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br ET Antagonist for the Future Macitentan and
2020-07-01

ET Antagonist for the Future: Macitentan and Atresentan Macitentan is an insurmountable antagonist, resulting from structure-activity studies to improve the efficacy and tolerability of bosentan, and gained approval in the United States in 2013 for the treatment of PAH. Actelion describes the com
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br Introduction Mammalian proteases comprise both the peptid
2020-07-01

Introduction Mammalian proteases comprise both the peptidases or exopeptidases, which act at the N- or C-terminal positions of polypeptides, and proteinases or endopeptidases, which are capable of cleaving peptide bonds in the central regions of polypeptides. The endopeptidases are classified in
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ApoE is secreted from astrocytes glia into the
2020-07-01

ApoE is secreted from astrocytes/glia into the interstitial fluid and is important for metabolizing Aβ because of its propensity for binding Aβ as a cholesterol and phospholipid acceptor in reverse cholesterol transport [8]. Aβ oligomers show a direct toxicity to neurons, and ApoE inhibits oligomer
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br Acknowledgements br Introduction Supramolecular collagen
2020-07-01

Acknowledgements Introduction Supramolecular collagen assemblies are crucial for the mechanical stability of animal bodies (Myllyharju and Kivirikko, 2004). The basic collagen structure is a triple helix of three chains containing multiple Gly-X-X\' repeats; X and X\' are often proline and 4-h
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In humans several different small ubiquitin related
2020-07-01

In humans, several different small ubiquitin-related modifier (SUMO) paralogs can be conjugated to cellular proteins. The human genome codes for five SUMO paralogs (SUMO1–5); of these, SUMO1 and the almost identical SUMO2 and SUMO3 are ubiquitously expressed. Sumoylation is executed by an enzymatic
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In contrast to SQLE HMGCR could
2020-07-01

In contrast to SQLE, HMGCR could be efficiently degraded in AZD-4547 lacking UBE2J2. However, this was not the case in cells devoid of UBE2G2, as these cells were unable to support 25-hydroxycholesterol (25-HC)-stimulated degradation of HMGCR (Fig. 1C). This finding is consistent with our recently
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A number of factors have been shown to
2020-07-01

A number of factors have been shown to remove blocking end groups in order to make the termini of DSBs ligatable. A common non-ligatable end is one that contains either a 3′ phosphate or 5′ hydroxyl. The polynucleotide kinase/phosphatase (PNKP) is the NHEJ processing enzyme responsible for removing
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In summary these results are consistent with our hypothesis
2020-07-01

In summary, these results are consistent with our hypothesis that chemical nitrosation of BMAA to N-BMAA results in the formation of an alkylating agent. Furthermore, we have shown that N-BMAA is more toxic than BMAA itself. Previously, methylazoxymethanol (MAM), which is also present in the cycad n
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br Methods br Discussion In a recent
2020-06-30

Methods Discussion In a recent survey among 2625 high risk patients on atorvastatin, 10.5% of patients achieved an LDL-target of rho kinase inhibitors level for improvement of acceptance and adherence to effective lipid lowering therapy are warranted to maximize the benefits of standard treat
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The use of the periplasmic
2020-06-30

The use of the periplasmic fraction as starting material and the presence of a unique purification step concurred in improving the purification yield to 25.3%, which is significantly higher than what obtained with the previous purification protocol (6.7%). In addition, the analysis of the kinetic co
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In a recent report Yoshihara and colleagues used transcripto
2020-06-30

In a recent report, Yoshihara and colleagues (2016) used transcriptomes derived from freshly isolated islets of 2-week-old neonatal, 6-week-old young adult, or 12-week-old adult mice to interrogate how maturation is regulated to acquire glucose responsiveness. The authors observed that estrogen-rela
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br Introduction Receptor tyrosine kinases RTKs
2020-06-30

Introduction Receptor tyrosine kinases (RTKs) are critically involved in the development and progression of human cancers and are therefore useful targets for anti-cancer therapies [1]. The Eph receptors represent the largest subfamily of receptor protein kinases and interact with ligands called
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The assembly and maturation of invadopodia can be initiated
2020-06-30

The assembly and maturation of invadopodia can be initiated by chemical stimuli such as the epidermal growth factor (EGF), as well as the mechanical signals from extracellular matrix (ECM). Upon binding, EGF activates the EGF receptor (EGFR), which further activates several intracellular signaling p
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br Assessing DUB activity The Ub field
2020-06-30

Assessing DUB activity The Ub field has benefited greatly from the past efforts of biochemists and chemical biologists who have reconstituted Ub signals in vitro and generated tools for capturing or measuring DUB activities, many of which can be readily produced or are commercially available (Ekk
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br Discussion The differences in the kinetic
2020-06-30

Discussion The differences in the kinetic properties of L-AmDH and LeuDH presented herein reflect a different kinetic mechanism. When compared to its parent enzyme, L-AmDH displayed a different substrate binding order, lower affinity for the keto substrate, and stronger product inhibition. The tw
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