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The chemical structure of curcusone D is different
2020-08-05
The chemical structure of curcusone D is different from all of the reported DUB inhibitors. It contains cross-conjugated α, β-unsaturated ketones (Fig. 1A). A similar pharmacophore was previously described in the pan-DUB inhibitor prostaglandin lipid derivatives, which function as potent Michael rec
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Steroid sexual hormones enter the
2020-08-05
Steroid sexual hormones enter the aquatic environment mainly via effluents from waste water treatment plants (WWTPs) (after incomplete removal in the plant) [10], [11]. Once in waterways, they may sorb to solid particles (bed sediments, soils) where estrogens and progestogens may persist for long pe
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Our data revealed for the first
2020-08-05
Our data revealed, for the first time, that CRL activity is required for myoblast differentiation and for the commitment of the skeletal muscle stem cells into the myogenic differentiation program. Our data highlight that MLN4924, a CRL activity inhibitor used currently as a potential cancer therapy
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Structural comparison analysis of the
2020-08-04
Structural comparison analysis of the active site cleft of CHIKV nsP2pro with that of VEEV nsP2pro revealed the substrate binding position and has led to the identification of the active site groove residues that participate in the substrate binding (Table 2). The prefixes P and S refer to the subst
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br Introduction Human urocortin II hUcn II also known
2020-08-04
Introduction Human urocortin II (hUcn II, also known as stresscopin-related peptide) and urocortin III (hUcn III also known as stresscopin) are novel members of the corticotropin-releasing factor (CRF) family that have been recently identified from the human genome data Levonorgestrel and from h
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br Conclusion This study demonstrates the presence
2020-08-04
Conclusion This study demonstrates the presence of functionally viable ET receptors in the surgically extracted tissue from patients with CTEPH. The ET receptor was associated with smooth muscle cells, mainly the contractile phenotype of SMC that surrounds the recanalised NG,NG-dimethyl-L-Argini
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There is a functional ubiquitin association UBA domain
2020-08-04
There is a functional ubiquitin association (UBA) domain at the N terminus of MCPIP1. Liang et al. have discovered that MCPIP1 may be a deubiquitinase and defined a novel DUB domain of MCPIP1 [22]. Ubiquitin and deubiquitin modification emerge as the key mechanisms that regulate the virus-induced ty
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The purposes of this study are to investigate the
2020-08-03
The purposes of this study are to investigate the molecular function of DDR2, especially in cellular proliferation in prechondrocytes, and to examine the relationship between the proliferation and differentiation of prechondrocytes through both in vitro and in vivo analysis. Materials and methods
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A recent letter by Pfizer
2020-08-03
A recent letter by Pfizer of a directed library of pyrazole-4-acetic acids also highlighted a general absence of activity for this substructure. However, this was in salubrinal to some very potent pyrazoles of similar general structure exemplified by Boehringer Ingelheim. When we investigated furt
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Next zinc was reloaded via direct addition or redialysis
2020-08-03
Next, zinc was reloaded via direct addition or redialysis. The activities of CPG2 exposed to 8-, 16- and 24-ns pulses recovered to 81.1±3.9%, 70.0±4.4% and 67.9±3.6% (p=0.1258, 0.0011, 0.0002) after direct addition, and to 94.7±3.4%, 84.0±5.2% and 81.7±7.0% (p=0.0853, 0.0741, 0.0668) after redialysi
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We observed that mutation of substrate degrons
2020-08-03
We observed that corticotropin-releasing factor of substrate degrons greatly reduces the impact of activator on the Km for E2, suggesting that degron binding promotes an increase in E2 affinity. How might this occur? Perhaps substrate binding to the activator C-terminal WD40 domain influences the a
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br Experimental section br Acknowledgements This work was su
2020-07-31
Experimental section Acknowledgements This work was supported by the Natural Science Foundation for Colleges and Universities in Jiangsu Province (No. 11KJB350002), the Natural Science Foundation of Jiangsu Province (No. BK2012422, BK20141015) and the National Natural Science Foundation of Chi
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br Introduction A major limiting factor in cancer chemothera
2020-07-31
Introduction A major limiting factor in cancer chemotherapy is the toxicity of cytotoxic drugs to normal tissues. Attempts to circumvent this problem have led to the tumour targeting approach, and TPMPA to tumour-associated proteins have been used in the development of a number of targeted anti-t
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Chiral pesticides may behave with significant enantioselecti
2020-07-31
Chiral pesticides may behave with significant enantioselectivity toward non-target organisms, including humans (Drăghici et al., 2013). Therefore, evaluating how MCL interacts with non-target organisms from an enantioselective standpoint is essential to assess its risks (Drăghici et al., 2013). In t
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br Conflicts of interest br Financial support
2020-07-31
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; 91818
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