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In humans the major LOs are subdivided
2025-01-26
In humans, the major LOs are subdivided by their positional specificity into 5-(ALOX5), 12-(ALOX12) and 15-LO (ALOX15) (Kuhn et al., 2015). 5-LO is the key enzyme for LT biosynthesis and mainly found in mature cells from myeloid origin, including neutrophil, eosinophil and basophil granulocytes, mo
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Many metalloenzyme inhibitors consist of two
2025-01-26
Many metalloenzyme inhibitors consist of two chemical components: the MBG, the portion of the inhibitor designed to bind to the metal, and the scaffold, the portion of the inhibitor recognized by the amino AZD 5153 mg residues that form the substrate-binding site of the metalloenzyme. The MGB is of
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Introduction Cancer which is responsible for a million
2025-01-26
Introduction Cancer, which is responsible for a million deaths each year, is universally feared, and approximately 50% of newly diagnosed cases can be cured [1]. The existing cancer treatments, including surgery, chemotherapy, radiotherapy or a combination of them, are quickly losing efficacy. The
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What can we learn about the anticancer therapeutic efficacy
2025-01-26
What can we learn about the anticancer therapeutic efficacy of Aurora kinase inhibitors from our experience with the Bcr-Abl inhibitors and the long term clinical consequence of their use in treating leukemias? As discussed, all Aurora kinase inhibitors developed to date are ATP-competitive inhibito
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Although the LB domains of mGlu
2025-01-26
Although the LB2 domains of mGlu receptors have not been shown to form an extensive interface during activation, they do draw closer to each other, as demonstrated in crystal structures (Kunishima et al., 2000, Muto et al., 2007, Tsuchiya et al., 2002) and by FRET analysis (Doumazane et al., 2013, V
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Pathological angiogenesis occurs when an imbalance of endoge
2025-01-24
Pathological angiogenesis occurs when an imbalance of endogenous proangiogenic and antiangiogenic factors occurs. Although the focus of angiogenesis-related drug development has been geared to the discovery of antiangiogenic compounds for use in pathologies where excessive angiogenesis occurs (cance
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br Implementation of sacubitril valsartan into clinical prac
2025-01-24
Implementation of sacubitril/valsartan into clinical practice Following on from the results of PARADIGM-HF, sacubitril/valsartan was given regulatory approval for use in patients who conform to the main inclusion criteria of the trial; NYHA functional class II–IV, reduced left ventricular ejectio
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We designed SSOs that block APP
2025-01-24
We designed SSOs that block APP exon 17 splicing and induce the production of an alternatively spliced APP mRNA lacking exon 17 (APPΔex17). APPΔex17 mRNA encodes an APP protein isoform that lacks 49 indole-3-carboxaldehyde including the γ-secretase cleavage sites that give rise to the toxic, AD-ass
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In light of several reports of defects in memory
2025-01-24
In light of several reports of defects in memory-related tasks for the dysbindin-deficient mice (Cox et al., 2009, Takao et al., 2008), it was rather unexpected that an enhancement of CA3–CA1 LTP was observed in our investigation as well as in another independent study (T.T. Tang et al., 2009). The
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Several ceritinib resistant mutations following the second l
2025-01-24
Several ceritinib-resistant mutations following the second-line treatment of ALK+-NSCLC have been discovered [64]. These mutations include C1156Y, F1174L, and L1152R, which were first observed in crizotinib-resistant tumor samples. The G1202R ceritinib-resistant mutation occurs within the hinge and
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However although in vitro studies in heterologous systems
2025-01-24
However, although in vitro studies in heterologous systems have provided very important indications of potential novel pharmacology, the studies with endogenous receptors in native tissues are essential to provide evidence for GPCR heteromerization in vivo and to confirm its physiological relevance.
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Streptomycetes are a group of filamentous
2025-01-24
Streptomycetes are a group of filamentous Gram-positive, soil-inhabiting bacteria which have captured enormous screening interest because of their ability to produce and secrete a variety of LDN193189 Hydrochloride and extracellular proteins [7]. Among the diverse antibiotics produced by Streptomyc
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rs G allele was previously associated with a decrease in
2025-01-24
rs523349 G allele was previously associated with a decrease in the conversion rate of testosterone to DHT (Beesley et al., 2007). This SRDA52 variant may have a trend towards higher testosterone availability, which according to the US Food and Drug Administration is described as a teratogen of categ
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We demonstrate a role for low oxygen
2025-01-23
We demonstrate a role for low oxygen to regulate ATX mRNA in hepatocyte-derived HuH7 phospholipase a2 inhibitor and human liver slices, consistent with reports of increased ATX expression in a variety of tumours that are frequently hypoxic. Importantly, we show a positive association between elevat
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br The complementary role of
2025-01-23
The complementary role of chaperone mediated autophagy Chaperone-mediated autophagy (CMA) mediates the degradation of specific cellular proteins and participates in the regulation of lipid metabolism, DNA repair, or the response to stress (Kaushik and Cuervo, 2018). CMA provides an alternative pa
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