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E ubiquitin ligases are key players in the
2019-11-12
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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The findings of Qiu et al represent the
2019-11-12
The findings of Qiu et al. (2016) represent the first instance of a Ub-specific mono-ADP-ribosyltransferase, as well as the first documentation of E1/E2 independent ubiquitination. Post-translational modification of Ub certainly adds layers of complexity to our understanding of the Ub signal and sho
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Historically covalent drugs have had great success e g
2019-11-12
Historically, covalent drugs have had great success (e.g., aspirin and penicillin), and covalent drugs have become a focus in anticancer and antiviral drug discovery (Kalgutkar and Dalvie, 2012, Singh et al., 2011). These compounds contain low reactivity warheads that allow covalent adducts to form
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DGAT is specifically responsible for
2019-11-12
DGAT2 is specifically responsible for endogenous synthesis of TAGs which are then packed into cytosolic LDs in the cytosol for storage and luminal apolipoprotein B (apoB)-containing LDs in the ER lumen destined for VLDL secretion [122,127]. DGAT2 can also synthesize TAG using exogenous FAs and suppo
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Compounds were prepared via the
2019-11-12
Compounds were prepared via the routes shown in , varying the sequence of reactions to install the thiazole or the phenyl ring at the end of the synthesis (pyridyl examples were prepared using similar chemistry). The aminothiazole building blocks were prepared as shown in . 5-Aminothiazole was prep
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One significant finding in this
2019-11-12
One significant finding in this study was the overexpression of a protein identified as LysM domain/BON superfamily protein [29], [30]. This protein was highly overexpressed in the meropenem-treated condition. InterProScan analysis revealed that the LysM domain/BON superfamily protein consisted of t
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CBiPES hydrochloride Defensins are one major class of antimi
2019-11-11
Defensins are one major class of antimicrobial, cationic peptides that are released from CBiPES hydrochloride and imbedded in the mucus layer on mucosal surfaces [45]. They can be categorized into two major families; α- and β-defensins. In humans there are two α-defensin members, defensin 5 (HD5) a
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While lowering the TID exposure of electronics is fairly str
2019-11-11
While lowering the TID exposure of electronics is fairly straightforward, there are other ic propranolol induced effects that are not as easily mitigated, especially with COTS components. Single Event Effects (SEE) occur when a high-energy particle strikes the active area of an integrated circuit, c
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The availabilities of serotonin and dopamine are modulated b
2019-11-11
The availabilities of serotonin and dopamine are modulated by the serotonin transporter and catechol-O-methyltransferase enzyme. The serotonin transporter (5-HTT) is a key protein that reuptakes serotonin from the synaptic cleft back into synaptic boutons (Coleman et al., 2016; Talvenheimo et al., 1
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In SLO permeabilized human sperm the AR
2019-11-11
In SLO-permeabilized human sperm, the AR elicited by calcium, persistently active Arf6 [41] and Rab3A, 8-pCPT-2′-O-Me-cAMP [8], diacylglycerol and a non-hydrolyzable analog [35], is sensitive to the PLC blocker U73122. Furthermore, 8-pCPT-2′-O-Me-cAMP elicits a calcium signal in non-permeabilized sp
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br Lymphoplasmacytic lymphoma Waldenstrom macroglobulinemia
2019-11-11
Lymphoplasmacytic lymphoma/Waldenstrom macroglobulinemia Lymphoplasmacytic lymphoma (LPL) and its subgroup Waldenstrom macroglobulinemia (WM) are rare and indolent lymphomas that arise from fully differentiated B cells. The only family of GPCRs that has been well studied in LPL/WM is the chemokin
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Introduction Double strand break DSB
2019-11-11
Introduction Double strand break (DSB) is the most deleterious damage that threats DNA integrity. This frequent damage arises from environmental stress like UV, chemical agents or ionizing radiations (IRs). Although environmental stress does not lead directly to DSB, it produces [Ala92]-p16 (84-103
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In a previous study we reported that the
2019-11-11
In a previous study we reported that the systemic administration of the α1-adrenergic receptor antagonist prazosin attenuates the deficit in Erteberel reward function associated with precipitated nicotine withdrawal (Bruijnzeel et al., 2010). One of the aims of the present experiments was to investi
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In attempts to further purify His
2019-11-08
In attempts to further purify [His]6-Artemis, numerous matrices were assessed including anion and cation exchange, and Ac-YVAD-CHO 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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AAG has a broad substrate
2019-11-08
AAG has a broad substrate specificity and besides 3-methyladenine can excise other altered purine residues, such as the minor lesions hypoxanthine and 1, N6-ethenoadenine from DNA. AAG initially activates these neutral base lesions by protonation of the base to allow for general thing catalysis [16]
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