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Considering the protumoral functions of TAMs new
2019-09-24
Considering the protumoral functions of TAMs, new therapies against TAMs have recently gained interest. Such treatments, particularly inhibitors of the colony stimulating factor 1 receptor (CSF-1R), are currently evaluated in several clinical trials [19]. CSF-1R inhibitors may also be of interest in
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The inhibition of FAS by
2019-09-24
The inhibition of FAS by C75 produces an accumulation of malonyl-CoA which is difficult to reconcile with the activation of CPT1 reported by others [2], [16], [17], [18]. To unravel this paradox the mechanism of action of C75 needs to be examined. We recently demonstrated that C75 is converted in vi
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Pirarubicin clinical br Acetylcholinesterase and cholinergic
2019-09-24
Acetylcholinesterase and cholinergic signaling The concept of a synapse between a neuron and an innervated cell, and the receptors that mediated their interaction, was developed by Bernard, Ehrlich, Sherrington, Langley and others (see [7], [8], [9]. It was long debated whether transmission of ne
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Compounds and possessed relatively low clogP values and
2019-09-24
Compounds 11–13 and 15 possessed relatively low clogP values and tended to show relatively weak antagonist activity regardless of their potent EP1 receptor affinity. Compounds 2–4, which were selected based on their potent in vivo antagonist activity, were found to be effective in an animal model.
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Introduction Proteins play an important role in cellular
2019-09-24
Introduction Proteins play an important role in cellular functions; however, being and remaining properly folded is necessary for their function. Understanding the stability of the protein is necessary to investigate the folding of proteins, as well as their conformation, functions and interactions
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Inflammatory action of certain cytokines can influence cell
2019-09-24
Inflammatory action of certain cytokines can influence cell proliferative routes (Deshmane et al., 2009). When mTOR is inhibited, for instance by the action of Rapa, TGF-β1, which has an anti-inflammatory action, is increased. The relationship between high levels of TGF-β1 and cAMPS-Rp, triethylammo
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One of the critical functions of the product of
2019-09-24
One of the critical functions of the product of the AR gene is to activate the expression of target genes. This transactivation activity resides in the N-terminal domain of the protein encoded in exon 1, which contains polymorphic repeats. These trinucleotide repeats, (CAG) and (GGC), encode polyglu
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Verapamil a calcium channel blocker used clinically
2019-09-24
Verapamil, a calcium channel blocker used clinically as a coronary vasodilator, was amongst the first compounds identified that could reverse MDR and potentiate the effects of MDR1 substrates such as vincristine [15], [16]. Verapamil, along with a number of other MDR1 blockers, have proved largely u
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Three DDR binding sites have
2019-09-24
Three DDR2 binding sites have been mapped on the collagen triple helix by us for collagen type 1 and by others using the collagen toolkit for collagen type 2. All of the three reported binding sequences are conserved in the α1 chain of collagen types 1, 2 and 3. The central motif sequence GARGQAGVMG
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We examined the function of immobilised THPs by
2019-09-24
We examined the function of immobilised THPs by seeding cells transfected with DDR2-Flag on derivatised crosslinked collagen films, then detecting the phosphorylation of tyrosine 740 (Y740) on the intracellular domain of DDR2 [50]. This regulatory residue is a target for the intracellular tyrosine k
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It is well established that p
2019-09-23
It is well established that p53 maintains genomic integrity in response to a variety of cell stresses including DNA damage and oncogenic stress among others [6], [7], [8], [9]. p53 promotes the expression of several genes to cause DRB and arrest and to repair cellular damage. There is growing eviden
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A range of inhibitors were therefore
2019-09-23
A range of inhibitors were therefore synthesized containing either carboxylic p-nitro-Cyclic Pifithrin-α or ester functionality at the ‘tail’ group as well as variations in the ‘head.’ These were assayed in vitro using the DCIP assay for binding affinity against and human DHODH at 50μM, respectively
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Redundancy of tumor promoting signaling
2019-09-23
Redundancy of tumor promoting signaling pathways is one of the mechanisms that prevent a lasting effect of targeted therapies, as has been demonstrated by the growing number of alternative pathways that confer resistance to EGFR-targeted therapies [3]. We show here that CSF-1R can, at least partiall
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Prostaglandins production and some of
2019-09-23
Prostaglandins production and some of their possible biological functions have been reported in protozoa, helminths, and fungi organisms, for example amphizoic amoebas of the genus Acanthamoeba and Entamoeba (E. histolytica) produce PGA2, PGE2 and PGF2α [5,6]. PGA2 is believed to be an intrinsic osm
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Gamboge is a dry resin obtained from
2019-09-23
Gamboge is a dry resin obtained from Garcinia hanburyi HOOK. f. (Guttiferae). It has a variety of bioactivities, including detoxifying, homeostasis maintaining, anti-inflammatory and parasiticidic effects. Available evidence suggests that gamboge bears anticancer characteristics with gambogenic Bort
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