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CPG a metalloenzyme derived from sp was the elected enzyme
2020-02-12
CPG2, a metalloenzyme derived from sp., was the elected enzyme for the first pilot-scale clinical trial of ADEPT. This enzyme has no mammalian homologue and activates glutamic CU CPT 22 prodrug derivatives of several nitrogen mustards alkylating agents., , , , , A bond cleavable by CPG2 is essent
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The aim of the following work
2020-02-11
The aim of the following work was to untap the potential of DIS as a low-cost substrate for fungal production of lignocellulolytic enzymes via SSF. Fungal strains with the ability to transform the unpretreated DIS to a mixture of industrially relevant lignocellulases were identified. Furthermore, th
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Preliminary studies suggest that dimerization of the AT
2020-02-11
Preliminary studies suggest that dimerization of the AT1 receptor occurred during the biosynthesis in the endoplasmic reticulum before surface expression [27,40], which may explain the presenece of these BIO-acetoxime receptor before the addition of any ligand. Our results showed that the presence
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CXCR is not only critical in
2020-02-11
CXCR5 is not only critical in the B cell lineage in FL. A high proportion of CXCR5-expressing follicular helper T cells (TFH) were observed in FL but not in closely related DLBCL [141] and further investigation revealed that FL regulatory T cells (Tregs) used a CXCL13-CXCR5 autocrine loop for positi
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DNA bound Ku proteins recruit DNA PKcs and
2020-02-11
DNA-bound Ku proteins recruit DNA-PKcs; and thereby translocate into the duplex by one helical turn, leaving DNA-PKcs near the DNA terminus to assist in tethering the broken ends together [25]. In addition to keeping the DSBs in close proximity, DNA-PKcs may prevent exonucleolytic degradation of the
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Of the acidic hydroxyazoles involved hydroxypyrazole had
2020-02-11
Of the acidic hydroxyazoles involved, hydroxypyrazole had the weakest acidic profile (pKa in the range of 6–7), although highly deprotonated at physiological pH. During hit optimization, the two pyrazole ring positions available for substitution provide an opportunity for a better exploration of the
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br DDR receptor and MMP expression Type
2020-02-11
DDR2 receptor and MMP-13 expression Type II collagen protein in articular cartilage is highly stable structure as its half-life is 117 years [43]. The chondrocytes have limited ability to synthesis type II collagen protein in the matrix of mature articular cartilage once the collagen gets disrupt
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The all NTP pyrophosphatase and NUDIX families maintain
2020-02-11
The all-α NTP pyrophosphatase and NUDIX families maintain the deoxynucleotide triphosphate (dNTP) pool balance, limit the incorporation of harmful nucleotides, and represent a promising therapeutic approach to develop anticancer and immunosuppressive agents., , , , Among these housekeeping enzymes
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br Advantages of modified proteins over unmodified ones
2020-02-11
Advantages of modified proteins over unmodified ones In contrast to small-molecule drugs, proteins are readily amenable to site-specific alterations through genetic engineering. In principle, therefore, it is possible to build in features that allow them to remain active for longer in the body an
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br System description and data collection Fig
2020-02-11
System description and data collection Fig. 1 shows the arrangement of the system studied. It provided cooling Biotin-azide to maintain thermal conditions in an institutional building. The locations of the measured variables (, and ) relating to temperature and flow rate are indicated in Fig. 1.
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The previously described endogenous patterns of IGF induced
2020-02-11
The previously described endogenous patterns of IGF-1-induced kinase signaling, and resulting interaction between MAPK and PI3K, differ across neuronal sub-types. In R28 retinal neuron-like cells, IGF-1 treatment elicits prolonged activation (at least 80 min) of both PI3K and MAPK (Kong et al., 2016
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br Significance Our understanding of the
2020-02-11
Significance Our understanding of the ubiquitin biology has been rapidly expanding. The role of the ubiquitin system in the pathogenesis of numerous disease states has increased the interest in finding new strategies to pharmacologically interfere with the enzymes responsible of the ubiquitinatio
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Air trapping at the small
2020-02-10
Air-trapping at the small airways is related to severe stat 3 inhibitor (Bjermer, 2014), and acute exacerbation (Mahut et al., 2010). Although asthma patients are generally treated with inhaled corticosteroid (ICS) or with ICS and long-acting β2 agonist (LABA), the efficacy of such treatment depend
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During the course of our
2020-02-10
During the course of our research on mGlu PAMs,, the hydroxyacetophenone scaffold was found to possess dual mGlu PAM and CysLT1 antagonism activity, presumably as orthosteric antagonist (). There is currently an increasing interest in drug discovery to explore multitarget drugs or polypharmacology
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Key molecules in the EP second messenger signaling cascade
2020-02-10
Key molecules in the EP1 second messenger signaling cascade that are necessary for potentiation of GluK2/GluK5 were identified. We also identified three GluK5 serines located in a membrane-proximal C-terminal domain that, when mutated to the phosphomimetic aspartate and expressed with GluK2, rendere
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