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Our data show a site specific interaction of DDR
2021-01-06
Our data show a site-specific interaction of DDR2 with collagen II. This indicates that the DDRs recognise a particular sequence within collagen and not simply the collagenous triple helix per se. This common tertiary structure of all collagens is formed by three α chains, each with a repeating G-X-
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van Linden et al developed a comprehensive
2021-01-06
van Linden et al. developed a comprehensive guide that describes drug and ligand binding to more than 1200 human and mouse protein kinase domains [77]. Their KLIFS (kinase–ligand interaction fingerprint and structure) directory includes an alignment of 85 potential ligand binding-site residues occur
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The conventional medical therapy for
2021-01-06
The conventional medical therapy for IBD consists in reducing the inflammatory response using various strategies that exert severe side-effects, a strategy that also decreases the risk of colon carcinoma [13], [14]. During the last decade, the activation of the cholinergic system has been proposed f
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Emi protein consists of an N terminal
2021-01-05
Emi2 protein consists of an N-terminal regulatory region and a C-terminal functional region. The C-terminal region contains a destruction box (D-box), which likely competes with APC/C substrates (including cyclin B) for APC/C binding, and a zinc-binding region (ZBR), which somehow inhibits APC/C ubi
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br Phylogenetic analysis KSTDs have rather diverse amino aci
2021-01-05
Phylogenetic analysis — Δ1-KSTDs have rather diverse amino orphan receptor sequences. A sequence distance analysis using the program MEGA6 [75] of all currently biochemically characterized Δ1-KSTDs yielded a largest p-distance [76] of 0.67 (on a scale of 0-1) for the Δ1-KSTDs from the actinobacter
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Finally we have determined for the first time
2021-01-05
Finally, we have determined for the first time that aromatase enzyme activity is necessary to observe IGF-1-dependent fluorescent probes receptor activation. Neuroestrogen synthesis has been shown to be important for the maintenance of synaptic spine density in hippocampal slice cultures (Kretz et
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Identification of the drug to be used as
2021-01-05
Identification of the drug to be used as first-step antihypertensive treatment has always been, and remains, a matter of debate. The decision wihich drug (or drug combination) to choose as first-line therapy depend on many variables such as coexisting metabolic disorders, obesity, presence of subcli
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Due to the high attractiveness of
2021-01-05
Due to the high attractiveness of E2 and E3 ligases as drug targets, a number of drug discovery assays have been published, based on detection by fluorescence (Dudgeon et al., 2010, Krist et al., 2016, Zhang et al., 2004), MRS 1220 australia (Davydov et al., 2004, Huang et al., 2005, Kenten et al.,
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Anisomycin Currently much effort has been made to
2021-01-05
Currently, much effort has been made to design and synthesize ThDP analogs (such as ThTDP, ThTTDP, and triazole-ThDP in Fig. 2)8, 9, 10, 11, 12 as PDHc E1 inhibitors. These ThDP analog inhibitors, such as ThTDP and ThTTDP, can block the ThDP binding site, and exhibit significantly stronger binding a
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We have previously characterized the leucine rich NESs locat
2021-01-05
We have previously characterized the leucine-rich NESs located within the zinc-binding domains of mucosal high risk HPV16 E7 (76IRTLEDLLM84) and low risk HPV11 E7 (76IRQLQDLLL84) mediating their nuclear export in a CRM1 dependent manner (Knapp et al., 2009, McKee et al., 2013). The zinc-binding doma
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T helper Th cells play a central role in activation
2021-01-05
T helper (Th) Pyridoxal 5 phosphate mg play a central role in activation of immune system against infectious agents through secretion of lymphokines or cytokines. African trypanosomes target the Th cells and alter their activation, possibly for their own survival and perpetuity (Namangala, 2011). T
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The previously described endogenous patterns of IGF
2021-01-05
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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E ubiquitin ligases are key players in
2021-01-04
E3 ubiquitin ligases are key players in the ubiquitin-proteasome pathway because they catalyse ubiquitination of substrate proteins.39, 40, 41 As important regulators of cellular ubiquitination, E3 ligases are emerging as attractive drug targets, particularly in cancer.42, 43, 44 However, E3 ligases
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We have reported previously that aminoacrylate derivatives o
2021-01-04
We have reported previously that β-aminoacrylate derivatives of the general structure () are inhibitors of DHODH. In particular, tricyclic derivatives and displayed sub-micromolar IC values against DHODH, and in the case of there was a 1000-fold greater potency compared to the human enzyme (DHOD
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Fig D shows that E lagascae
2021-01-04
Fig. 2D shows that E. lagascae VIR E gives two species of radioactive TAG: one represents 45% of total labelled TAG and the smaller more-polar spot (15%) is probably derived from the endogenous 1,2-divernolin instead of the exogenous 1,2-diolein. In this case, the total scintillation counts were gre
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