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The second DDR binding partner identified
2020-05-13

The second DDR1-binding partner identified here, Shp-2, which was not found in the two-hybrid screen but using a bioinformatics approach, is also a mediator of cell migration. Since Shp-2 has two SH2 domains, as well as phosphotyrosine phosphatase enzymatic activity and two C-terminal tyrosines targ
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br Ubiquitination and deubiquitination pathways Ubiquitinati
2020-05-12

Ubiquitination and deubiquitination pathways Ubiquitination is a part of the post-translational modification (PTM) process. Ubiquitination affects proteins in various ways, but its main functions are to signal protein degradation via the 26S proteasome, modify cellular location of proteins, affec
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Fig D shows that E lagascae
2020-05-12

Fig. 2D shows that E. lagascae VIR E gives two species of radioactive TAG: one represents 45% of total labelled TAG and the smaller more-polar spot (15%) is probably derived from the endogenous 1,2-divernolin instead of the exogenous 1,2-diolein. In this case, the total scintillation counts were gre
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Preparation of the regioisomeric pyridooxazepinones
2020-05-12

Preparation of the regioisomeric pyridooxazepinones 10 and 11 was accomplished utilizing the synthetic sequence depicted in Scheme 3. Amide coupling of 63 and BRD 7389 chloride 64 afforded amide 65. Removal of the alcohol protecting group, followed by base catalyzed cyclization afforded a 1:2.4 mixt
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Saito et al reported that
2020-05-12

Saito et al. reported that diabetic bone has lower lysyl oxidase-derived enzymatic cross-links in collagen compared to non-diabetic bone, based on studies performed in a rat model [9]. Lysyl oxidase plays a pivotal role in bone development and function, as revealed in classical studies [10], [11]. L
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br Materials and methods br Acknowledgments br Introduction
2020-05-12

Materials and methods Acknowledgments Introduction Proton pumps convert the energy of high-energy compounds into the DL-α-Difluoromethylornithine hydrochloride hydrate mg of protons across biomembranes. They play two physiological roles: pH regulation and the formation of proton-motive forc
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In the particular case of metals several authors showed
2020-05-12

In the particular case of metals, several authors showed that AChE inhibition is somewhat contradictory and even questionable (Frasco et al., 2005, Nunes et al., 2005, Sáenz et al., 2010). Uranium is a particular metal, and one that has been shown to complex with several biologically important prote
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In S cerevisiae Mek a paralog of the checkpoint
2020-05-12

In S. cerevisiae, Mek1, a paralog of the checkpoint kinase Chk2, mediates cell-cycle arrest in response to meiotic defects (Bailis and Roeder, 2000, Xu et al., 1997). Mek1 is associated with meiotic chromosome axes, where its activation requires interactions with two other axis proteins, Hop1 and Re
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br Materials and methods br Results br Discussion DAS
2020-05-12

Materials and methods Results Discussion DAS and nilotinib, as the second potent, oral generation TKIs, bind to both the active and inactive conformation of the ABL1 kinase domain, have been found to be effective in treating patients with IM resistant or intolerant CML-CP, and inhibit all t
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For the current studies we used the selective Epac agonist
2020-05-12

For the current studies, we used the selective Epac agonist 8CPT-AM to directly activate the proteins. We chose this pharmacological approach since it allows a direct activation of Epacs rather than using receptor agonists such as PGE2 which could introduce confounding variables. One potential conce
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Proof of concept studies with disulfiram suggest the
2020-05-12

Proof-of-concept studies with disulfiram suggest the potential utility of DβH inhibitors for treatment of cocaine use disorder. In a study of 74 subjects stabilized on methadone and randomized into disulfiram and placebo groups for 10weeks, disulfiram treatment reduced cocaine-positive urines, and d
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Some pyrimidine analogs are substrate based inhibitors that
2020-05-12

Some pyrimidine analogs are substrate-based inhibitors that bind to the dihydroorotate binding site, but most reported inhibitors of DHODH bind to the site occupied by the ubiquinone co-factor., , , , , , , , , , , , , , , , , X-ray crystallographic studies of inhibitor complexes with DHODH and DHO
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PD 169316 br Acknowledgements This work was supported by gra
2020-05-12

Acknowledgements This work was supported by grants from Agence Nationale de la Recherche (ANR CAPHE) and from Ligue contre le Cancer. We acknowledge the continuous support of CNRS and the University of Strasbourg. We thank the technical assistance of the “Plateforme de Chimie Intégrative de Stras
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br Acknowledgment This work was supported
2020-05-11

Acknowledgment This work was supported by the Estonian Science Foundation (Grant ETF8862). Introduction In higher eukaryotes ionizing-radiation (IR) induced DNA double-strand breaks (DSB) are primarily repaired by the non-homologous end joining (NHEJ) pathway [1]. Ku, a heterodimeric protein
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br Results br Discussion Our UbV library was
2020-05-11

Results Discussion Our UbV library was originally designed to develop inhibitors of deubiquitinases (Ernst et al., 2013). Recently, we showed that UbVs could exhibit multiple binding modes and mechanisms to modulate HECT E3 activity (Zhang et al., 2016)—one set occupied the HECT domain E2-bind
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