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Imatinib was first approved for
2023-10-11
Imatinib was first approved for the treatment of Philadelphia chromosome positive chronic myelogenous leukemia in 2001 [25]. This first approved small molecule antagonist is quite unusual in that it provides a durable response that lasts for more than a decade in the majority of patients. Imatinib h
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Because LTs are proved to mediate multiple biological
2023-10-10
Because LTs are proved to mediate multiple biological and pathological responses in various disease states, the 5-LO biosynthetic pathway producing LTs from AA have been the target of drug discovery efforts for over two decades. As observed from literature, a pile of research efforts has been direct
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Compounds are representatives of an array of MBG
2023-10-10
Compounds – are representatives of an array of MBG targets (, ) related to imidazole standard that were synthesized and initially tested in a rat CYP17 lyase screening assay (). The inhibitors were synthesized as racemates by coupling of 6,7-dimethoxy-naphthalene-2-isopropyl ketone with the requisi
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It was previously demonstrated that dissociation
2023-10-10
It was previously demonstrated that dissociation of the V-ATPase in response to glucose depletion in yeast requires an intact microtubular network [28] and a catalytically active enzyme [29]. Interestingly, mutations in the non-homologous region of the catalytic subunit A are able to block dissociat
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A different mechanism has been suggested for the role
2023-10-10
A different mechanism has been suggested for the role of TRX1 in ASK1 regulation based on disulfide bond-mediated ASK1 multimerization and its reduction through the thiol-reductase activity of TRX1 (Nadeau et al., 2007, Nadeau et al., 2009). In this model, oxidative stress induces intermolecular dis
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Thirdly and finally multiple studies have analyzed
2023-10-10
Thirdly and finally, multiple studies have analyzed the activation of neurons in the auditory telencephalic areas of songbirds in response to various auditory stimuli. Neuronal activation was identified by the increased expression of immediate early genes such as fos or ZENK (also know as zif-268, e
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Here the so called alkali
2023-10-10
Here the so-called alkali assay [18] is proposed as a method to be applied directly on the purified recombinant enzyme sharing the same structural and functional features of the wild-type enzyme [19], [20], [21] using its physiological substrate androstenedione. The assay that was already successful
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Natural compounds present in medicinal and or nutritional
2023-10-10
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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Sorafenib was the first small
2023-10-10
Sorafenib was the first small RTK inhibitor drug to be developed and was initially approved against renal cell carcinoma, then against hepatocellular carcinoma (HCC) and more recently for differentiated thyroid treatment [111]. Sunitinib soon followed, being approved for gastrointestinal stromal tum
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First the complete canonical brain
2023-10-10
First, the complete canonical brain original RAS (Angiotensinogen, Renin, Angiotensin I, Angiotensin Converting Enzyme (ACE), Angiotensin II) has not been conclusively identified in any specific cell type within the brain [1]. Validated evidence for the presence of brain Angiotensinogen and ACE was
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Aggregated A species have been studied by an array of
2023-10-10
Aggregated Aβ species have been studied by an array of biophysical techniques, including atomic force microscopy (AFM) [55], transmission electron microscopy (TEM) [56], [57], X-ray diffraction [58], Fourier transform infrared (FTIR) [59], [60], circular dichroism (CD) [61], and nuclear magnetic res
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Bioinformatics tools are becoming more powerful
2023-10-10
Bioinformatics tools are becoming more powerful and reliable due to the growing number and availability of experimentally determined protein structures (Arnold et al., 2006, Suplatov et al., 2015, Wiltgen and Tilz, 2009). The SWISS-MODEL and MODELLER programs are most frequently used for homology or
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FTI 277 HCl br Introduction Chronic kidney disease
2023-10-10
Introduction Chronic kidney disease (CKD) is a worldwide public health problem. This problem is even worse in socioeconomically deprived countries because lower income and social deprivation are associated with higher incidence of reduced GFR, progressive kidney function loss and end stage renal
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The proposed formulation is however challenging to solve
2023-10-10
The proposed formulation is, however, challenging to solve since the structured sparsity-inducing norms are non-smooth. In order to solve the new objective function, we consider two different approaches: proximal averaging, which takes the average the solutions from the proximal operator for the ind
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br Development of lorlatinib from
2023-10-10
Development of lorlatinib from crizotinib (1) to a clinical candidate (6) Xalkori (1, PF-02341066, crizotinib), was the first-in-class ALK inhibitor approved by the Unites States Food and Drug Administration (FDA) in 2011 as a first-line treatment for ALK+- NSCLC patients. This section describes
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