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E ubiquitin ligases are key players in the ubiquitin
2021-05-17
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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In attempts to further purify His Artemis
2021-05-17
In attempts to further purify [His]6-Artemis, numerous matrices were assessed including anion and cation exchange, and Eltrombopag interaction chromatography. The results from these matrices were universally poor (data not shown). Fractionation via adsorption chromatography on a hydroxyapatite (HAP)
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Our previous studies have demonstrated that the DDR discoidi
2021-05-17
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
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br Experimental procedures br Introduction Protein
2021-05-17
Experimental procedures Introduction Protein kinases represent one of the largest enzyme MPI-0479605 synthesis in the human genome and act as signaling mediators in a variety of cellular processes (Manning et al., 2002). Because many diseases are associated with aberrant protein kinase activit
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5224 synthesis br Materials and methods br Acknowledgments b
2021-05-17
Materials and methods Acknowledgments Introduction Proton pumps convert the energy of high-energy compounds into the 5224 synthesis of protons across biomembranes. They play two physiological roles: pH regulation and the formation of proton-motive forces in their membranes. The simplest of
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Moreover a ligand for fusin has recently been found
2021-05-17
Moreover, a ligand for fusin has recently been found: the lymphocyte chemoattractant stromal-derived factor-1 (SDF-1) binds to CHO resazurin mg transfected with fusin and promotes secondary messenger production (Bleul et al., 1996; Oberlin et al., 1996). A new name, CXCR-4, has been proposed for th
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Another important mediator in fear
2021-05-17
Another important mediator in fear learning is the neuropeptide corticotropin-releasing factor (CRF). For example, local repeated administration of CRF into the basolateral amygdala potentiates the acquisition of cue-conditioned fear (Bijlsma et al., 2011) and CRF1 receptor antagonists effectively b
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br Acknowledgements Professor Olli A J nne is
2021-05-17
Acknowledgements Professor Olli A. Jänne is warmly thanked for support and for providing excellent research facilities. Professor Patrik Finne is acknowledged for his help with statistical analyses. Drs Ronald Evans, Vincent Giguère, Jorma Palvimo, Malcolm Parker, and Anastasia Kralli are acknowl
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br Role of ERK signaling
2021-05-17
Role of ERK signaling in preventive and therapeutic potential of flavonoids in neurodegenerative diseases ERK is one of the main pharmacological targets of natural phenolic compounds and contributes to several therapeutic approaches including anti-atherogenic, anti-cancer, anti-colitis, anti-arth
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Our previous high throughput screening HTS campaign
2021-05-17
Our previous high-throughput screening (HTS) campaign using automated, robust, and sensitive fluorescence based 1,3-PBIT dihydrobromide assay [10], [11] led to the identification of several EPAC specific inhibitors (ESIs), and was subsequently followed by extensive hit-to-lead optimizations [20], [
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A769662 br Introduction Cerebral stroke causes an efflux of
2021-05-17
Introduction Cerebral stroke causes an efflux of various groups of progenitor and stem cells from bone marrow to bloodstream and the levels of these cells correlate with neurological status of stroke patients (Gójska-Grymajło et al., 2012, 2018). It is thought that paracrine factors produced by t
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The roles of ginsenoside in E and S
2021-05-17
The roles of ginsenoside in E1 and 26S proteasome inhibition are shown in Table 2. The nitro substitute on the furan ring may be important for PYR-41 inhibition of the E1 enzyme (Yang et al., 2007). The macrocycle core and aliphatic tail of Largazole are responsible for inhibiting E1 activity (Unger
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Here we explored the relative contribution of D
2021-05-17
Here we explored the relative contribution of D1-like and D2-like receptor subtypes in the control of glutamate release, as well as their pharmacological properties and their interactions modulating the release. The pharmacological parameters (EC50 and Emax) of dopamine for the different types of re
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br Acknowledgements The authors are supported by National In
2021-05-17
Acknowledgements The authors are supported by National Institutes of Health grants (CA162804, CA92584, and CA13499 to DJC and CA166677 to BPPC) and Cancer Prevention and Research Institute of Texas (RP110465 to DJC). The cellular response to DNA double-strand break (DSB) formation is an essent
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The collagen binding membrane proteins
2021-05-14
The collagen-binding membrane proteins, discoidin domain receptors 1 and 2 (DDR1 and DDR2) belong to the family of receptor tyrosine kinase and are expressed in a variety of mammalian cells.7, 8 These transmembrane glycoproteins (∼125 kDa) have been found to be over-expressed or atypically expressed
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