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Historically covalent drugs have had great success
2021-04-09
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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In children only the genotype was
2021-04-09
In children, only the 6/7 genotype was associated with spina bifida, increasing the risk about 4 times relative to the DHFR 3/3 and 6/6 genotypes. However, the 95%CIs are broad and only few spina bifida patients have the DHFR 6/7 genotype. The effect of the 6/7 genotype on spina bifida risk is there
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The interest for lanthanide and actinide complexes appeared
2021-04-08
The interest for lanthanide and actinide complexes appeared again recently, due to their unique features in the design of Single Molecule Magnets (SMM). Lanthanide SMMs are interesting due to large their intrinsic magnetic anisotropy, but their core 4f orbitals minimally participate in exchange inte
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Finally we demonstrated for the first time
2021-04-08
Finally, we demonstrated for the first time that the physiological combinations of estradiol and progesterone levels of premenopausal and postmenopausal women efficiently stimulated the growth of T47D spheroids while clinically relevant concentrations of TPA and UPA suppressed the growth of T47D sph
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As for the molecular mechanism Ferguson
2021-04-08
As for the molecular mechanism, Ferguson BD suggested that EphB4/EphrinB2 stimulation induced topoisomerase I activity in small cell lung cancer cell lines. Treatment of Tolvaptan with EphrinB2/Fc induced topoisomerase activity as assessed by DNA relaxation in cells with high EphB4 expression level
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br Abbreviations br Introduction br Collagen
2021-04-08
Abbreviations Introduction Collagen-induced DDR activation A key feature of DDRs is their ability to bind both fibrillar and non-fibrillar collagens (Shrivastava et al., 1997, Vogel et al., 1997). DDR1 and DDR2 recognize the GVMGVO (O, hydroxyproline) motif within fibrillar collagens I–III
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Splitomicin br Conflicts of interest br Financial
2021-04-08
Conflicts of interest Financial support NZ is an Established Investigator of the Dutch Heart Foundation (2013T111) and is supported by an ERC Consolidator grant (617376) from the European Research Council and by a Vici grant from the Netherlands Organization for Scientific Research (NWO; 9181
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In conclusion adipose PGD suppressed the lipolysis by
2021-04-07
In conclusion, adipose PGD2 suppressed the lipolysis by decreasing the intracellular cAMP level through DP2R. Therefore, PGD2 enhanced adipocyte differentiation (lipid accumulation) through both repression of the lipolysis via DP2R and activation of the lipogenesis via PPARγ. Thus, L-PGDS and DP2R a
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In the original ELF study patients were
2021-04-07
In the original ELF study [7], patients were considered eligible if they were due to undergo liver biopsy for the investigation of chronic liver disease, defined as abnormal biochemical liver function tests persisting for more than 6 months, ability to provide informed consent and age between 18 and
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Phytophthora capsici is a phytopathogenic oomycete a lineage
2021-04-07
Phytophthora capsici is a phytopathogenic oomycete, a lineage of eukaryotic microorganisms in the kingdom Stramenopila, which causes devastating diseases on many economically important vegetables [15]. Hyps are present in the Phytophthora cell wall proteins [16] and phytotoxic elicitor proteins [17]
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Next to organophosphates carbamates and
2021-04-07
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
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2 hydroxyglutarate Neutrophils produce high amounts of ROS w
2021-04-06
Neutrophils produce high amounts of ROS, which act as antimicrobial agents, signaling molecules or initiators during PMA-induced NET formation. Of the intravenous anesthetics used in this study, propofol was the best at decreasing PMA-induced ROS levels (Fig. 3A and B). Our previous study also demon
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Apart from the ET system s role in regulating blood
2021-04-06
Apart from the ET system's role in regulating blood vessel tone, it is also involved in a variety of cellular processes that are relevant to DR. For example, the ET receptors influence the survival of retinal ganglion Tolfenpyrad (McGrady et al., 2017; Tonari et al., 2012), development of the reti
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Metal ions are known not to
2021-04-06
Metal ions are known not to be necessary for catalytic activity of serine proteinases. Nevertheless, Co2+ and Ca2+ ions were found to stabilize glutamyl endopeptidase molecule [1], [7], [19]. In our previous study, we have described significant stimulating effect of Ca2+, Mg2+, and Co2+ on biosynthe
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In studies directed toward the development of sequence speci
2021-04-06
In studies directed toward the development of sequence-specific major-groove binding small bcrp transporter [11], we desired a non-intercalating molecular scaffold that could direct attached moieties into the major groove. As an initial step toward this goal, we wished to study the DNA binding mode
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