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Apart from its high affinity the selection of GW as
2020-07-20
Apart from its high affinity, the selection of GW2580 as epz lead in our radiotracer development program was motivated by its exceptional selectivity. The observed profound impact of small structural modifications on the selected panel of four kinases tested prompted us to conduct comprehensive kina
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Previous studies from our laboratory in CD mice using the
2020-07-20
Previous studies from our laboratory in CD1 mice using the incisional postoperative pain model have shown that the incision induces significant mechanical postoperative hyperalgesia lasting between 7 and 10days, with peak effect between 4h-2days (Cabañero et al., 2009a, Cabañero et al., 2009b, Campi
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Notably HSP expression is under control of the
2020-07-20
Notably, HSP27 expression is under control of the tetrameric form of CK2 holoenzyme, as knockout or knockdown of the β regulatory subunit alone reproduces the same effects of targeting the α/α′ catalytic subunits. This observation discloses the possibility to use more specific drugs that affects onl
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In ER group Histopathological examination followed by Fluore
2020-07-20
In ER + group, Histopathological examination followed by Fluorescence in situ hybridization (FISH) had revealed the absence of HER2 receptors. Co-targeting of ER and HER2 appears to provide benefit without a significant increase in toxicity although formal trials have not been carried out [18]. Adop
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Introduction Fish commonly employ pheromones to regulate a
2020-07-20
Introduction Fish commonly employ pheromones to regulate a variety of functions including reproductive communication [1]. Reproductive pheromones induce both primer effects, such as changes in the endocrine or physiological state of conspecifics, and releaser effects such as rapid behavioral respon
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Predictions of enzyme topology for
2020-07-17
Predictions of enzyme topology for DGAT2 are more difficult since the DGAT2 polypeptide sequences are more diverse across species than those of DGAT1. The length and function of the hydrophilic N-terminus preceding the first hydrophobic segment varies with species – for example, segments in fungi ar
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DDR was originally cloned by the
2020-07-17
DDR1 was originally cloned by the group of Michele de Luca, at the time named TrkE. The Genoa-based research team identified the skin, and the keratinocytes in particular, as a major site of DDR1-binding activity [20]. DDR1 is also expressed in kidney, liver and lung (Fig. 2). The functional role of
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The first transcription factor TF known
2020-07-17
The first transcription factor (TF) known to interact with one of the cis-acting GAREs is GAMYB protein, the expression of which is induced by GA in the aleurone panx receptor of barley (HvGAMYB) (Gubler and Jacobsen, 1992). GAMYB is an important regulator of endosperm functions during seed develop
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Chemokines act as ligands for the chemokine receptors which
2020-07-17
Chemokines act as ligands for the chemokine receptors, which possess 7-transmembran domain-type proteins functionally coupled to G proteins. Leukocytes express 19 chemokine receptors which control their influx and activation at the site of inflammation. Human neutrophils express both CXCR-1 and CXCR
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Endothelins ETs are peptides expressed in
2020-07-17
Endothelins (ETs) are peptides expressed in both the peripheral and the central nervous systems, which can contribute to sensory changes seen in animal models of inflammatory, cancer and neuropathic pain [10], [11]. All three mammalian isoforms (ET-1, ET-2 and ET-3) activate specific G protein-coupl
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Estrogen treatment in postmenopausal women requires combinat
2020-07-17
Estrogen treatment in postmenopausal women requires combination with a progestogen in order to prevent endometrial stimulation. This is not necessary, however, with tibolone as progestogenic activity is associated with its Δ4-metabolite that is formed in the liver, as well as locally in the endometr
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The expression of DDR receptor has regulated
2020-07-17
The expression of DDR2 receptor has regulated by numerous types of factors depending upon the cell type. During the osteogenic differentiation, the transcription factorATF4 combined with CCAAT/enhancer binding site in the DDR2 promoter, which is responsible for induction of DDR2 transcription [24].
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One of the isolated interactors against Mulan Ube E fusion
2020-07-17
One of the isolated interactors against Mulan259–352–Ube2E3 fusion bait was found to be the GABARAP protein, a known member of the Atg8 family that includes LC3 [20]. The Atg8 family-of-proteins are major players in autophagy/mitophagy since they are part of the autophagosome [20], [21], [22]. Our s
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Moreover recent structural studies of VEEV nsP pro in
2020-07-17
Moreover, recent structural studies of VEEV nsP2pro in complex with E-64d revealed an important molecular interaction at the interface of two subdomains. In this structure, Asn475 which is in polar contact with carbonyl oxygen of Asp507 of the protease subdomain makes an H-bond with Arg662 of the MT
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Each of the CYP enzymes alluded to
2020-07-17
Each of the CYP450 enzymes alluded to above are highly selective catalysts, in that, the three aryl coupling reactions en route the biosynthesis of 1 are catalyzed by three different CYP450 enzymes in a sequential manner (Fig. 1). In sharp gaboxadol is the recently described marine bacterial CYP450
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