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Several tertiary prevention studies are currently
2025-02-20
Several tertiary prevention studies are currently underway examining the use of dutasteride for prostate cancer treatment: (1) during expectant management of prostate cancer, (2) after radical prostatectomy in men at high risk for relapse, and (3) in men with metastatic disease. The Reduction by Dut
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The first rationally designed dual mPGES
2025-02-20
The first rationally designed dual mPGES-1/5-LO inhibitor was reported in 2008 and represents a structural derivative of pirinixic vinblastine shortage - a synthetic agonist of PPARα with lipid-lowering properties (Koeberle et al., 2008b). Further α-alkyl- and α-aryl-substituted derivatives have bee
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Among the AXL positive tumors that
2025-02-20
Among the AXL-positive tumors that we screened, the TNBC cell line MDA-MB-231 showed the highest AXL expression level. Additionally, AXL protein levels were higher in TNBC patient samples than in other breast cancers. Considering the difficulty of, and the urgent need for, effective treatments of TN
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By performing knockdown of AXL once HER cancer
2025-02-20
By performing knockdown of AXL once HER2+ cancer Z-YVAD-FMK have achieved lung colonization, we demonstrated that AXL contributes to the establishment of macrometastases. While inhibition of AXL impairs the efficiency of metastasis, the later finding has major clinical implications since pharmacolo
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The levels of Mcl and FLIP are homeostatically
2025-02-19
The levels of Mcl-1 and FLIP are homeostatically controlled by transcriptional and posttranslational processes. Accumulating evidence suggested that intracellular signaling molecules such as Akt are crucial to the transcription of Mcl-1 and FLIP [30], [31]. The constitutive activation of Akt is dete
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Given that the FST protocol
2025-02-19
Given that the FST protocol for mice does not engage the exposure to a previous stressful session, posits that Agtr1a levels could be kept higher by basal glutamatergic transmission rather than by stressful stimuli as postulated before. To address this possibility, we used the EMBL-EBI Expression At
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The sequential behavioral approach used in the present study
2025-02-19
The sequential behavioral approach used in the present study reinforced the involvement of the BDNF/TRKB system in the effect of losartan. In mice with dampened BDNF expression, losartan was no longer able to exert antidepressant-like effects. Similar to what was observed after losartan treatment, t
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In receptor binding terminology both receptor
2025-02-19
In receptor binding terminology, both receptor and acceptor contain a receptive site for the ligand, although only the receptor induces a biological function. Moreover, the acceptor lacks an endogenous ligand. Many proteins have been described as receptors for toxic Aβ assemblies, implying a designe
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Various compounds have been designed to
2025-02-19
Various compounds have been designed to inhibit aldose reductase (AR) [12]. These compounds can be classified into two main categories, the first category comprises those containing a carboxylic MCL1 binding S63845 moiety, for example, 3-thiazolidineacetic acid derivative, which has been reported to
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br Concluding Remarks The effects of point mutations of
2025-02-19
Concluding Remarks The effects of point mutations of the four ARs on ligand binding affinities, functional potencies, and efficacies constitute a valuable source of pharmacological information. We analyzed the existing data and mapped it on the collection of available AR crystal structures, allow
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ACK can be localized to clathrin coated vesicles The associa
2025-02-19
ACK1 can be localized to clathrin-coated vesicles [1]. The association of SNX9 with synaptojanin-1 would suggest the two cooperate during endocytosis at the synapse by coupling the sorting nexin to changes in phospholipid composition. ACK1 in turn negatively regulates the association of SNX9 with ta
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5-Methyl-UTP Two patients developed diffuse mesangio prolife
2025-02-19
Two patients developed diffuse mesangio-proliferative glomerulonephritis (DMPG) postoperatively, presenting as nephrotic syndrome and benign haematuria, respectively. DMPG has been reported in an adult patient with thymomatous MG following thymectomy [35], and various types of glomerulonephritis hav
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br Acknowledgements We thank Dr Stefan Schulte Merker and
2025-02-18
Acknowledgements We thank Dr. Stefan Schulte-Merker and his group members at the Hubrecht Institute (Utrecht, the Netherlands) for their invaluable support of the zebrafish studies. Our work is supported by grants from the Dutch Cancer Society (KWF) and the Netherlands Organisation for Scientific
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Autophagy is finalized through the coordinated positioning a
2025-02-18
Autophagy is finalized through the coordinated positioning and fusion of autophagosomes with lysosomes, during which an array of common and specific membrane traffic-associated proteins is mobilized. Among these proteins, small GTPases, like Rab7, Rab34, or Arl8, and their EdU proliferation detectio
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Carbenoxolone disodium PF also a dual Aurora
2025-02-18
PF-03814735, also a dual Aurora-A and Aurora-B inhibitor, was administered in a phase I dose escalation study in a 3-weekly Carbenoxolone disodium for 5 or 10 consecutive days [69], [70]. To date 25 patients have been included in 7 dose levels (5–100mg/day for 5 days). Using the 5-day schedule the
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