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IC values were obtained for an expanded version
2025-02-27
IC50 values were obtained for an expanded version of the fragment library using the previously described mobility shift assay. Subsequently, Ki values were estimated from IC50 values to allow better comparison of the activity against targets which were measured at different substrate concentrations
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Introduction Mitotic kinases play an essential role in
2025-02-27
Introduction Mitotic kinases play an essential role in mitosis, Aurora and other mitotic kinases are often observed over-expression in human solid and many hematologic cancers. As one of serine/threonine kinases, Aurora kinase family is involved in centrosome maturation, mitotic spindle formation,
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The skin permeability barrier is important for the
2025-02-27
The skin permeability barrier is important for the prevention of loss of water and electrolytes from inside the body and for protection against the invasion of external pathogens, allergens, and harmful compounds. Multi-layered lipids, called lipid lamellae, are present in the outermost cell layer o
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br Conflict of interest statement
2025-02-26
Conflict of interest statement Acknowledgement Introduction Lipoxygenases (LOs) are enzymes catalyzing the positional as well as stereo-specific introduction of molecular oxygen into 1,4-pentadiene structures found in unsaturated fatty acids such as arachidonic autotaxin inhibitor or linol
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In this study using pure enzyme
2025-02-26
In this study, using pure enzyme preparations of human placental recombinant AR (hAR) and of AR isolated from bovine lens (bAR), which behave as Michaelis procollagen c proteinase with glyceraldehyde as substrate, is shown that an apparent negative cooperativity action for glucose still occurs. We
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The excellent potencies selectivities and improved PK associ
2025-02-26
The excellent potencies, selectivities and improved PK associated with the piperazine class triggered more extensive off-target screenings of the highlighted compounds. A screen of more than 100 enzymes, receptors, and ion channels resulted in activity at the norepinephrine transporter (NET). This m
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The only psychostimulant treatment option in Turkey is
2025-02-26
The only psychostimulant treatment option in Turkey is methylphenidate (Çetin et al., 2015). It is broken down by carboxylase enzyme (CES1) (Sun et al., 2004). From the point of pharmacokinetics, it may be suggested that CES1 gene polymorphisms may be the key responsible factors in patients resistan
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One study has demonstrated that PUFA reduced both cholestero
2025-02-26
One study has demonstrated that ω-3 PUFA reduced both cholesterol and caveolin-1 (a marker of raft), thereby displacing raft-associated signaling molecules from lipid raft [36]. Additionally, DHA treatment decreased the amount of lipid raft in the cell surface and displaced several lipid raft-associ
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br A Rs which were cloned and then pharmacologically identif
2025-02-26
A3Rs, which were cloned and then pharmacologically identified in the early 1990s, are expressed in multiple organs and peripheral tissues including AZ 628 involved in inflammatory responses (Gessi et al., 2008, Borea et al., 2014). While low levels are expressed in the CNS, A3R agonists produce f
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apexbio dilution All scientific data over the years
2025-02-26
All scientific data over the years points that 5α-reductase inhibitors undoubtedly are an effective treatment for BPH and associated LUTS, having a favorable risk-benefit profile. In contrast, although some studies indicated positive results, there is still no consensus about their use in BPH or PC
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Jesus et al discovered a new series
2025-02-26
Jesus et al. discovered a new series of azaindole as Aurora inhibitors through various modification of GSK1070916 (47). They synthesized series from modification of the GSK1070916 and evaluated for in-vitro Aurora-B/INCENP and Aurora-A/TPX2 inhibition assays. Modified Zanamivir 48 and 49 showed IC5
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In addition to pH regulation by ion
2025-02-26
In addition to pH regulation by ion (counter-) fluxes, acidification is regulated by the abundance of V-ATPase on organelles, by the pumping activity of the complex and by proton leakage. In yeast, the V-ATPase VO subunit a is the only subunit expressed in two isoforms termed Stv1p and Vph1p. V-ATPa
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br Materials and methods br Results A
2025-02-25
Materials and methods Results A first series of experiments explored whether the Ampkα1 isoform is involved in the regulation of cardiac Pkcζ. To this end, HL-1 cardiomyocytes were transfected with a construct encoding constitutively active Prkaa1T183D (CAα1) or with the empty vector as contro
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Methods We conducted a secondary
2025-02-25
Methods We conducted a secondary analysis of an extant cohort of 580 infants hylaxis, premature rupture of membranes, chorioamnionitis, and to prolong pregnancy (latency). Maternal antibiotic exposure did not include Salirasib given after the time of delivery or antibiotic initiated by surgeons du
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The reception of antiangiogenic treatment
2025-02-25
The reception of antiangiogenic treatment in neuro-oncology has yet to achieve the wide success rapidly accomplished for other malignancies. In 1984, mutated receptor tyrosine kinase became a culprit for aberrant tumorigenesis signal, providing a target for monoclonal idasanutlin (mAbs) and small-m