C.

• 821 receptor Thalidomide is now a well known antiangiogenic

  2024-10-22

  

  Thalidomide is now a well known antiangiogenic agent. This property of thalidomide is being extensively researched upon, for its significant utility in the treatment of various malignant tumors. Studies show that thalidomide efficaciously inhibits various pro-angiogenic factors such as tumor necrosi

• br Angiotensin receptor neprilysin inhibitors Sacubitril val

  2024-10-22

  

  Angiotensin receptor-neprilysin inhibitors Sacubitril/valsartan is the first-in-class ARNI, comprising of molecular moieties of valsartan (ARB) and a neprilysin inhibitor prodrug, sacubitril (AHU377) [51]. Upon ingestion, sacubitril is rapidly metabolised into an active neprilysin inhibitor, sacu

• br Methods br Results br Discussion Agitation in dementia ha

  2024-10-22

  

  Methods Results Discussion Agitation in dementia has recently been defined as a syndrome characterized by inferred or observed evidence of emotional distress associated with at least one behavioral component, i.e. excessive motor activity, verbal or physical aggression (Cummings et al., 201

• The aldehyde reductase AKR A

  2024-10-22

  

  The aldehyde reductase (AKR1A1) and aldose reductase (AKR1B1) belong to aldo-ketoreductase (AKR) superfamily catalyzing the reduction of corresponding aldehydes and ketones involved. Both the closely related enzymes AKR1A1 and AKR1B1 have 65% structural similarity and differ only at the active site.

• A number of studies suggest that adiponectin promotes osteob

  2024-10-22

  

  A number of studies suggest that adiponectin promotes osteoblast differentiation and bone formation by directly targeting GSK-3β and β-Catenin signaling [64], [65], favoring bone marrow mesenchymal stem cell (BMSC) differentiation toward the osteoblastic lineage [66], [67], decreasing sympathetic to

• br Results br Discussion Members of the PfkB

  2024-10-22

  

  Results Discussion Members of the PfkB family of proteins, which exhibit AK activity, have only been found in the eukaryotic organisms in the past. Hence, the report of a PfkB family protein in MTub that exhibited AK activity was of much interest, and it necessitated closer examination of its

• Here we report discovery of highly selective pan Aurora kina

  2024-10-21

  

  Here we report discovery of highly selective pan-Aurora kinase inhibitors through phenotypic screening. The co-crystal structure of nvp-aew541 bound in the ATP binding site of Aurora A is described, and provides insight into the possible structural basis for the selectivity of the interaction. To

• This project was funded by the University of the Philippines

  2024-10-21

  

  This project was funded by the University of the Philippines Diliman through the Natural Sciences Research Institute with grant No. CHE-09-2-02. Introduction There is compelling evidence for an anti-inflammatory effect of 12- and 15-lipoxygenases through the generation of lipid mediators involve

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