• For a physiologically relevant interaction ligand and recept

  2020-08-10

  

  For a physiologically relevant interaction, ligand and receptor have to be expressed in the same place. Collagen II is found primarily in cartilage. DDR2 is expressed in proliferating chondrocytes in vivo, and its staining pattern in tibial growth plates is similar to that of collagen II. In additio

• Leupeptin In a cell based functional assay the antagonist

  2020-08-10

  

  In a cell-based functional assay, the antagonist properties of were assessed by measuring inhibition of CRF-stimulated cyclic adenosine monophosphate (cAMP) production in human Y-79 retinoblastoma cells. produced a concentration-dependent inhibition of CRF (1nM)-induced cAMP production with an IC va

• Next to organophosphates carbamates and metals

  2020-08-10

  

  Next to organophosphates, carbamates and metals, cholinesterase activity can also be affected by other pesticides, such as newer generation neonicotinoid insecticides (NN). NNs do not inhibit AChE activity via the organophosphate-sensitive binding site of the enzyme, but rather, by acting as a struc

• We showed for the first time that ivermectin significantly

  2020-08-10

  

  We showed for the first time that ivermectin significantly reduced the pH-induced response of the pHCl-A variant at 300nM, whereas fipronil and γ-BHC had no significant effects on the channel unlike in RDL and GluCl (Fig. 4). Such a concentration is similar to the threshold at which ivermectin activ

• br Materials and methods br Results br Discussion In particu

  2020-08-10

  

  Materials and methods Results Discussion In particular, we showed that pancreatic neuroendocrine tumor 486 2 synthesis recognize cAMP as a stimulatory signal for cell proliferation. Conversely, cAMP was found to have an inhibitory effect on cell proliferation in bronchial carcinoids cells.

• From an industrial perspective the

  2020-08-10

  

  From an industrial perspective, the low turnover numbers and limited substrate scope of α-KG halogenases still represents a significant challenge. However, in light of the fact that currently no chemical processes are available for the selective halogenation of aliphatic carbon centers in complex mo

• Several effective strategies have been developed

  2020-08-10

  

  Several effective strategies have been developed to design activatable MR probes according to the Solomon, Bloembergen and Morgan (SBM) theory, including modulation of the number of inner-sphere water molecules (q), the rotational tumbling time (τ) and the residence lifetime of inner-sphere water mo

• The generation of ROS in addition to eliciting oxidative str

  2020-08-10

  

  The generation of ROS, in addition to eliciting oxidative stress, is an important proapoptotic signal (Ott et al., 2007). Apoptosis is clearly associated with the production of ROS, since ROS generation occurs in the mitochondrial respiratory chain and disturbs mitochondrial homeostasis, which plays

• We propose that unlike other

  2020-08-10

  

  We propose that, unlike other autophagy genes, the specific increase in the expression of IRGM by pEIF2A plays a major role as a checkpoint allowing host cell survival by autophagy or host cell elimination by necroptosis. The localization of IRGM to the mitochondrial inner membrane, its ability to i

• Exposure to ultraviolet radiation with

  2020-08-10

  

  Exposure to ultraviolet radiation with sunlight is generally accepted as the major cause of basal-cell carcinoma (Gallagher et al., 1995). The risk of this disease is significantly increased by age. Skin cancers are the most common tumours of the head and neck region and their prevalence shows progr

• br Ubiquitin Capture by the

  2020-08-10

  

  Ubiquitin Capture by the Mobile APC11 RING Domain Contributes to Processive Substrate Ubiquitylation Although the rules of Ub-mediated proteolysis are only beginning to emerge, the rate and order in which different APC/C substrates are degraded during the Nilotinib correlates with processivity of

• The human serotonin hydroxytryptamine HT receptor

  2020-08-09

  

  The human serotonin (5-hydroxytryptamine; 5-HT) receptor family consists of 14 receptor subtypes to date, which are primarily G protein-coupled receptors (GPCRs) with 5-HT3 being the sole ligand-gated ion channel (Alexander et al., 2017). These receptors are widely distributed in the central and per

• One series of EP receptor antagonists we

  2020-08-08

  

  One series of EP receptor antagonists we have reported is exemplified by the pyrazole derivative . We have also disclosed some related work from this series where we identified replacement heterocycles for the pyrazole, such as the thiazole derivatives and and the pyridine derivatives and . We fo

• (-)-p-Bromotetramisole Oxalate Our previous studies have dem

  2020-08-08

  

  Our previous studies have demonstrated that the DDR2 discoidin domain fully contains the binding site(s) for the fibrillar collagens I and II (Leitinger, 2003, Leitinger et al., 2004). The binding site for collagen I was mapped to three spatially adjacent surface loops within the DDR2 discoidin doma

• TRIM was first identified as glycogenin interacting

  2020-08-08

  

  TRIM7 was first identified as glycogenin interacting protein (GNIP) and has been reportedly involved in glycogen synthesis. Knockdown of Trim7 in the primary(KP) lung tumor vx 20 could reduce cell proliferation and decrease the tumor growth in xenograft experiments. Consistently, deletion of Trim7

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