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br Introduction Natural killer NK cells have an unique abili
2020-09-01

Introduction Natural killer (NK) cells have an unique ability to directly lyse transformed, virus-infected or stressed cells without prior sensitization or major histocompatibility complex (MHC) class I restriction [1], [2]. They were initially defined and shown to be important effectors of the i
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Among prostaglandins PG PGD remained the
2020-09-01

Among prostaglandins (PG), PGD2 remained the most elusive species for a long time and was initially regarded as having negligible biological activity [1]. In 1974 its inhibitory effect on platelet aggregation was discovered by Smith et al. [2] and Mills & McFarlain [3], and both pressor and depresso
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MAPKs are a family of
2020-09-01

MAPKs are a family of phosphorylating enzymes that orchestrate various cellular response in proliferation, apoptosis, inflammation, stress response, and energy metabolism [11]. There are at least four major members including extracellular signal-regulated kinase 1 and 2 (ERK1/2), p38 mitogen-activat
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br Advent of SMEPT br SMEPT
2020-09-01

Advent of SMEPT SMEPT for localized synthesis of nitric oxide Critical evaluation and outlook Examples discussed in this review present SMEPT as a methodology for localized drug synthesis – a unique opportunity for site specific therapeutic interventions using implantable biomaterials. This
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The isomeric phenyloxazole not only exhibited
2020-09-01

The isomeric 5-phenyloxazole not only exhibited increased potency against NEP, but also a decreased ACE inhibition thus providing encouraging selectivity. Changing the P1 group from an -propyl to a more polar methoxyethyl at the left hand beta lactamase inhibitor (as seen in compound pairs – and –
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br Activity based probes br Characterization of coronavirus
2020-09-01

Activity-based probes Characterization of coronavirus-encoded DUBs with activity-based probes To study the activity of specific DUBs, investigators frequently take advantage of the ~10kDa (monoUb or Ubl ABP) or ~20kDa (DiUb ABP) increase in MW on probe labeling. SDS-PAGE analysis or blotting f
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Total synthesis requires the two key intermediates and
2020-09-01

Total synthesis requires the two key intermediates 3 and 7, which were synthesized using the route described in below. Phenylethylamine 3 was readily synthesized from vanillin or isovanillin; the overall yield was 50–52%. To prepare the intermediates 7, bromination of 2-(4-hydroxyphenyl) acetate wi
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In some cases more than one CYP
2020-08-31

In some cases, more than one CYP450 enzyme may be involved in the metabolism of a drug, and an Eadie–Hofstee plot is usually more reliable for assessing the involvement of multiple squalene epoxidase (Bu, 2006). Therefore, we first plotted the Eadie–Hofstee curves and observed their shape to determ
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Exposure to ultraviolet radiation with sunlight is generally
2020-08-31

Exposure to ultraviolet radiation with sunlight is generally accepted as the major cause of basal-cell carcinoma (Gallagher et al., 1995). The risk of this disease is significantly increased by age. Skin cancers are the most common tumours of the head and neck region and their prevalence shows progr
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br STAR Methods br Acknowledgments We thank the City
2020-08-31

STAR★Methods Acknowledgments We thank the City of Hope core facilities, including the Animal Model Core, Bioinformatic Core, NMR Core, Flow Cytometry Core, and Florescence Microscopy Core for excellent technical support, and NIH grants R01GM086171, R01GM102538, and R01CA212119, R01CA216987, an
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The murine subfamily members including and have been identif
2020-08-31

The murine subfamily members including , , , and have been identified and their encoded proteins showed deubiquitinating enzymatic activity , , , . It has been demonstrated that is an immediate-early gene induced by IL-3 in B-lymphocytes and is an IL-2 specific immediate-early gene in T-lymphoc
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Hedamycin isolated from Streptomyces griseoruber
2020-08-31

Hedamycin, isolated from Streptomyces griseoruber, belongs to the highly cytotoxic pluramycin class of BMI-1 inhibitor (Figure 3(c)). It consists of a planar anthrapyrantrione chromophore attached to two amino sugar rings at one end and a bisepoxide-containing side-chain at the other end (Figure 3(
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br Materials and Methods br Results br
2020-08-31

Materials and Methods Results Discussion HSCs have been identified as major collagen-producing GSK2606414 in the injured liver (1), and activation of HSCs has become the central link for liver fibrosis (2). The factors that regulate the biological behavior of HSCs include soluble regulatory
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br Results br Discussion Our UbV library was
2020-08-31

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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HOIP s ability to build
2020-08-31

HOIP\'s ability to build linear Ub chains arises from a unique domain that follows directly after the RING2 domain, the linear ubiquitin chain-determining domain (LDD) (Fig. 1). Structures have revealed that the LDD is structurally integrated into RING2, creating a single RING2–LDD unit (Fig. 2D) [4
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