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The development of novel approaches to study GPCR
2021-03-02
The development of novel approaches to study GPCR-mediated transactivation in live elastase inhibitor is important, and this study describes a unique BRET-based quantification of Grb2 recruitment to the EGFR as a direct readout of GPCR-mediated transactivation. We have previously used the recruitme
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Muscle Ring Fingers MuRFs comprising TRIM MuRF
2021-03-02
Muscle Ring Fingers (MuRFs) comprising TRIM63 (MuRF1), TRIM55 (MuRF2) and TRIM54 (MuRF3) are the most studied TRIMs in the heart. However, with increasing knowledge of E3 ligases and recent advancements in the field, many other TRIMs such as TRIM8, TRIM21, TRIM24, TRIM32, TRIM45, TRIM69 and TRIM72 w
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br Anti inflammatory effects of MTX In addition to cytotoxic
2021-03-02
Anti-inflammatory effects of MTX In addition to cytotoxic and cytostatic effects, the anti-inflammatory activity of MTX was also described by several studies. Inhibition of ATIC by MTX has been found to result in the accumulation of 5-aminoimidazole-4-carboxamide-1-β-d-ribofuranosyl 5′-monophosph
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BIX 02565 In this review focusing on biocatalyst formate
2021-03-02
In this review, focusing on biocatalyst “formate dehydrogenase FDH” catalyzing both of the formic BIX 02565 oxidation to CO2 and the CO2 reduction to formic acid, representative examples of properties, types, structure of active-site of FDH and, reaction mechanism of formic acid oxidation and CO2 r
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In the course of our program which was
2021-03-02
In the course of our program, which was aimed at developing CRTH2 antagonists for the treatment of allergic diseases, we have been pursuing a new class of potent and selective CRTH2 antagonist lead based on the structures of CRTH2 antagonists known to date (, , ). Using a fused 6–6-membered ring sys
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Unlike the CRF receptor the CRF a receptor binds and
2021-03-02
Unlike the CRF1 receptor, the CRF2(a) receptor binds and is activated by agonists with a broad range of potencies. Therefore, we assessed the ability of strong and weak ligands to desensitize retinoblastoma CRF2(a) receptors. Although stresscopin's N-terminus is two Bikinin longer than the N-terminu
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Although differences in several nociceptive tests have previ
2021-03-02
Although, differences in several nociceptive tests have previously been described across strains (Mogil et al., 1999), it is the first time that pain sensitivity in response to chemical and thermal stimuli has been evaluated in B6,129CRHtklee mice. Our results showed no differences in pain sensitivi
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A recent report has shown that C elegans homozygous for
2021-03-02
A recent report has shown that C. elegans homozygous for a point mutation within the HORMA domain of HTP-1 (M127K), which disrupts its association with chromosome axes, displayed an extended zone of PLK-2 localization to PCs in response to asynapsis (Silva et al., 2014), which, as we show here, is a
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I bungarotoxin competes with ACh
2021-03-02
[125I] α-bungarotoxin competes with ACh, an endogenous activator of α7-nACh receptors by binding to the ACh binding site on the receptor (Albuquerque et al., 2009). For this reason, the effect of curcumin was investigated on the specific binding of [125I] α-bungarotoxin. Saturation curves for the bi
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The EGFR belongs to the ErbB family
2021-03-01
The EGFR belongs to the ErbB family of receptor tyrosine kinases (RTKs), comprised of four members: EGFR (ErbB1, HER1), HER2 (ErbB2), HER3 (ErbB3) and HER4 (ErbB4) [24]. HER receptors are activated by a group of epidermal growth factor (EGF) ligands and undergo homo- or hetero-dimerization during th
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At the therapeutic level the logical approach to address
2021-03-01
At the therapeutic level, the logical approach to address the cooperation between FGFR4 and EGFR was the combined inhibition of both receptors. To explore the potential efficacy and specificity of this approach, we tested the effect of FGFR and EGFR inhibitors in monotherapy or in combination in syn
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2-Amino-ATP br A brief history of RBR E s
2021-03-01
A brief history of RBR E3s RBR E3s were originally defined based on sequence alignments that predicted a tripartite motif of three zinc (Zn)-binding domains: two RING domains (RING1 and RING2) connected via an in-between-RING (IBR) domain [28], [29]. The prediction together with initial observati
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E is a classical initiator
2021-03-01
E1 is a classical initiator protein and, as such, plays several roles in the initiation and catalysis of viral DNA synthesis. E1 must first recognize a specific segment of the viral martphone known as the “origin of DNA replication”, or “ori” for short. For most PV types examined to date, the minim
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The authors identified inhibitors of SUMOylation using two a
2021-03-01
The authors identified inhibitors of SUMOylation using two assays to monitor the conjugation of SUMO1 to RanGAP1 by E1 and E2 enzymes: a fluorescence resonance energy transfer (FRET) primary screen that evaluated over 250,000 compounds and a chemiluminescence secondary screen. A counter screen was u
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Verapamil a calcium channel blocker used clinically as
2021-03-01
Verapamil, a calcium channel blocker used clinically as a coronary vasodilator, was amongst the first compounds identified that could reverse MDR and potentiate the effects of MDR1 substrates such as vincristine [15], [16]. Verapamil, along with a number of other MDR1 blockers, have proved largely u
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