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Natural compounds present in medicinal
2024-09-10
Natural compounds, present in medicinal and/or nutritional plants as well as in macrofungi sources, have stimulated a great interest from the pharmaceutical industry. Different natural compounds such as phenolic compounds, alkaloids, terpenoids among others, have shown strong antiangiogenic effects
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Sixth significant progress has been
2024-09-10
Sixth, significant progress has been made during the last few years regarding the molecular mechanisms underlying the activation of AMPK and this should aid to develop more potent and specific compounds. Information from crystallographic structures combined with computer-based drug design hold promi
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br Conflict of interest statement br Introduction
2024-09-10
Conflict of interest statement Introduction Currently, adenocarcinoma is the most common histological subtype of lung cancer. Activating mutations and translocations with a potential for targeted therapy are reported predominantly in non-smokers. ALK rearrangement is found in less than 5% of u
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OCT also is known as POU F plays an important
2024-09-10
OCT4 (also is known as POU5F1) plays an important role in embryonic stem cell self-renewal, development and reprogram somatic cell into pluripotent stem cell [[5], [6], [7]]. Recently, many studies also find OCT4 promotes the progression of many tumors. For example, Wnt/β-catenin promotes the expans
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Constitutive tyrosine kinase activity of BCR ABL fusion
2024-09-09
Constitutive tyrosine kinase activity of BCR/ABL fusion genes causes uncontrolled cell growth and is also thought to be responsible for a variety of changes in normal cellular functions like differentiation, adhesion, migration and apoptotic response in CML. Therefore it is important to know the exp
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The direction of research then turned to investigating
2024-09-09
The direction of research then turned to investigating the long-term effects of adiponectin on insulin resistance. Adiponectin transgenic mice showed a reduction in insulin resistance and diabetes [5,6], while adiponectin-deficient mice showed mild insulin resistance with glucose intolerance, as wel
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A key step in the ADAR reaction is the formation
2024-09-09
A key step in the ADAR reaction is the formation of the adenosine covalent hydrate with a tetrahedral center at C6. The nucleoside analog 8-azanebularine (box in Fig. 6), with its relatively high propensity to form a covalent hydrate, is useful as an adenosine replacement in ADAR2 substrates to trap
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Introduction The cytoskeleton allows cells to
2024-09-09
Introduction The cytoskeleton allows cells to establish, maintain and transform their shape. In neurons, these include cell differentiation, migration, polarization and development of their unique arborization. Axons are very thin (~1 μm), long (up to 1m) and highly branched (>95% of the plasma mem
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Although effects of low concentrations of agonist were
2024-09-09
Although effects of low concentrations of agonist were not as thoroughly documented for heteromeric receptors such as the major ttp stock α4β2 nAChR, a similar mechanism of action was described to explain the potentiation of these receptors with low concentrations of acetylcholine-esterase-inhibiti
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ONX-0914 Our previous studies found that some steroid
2024-09-09
Our previous studies found that some steroid mimetic structures such as stilbene, biphenyl, naphthalene and benzothiophene rings were suitable for lipophilic moieties of 17,20-lyase inhibitors, and several inhibitors obtained using a steroid A, C-ring mimetic approach have already been published. Du
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A variety of quinazoline or
2024-09-09
A variety of quinazoline or fused pyrimidine-substituted diaminotriazoles showed sub-100nM inhibition of Axl (). Diaminotriazoles similarly substituted with quinolines, isoquinolines and benzothiazoles also showed potent Axl activity (data not shown), but generally exhibited potent cytotoxicity and
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br Conclusion In summary screening a small compound library
2024-09-09
Conclusion In summary, screening a small compound library based on the 3-aminopyridin-2-one motif in a target-blind manner against a 26-kinase panel, representative of the kinome, identified hits that possess good activity and excellent ligand efficiency against MPS1, Aurora A and Aurora B. The b
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Previously using a P lacZ reporter gene system it has
2024-09-09
Previously, using a P-lacZ reporter gene system, it has been shown that the β-galactosidase activity was 9-fold higher in the stationary phase latrunculin a when compared with those of the exponential phase [15]. Furthermore, inositol supplementation did not have a major effect on the expression of
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The canonical binding sites to which or contribute are
2024-09-09
The canonical CHC synthesis 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, lig
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br Discussion br Acknowledgments Writing of this review
2024-09-09
Discussion Acknowledgments Writing of this review and collection of data from our laboratories that are presented were supported by a grant from the Belgian Science Policy (BELSPO) SSTC Interuniversity Attraction Poles Plastoscine P7/17 to AVDL and JB, multiple grants from the Fund for Scienti
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