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br Colorectal carcinoma The growth rate of murine colon
2023-08-17

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
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The structural analysis of the ASK activation
2023-08-17

The structural analysis of the ASK1 activation segment, which was not phosphorylated in the crystal structure, showed interactions mimicking those found in activated kinases. In addition, the isolated unphosphorylated ASK1-CD is active and able to autophosphorylate itself at three sites, Thr813, Thr
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Several structural classes of ASK inhibitors mostly from ind
2023-08-17

Several structural Dryocrassin ABBA of ASK1 inhibitors, mostly from industry but also from academia, have been identified over the last decade. In 2012, Terao et al. (Takeda) reported imidazo[1,2-α]pyridine () as a potent ASK1 inhibitor derived from structure-based drug design. GSK, Merck and Gile
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br Experimental Section br Results and Discussion
2023-08-17

Experimental Section Results and Discussion Conclusions The advantages of the novel enzymo-chemical method for Mn and Co assay are simplicity of analytical procedure and economic effect due to the usage of only one enzyme in the form of apo-enzyme. An effectiveness of the apo-arginase-based
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Overall the expression of both components ligand and recepto
2023-08-17

Overall, the expression of both components (ligand and receptor) of the apelin signaling system allows for analysis of the direct role of apelin in CL function, and specifically P4 production. Although the CL secretes many different hormones, P4 is of predominant importance because it is necessary f
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These experiments make it clear that one can study the
2023-08-16

These experiments make it clear that one can study the effect of antimalaria drugs that target the DHFR enzyme of P. falciparum by transferring the malaria enzyme into S. cerevisiae. The ease of growth and manipulation of the yeast make it easy to measure the sensitivity of any particular dhfr allel
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The initial demonstration of the potential
2023-08-16

The initial demonstration of the potential of MALDI-TOF MS for testing antifungal susceptibility of pathogenic fungi came from a proof-of-concept study by Marinach et al. [31] who monitored the changes of the proteome of C. albicans c-met exposed to different concentrations of fluconazole. Using a r
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br Concluding Remarks Despite major advances in the developm
2023-08-16

Concluding Remarks Despite major advances in the development of antibody and small-molecule tumor angiogenesis inhibitors, therapy resistance, both innate and acquired, continues to limit further survival improvements for patients with cancer. Preclinical models of localized primary tumors and me
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Maynard et al demonstrated that serum
2023-08-16

Maynard et al. [54] demonstrated that serum levels of sFlt-1 were five times higher in pregnant women with PE than in normotensive women; as a consequence, VEGF and PlGF levels were found to be proportionally reduced in these women [54]. The literature confirms that there is a sharp increase in sFlt
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Preclinical models indicate roles for adiponectin in
2023-08-16

Preclinical models indicate roles for adiponectin in the maintenance of hepatic lipid metabolism. Adiponectin overexpression prevents accumulation of triglycerides or the deleterious lipid metabolites diacylglycerols or ceramides [5,8]. Direct manipulation of adiponectin expression demonstrates a po
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However although in vitro studies in heterologous systems ha
2023-08-16

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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In the late s Solvay
2023-08-16

In the late ‘90s, Solvay Pharmaceuticals discontinued the Phase 2 development of a promising potent and highly selective A1AR antagonist based on the pyrrolopyrimidine scaffold, SLV320 [43] (2, Chart 1, also named derenofylline; Ki hA1AR = 1 nM), for the treatment of acute heart failure [24]. In the
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adenylate cyclase Targeting the BCR is the
2023-08-16

Targeting the BCR is the ideal strategy to identify the antigen reactive B cells. However, there is concern that B cells could be activated when BCR are bound and cross-linked by antigens, a possibility that is obviously negative for the treatment of autoimmune disease. Proby et al. (2000) tried to
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In summary this study reveals that the stability
2023-08-16

In summary, this study reveals that the stability of rapsyn is critically dependent on HSP90β, highlighting a novel function of HSP90β in NMJ formation and maintenance. It also identifies a mechanism in agrin signaling for AChR clustering, i.e., by upregulating the interaction between HSP90β and rap
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The purpose of the present study
2023-08-16

The purpose of the present study is (1) to characterize AChE from the monogonont B. koreanus and to analyze the modulation of the AChE activity and its transcription level after exposure to six pharmaceuticals, (2) to evaluate the usefulness of AChE as a molecular biomarker upon pharmaceutical expos
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