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A high throughput small molecule ACK biochemical inhibition
2023-04-25

A high-throughput small molecule ACK1 biochemical inhibition screen was performed in-house and led to the identification of 1μM inhibitor furanopyrimidine (). Further binding studies found SB 525334 to be both ATP-competitive and reversible. Early structure-activity relationship (SAR) work was perf
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NSAIDs induce gastrointestinal toxicity and evoke asthma by
2023-04-25

NSAIDs induce gastrointestinal toxicity and evoke clofibrate by decreasing the production of gastroprotective prostanoids and by redirecting the COX substrate AA into LT biosynthesis, thereby causing vasoconstriction in gastric mucosa and airways (Celotti and Laufer, 2001; Koeberle and Werz, 2015;
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The benzimidazole group seems to be a key feature
2023-04-25

The benzimidazole group seems to be a key feature for the excellent anti-tumor activity of galeterone (159), which motivated the synthesis of new steroidal inhibitors containing N-heterocyclic groups structurally related to benzimidazole. Thus, several 1H- and 2H-indazole derivatives of dehydroepian
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Aurora A overexpression is also
2023-04-25

Aurora-A overexpression is also related to the activation of NF-κB, a potent anti-apoptotic effector that may play a role in preventing apoptosis in cancer brucine [18]. These data show that we are still at the beginning of unraveling the complex mechanism by which these gene products and proteins
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Aurora A and B are required for
2023-04-25

Aurora A and B are required for the control of mitosis whereas Aurora C is mainly invoved in meiosis (Goldenson and Crispino, 2015). Interestingly, Aurora B is partnered with inner centromere protein (INCENP), survivin and Borealin to form a chromosomal passenger complex (CPC) that is critical for t
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The canonical binding sites to which
2023-04-24

The canonical LDN193189 to which α2, α3, or α5 contribute are highly similar. Therefore, differences in ligand affinity will not be large even if a ligand makes optimal use of the small differences in the pockets. As a possible alternative approach to achieve separation of compound effects, ligands
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About three weeks later the patient visited our outpatient
2023-04-21

About three weeks later, the patient visited our outpatient clinic complaining of gingival bleeding and pus discharge. In clinical examination bone exposure was observed in both mandibular posterior regions and bone necrosis had developed surrounding the #35=37 and 46, 47 implants installed 6 years
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br Acknowledgements This work was
2023-04-21

Acknowledgements This work was supported by National Natural Science Foundation of China (Nos. 21376172, 21528601 and 21621004) and the Natural Science Foundation of Tianjin from Tianjin Municipal Science and Technology Commission (Contract No. 16JCZDJC32300). Introduction Alzheimer’s disease
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Despite extensive studies on the expression of
2023-04-21

Despite extensive studies on the expression of T. pallidum-induced pro-inflammatory cytokines, very little is known about T. pallidum-mediated intracellular signaling pathway activation, that leads to cytokine expression in macrophages. A network of signaling molecules, transcription factors, epigen
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br Acknowledgments This work was
2023-04-21

Acknowledgments This work was supported by Grant-in-aid for Scientific Research (S) (20229008) (to T.K.), Targeted Proteins Research Program (to T.K.), the Global COE Research Program (to T.K.) and Translational Systems Biology and Medicine Initiative (to T.K.) from the Ministry of Education, Cu
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In previous research we determined that blocking mAC during
2023-04-21

In previous research, we determined that blocking mAC during heparin-induced capacitation result in sperm having a lesser oxygen consumption, suggesting that cAMP produced by this enzyme would be linked to mitochondrial activity and, therefore, with the regulation of sperm metabolism (Fernández and
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During years research efforts at Los Alamos National
2023-04-20

During 2002–2004years research efforts at Los Alamos National Laboratory (LANL) focused on constructing a quantum computer based on regular arrays build from neutral radical molecules possessing one single unpaired m-Chlorophenylbiguanide hydrochloride synthesis spin. The idea was built on the abil
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The adoptive transfer experiments additionally demonstrated
2023-04-20

The adoptive transfer experiments additionally demonstrated the role of cholinergic regulation in the antibody immune response. Injection of LPI-stimulated B lymphocytes significantly up-regulated both the IgM and IgG responses to cytochrome c in the host. Obviously, this effect was due to activatio
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Phospholipases cleave membrane phospholipids from inflammato
2023-04-20

Phospholipases cleave membrane phospholipids from inflammatory cells, activated platelets, erythrocytes, adipocytes and cancer pyruvate dehydrogenase kinase (Aoki et al., 2008, Neidlinger et al., 2006). Several reports have analysed the role of LPA and its receptors in the pathogenesis of RA. Zhao
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Arginase deficiency is a rare urea cycle disorder with hyper
2023-04-20

Arginase deficiency is a rare urea cycle disorder with hyperargininemia and profound neurological impairment as hallmark features. Arginase-1-deficient mouse models have been created, and they exhibit a profound lethal phenotype approximately 2 weeks after birth in the global knockout (KO) mice or a
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