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Carbamate and OP insecticides are still
2019-09-05

Carbamate and OP insecticides are still among the most widely used pesticides in the world [151]. In 2012, the OP insecticides chlorpyrifos and acephate were ranked 14th and 22nd overall in estimated amounts of agricultural pesticides used in the US. The carbamate insecticide carbaryl and the OP ins
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Contrary to the downregulation of S PR family GPCRs CLL
2019-09-05

Contrary to the downregulation of S1PR family GPCRs, CLL cells have increased mRNA expression of the lysophosphatidic sik inhibitor (LPA) family receptors LPAR1, LPAR3 and LPAR4 compared to normal B cells [47]. Increased LPAR1 mRNA has been shown to be associated with more aggressive disease [47] a
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Our study provides proof of principle
2019-09-05

Our study provides proof of principle for dimerizing two different E3 ligases as a novel approach to inducing one ligase to degrade the other one. The outcome of ‘ligase versus ligase’ PROTAC-mediated activity might be unpredictable a priori, but could reveal a new mechanism for proximity-mediated h
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br RING type E s and their
2019-09-05

RING-type E3s and their substrates There is enormous diversity in substrate ubiquitination and its regulation, as the targets of RING-type E3s are incredibly varied. RING-type E3s are implicated as tumor suppressors, oncogenes, and mediators of endocytosis, and play critical roles in complex mult
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br Acknowledgements The study of
2019-09-05

Acknowledgements The study of RING-type E3s continues to grow extremely rapidly. We regret that it was possible to only cite a fraction of the outstanding primary publications in this field. This work was supported by the National Institute of General Medical Sciences grants R01 GM088055 and R01
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Programmed cellular death or apoptosis is
2019-09-05

Programmed cellular death or apoptosis is a process genetically controlled that plays an important role in cellular homeostasis, being an important defense mechanism to remove cells that have been infected, damaged or mutated (Smith and Smith, 2012, Wlodkowic et al., 2011). Nevertheless, apoptosis s
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br Conclusions br Acknowledgement Grant support Ministry
2019-09-05

Conclusions Acknowledgement Grant support: Ministry of Health (n. of grant: RBAP10447J_004 to N. Baldini), Italian Association for Cancer Research (n. of grant: 11426 to N. Baldini). Introduction Ewing sarcomas (ES) and primitive neuroectodermal tumors (PNET) are related childhood tumors.
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An Emerging Role for the EphrinB
2019-09-05

An Emerging Role for the EphrinB2-EphB4-RASA1 Signaling Axis in Human Congenital Cerebrovascular Disorders Normal vascular development includes de novo blood vessel formation from endothelial cells (ECs) (vasculogenesis) 1, 2, expansion of the network through vessel sprouting, splitting, and remode
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Based upon these findings on portions A and B
2019-09-05

Based upon these findings on portions A and B, novel scaffolds of EP4 antagonist, and (R & R=()-Me; =Cl; R=H), shown in , were identified. We next focused on optimizing portion C of these scaffolds. We utilized for an alternative synthesis of nicotinamide scaffold , which is quite effective for
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Since the dideoxy analogues and served
2019-09-05

Since the 1,2-dideoxy analogues, and , served as substrates for TgTCEA and TgTCEB, respectively, with the higher affinity (lower ) and lower turnover number (lower ) than their authentic substrates, PosA and PosB (such trend was more evident on analogue for TgTCEB than on analog for TgTCEA), an i
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br Target enzyme attributes and substrate
2019-09-05

Target enzyme attributes and substrate peptide selection Protein kinases catalyze the phosphorylation of serine, threonine, and tyrosine residues in both proteins and peptides using ATP as the phosphoryl donor. The human kinome is comprised of 518 protein kinases and 40 lipid kinases. The vast ma
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It is believed that emphysema
2019-09-05

It is believed that emphysema in smokers is mediated by proteases released from inflammatory PF 04418948 that cause destruction of the extracellular matrix in alveolar septa [1]. Metalloprotease-12 is mainly released by macrophages and is considered the enzyme responsible for emphysematous lesions
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The total reduced glutathione content was determined
2019-09-05

The total reduced glutathione content was determined in both TH588 to examine whether retinol was decreasing glutathione concentrations and thus decreasing the conjugation of NAPQI. Total hepatic (3.9±0.3 vs 4.9±1.0 μmol/g, retinol vs untreated, respectively) and renal (0.4±0.1 vs 0.2±0.1 μmol/g, r
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Cyclosporine NEORAL Oral Solution Novartis is an
2019-09-05

Cyclosporine (NEORAL® Oral Solution, Novartis) is an immunosuppressant widely used in organ transplantation and many other clinical conditions [12]. It undergoes extensive hepatic and intestinal biotransformation mainly via the metabolizing enzyme, CYP3A4 [[12], [13], [14], [15]]. Considering the na
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br Physiological roles for EPAC
2019-09-04

Physiological roles for EPAC isoforms: vascular function The effects of cAMP on limiting vascular endothelial cell (VEC) inflammation and vascular smooth muscle cell (VSMC) proliferation have been well documented 36, 37, 38. However, recent work has demonstrated that several key effects of cAMP i
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