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Intriguingly one E residue may serve as a molecular gate
2019-12-14
Intriguingly, one E2 residue may serve as a molecular ‘gate’ to allow the C-terminus of ubiquitin to access the closed E2~Ub conformations favorable for ubiquitin transfer. This residue, Asp87 in UbcH5 family members, resides on one side of the opening that leads to the active site Cys (Fig. 4D). In
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br Restenosis after angioplasty remains a
2019-12-14
Restenosis after angioplasty remains a remarkable challenge, although drug-eluting stents have reduced the incidence of restenosis considerably . Vascular smooth muscle BMS 493 (VSMCs) play a pivotal role in the development of intimal thickening and restenosis. VSMCs proliferate and migrate from
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A An optimized BEI SEIscore based on the trends
2019-12-14
(A) An “optimized BEI-SEIscore” based on the trends, emerged from the statistical analysis of several optimization studies in pharmaceutical industry (Abad-Zapatero, 2007, Abad-Zapatero and Blasi, 2011). This type of optimized scores has been used in many previous studies. Ki=1nM at 300° K, compare
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Introduction Mycobacterium leprae the causative
2019-12-13
Introduction Mycobacterium leprae, the causative agent of leprosy, affects skin, peripheral nerves and upper respiratory tract [1]. Although leprosy has been eradicated from most of the countries, it still affects approximately a quarter of a million people from India [2]. Details of many bacteriol
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The role of ARA cyp metabolites
2019-12-13
The role of ARA-cyp450 metabolites in the liver is still unclear [44]. However, ARA-cyp450 genes metabolize other fatty acids such lauric and palmitic Rose Bengal receptor [45]. It was found that decreased cyp4a expression caused fatty livers through reduction of fatty acid metabolism [46]. In this
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Soon after the discovery of ET and the cloning of
2019-12-13
Soon after the discovery of ET1 and the cloning of its ETA and ETB receptors, low-molecular-weight compounds were identified that can prevent the binding and effects of radioactively labeled ET1 3, 5, 6, 8. Initially, these ERAs resulted from screening efforts (e.g. BQ123 39, 49 and bosentan [50]).
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In this report we evaluate if this molecular mechanism is
2019-12-13
In this report, we evaluate if this molecular mechanism is used universally by high-fidelity DNA polymerases during the replication of DNA lesions that are structurally distinct from abasic sites. This was approached by quantifying the kinetic parameters for the incorporation of modified and non-nat
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The following are the supplementary data related to
2019-12-13
The following are the supplementary data related to this article. Acknowledgments Introduction Drug-resistant epilepsy (DRE) occurs in approximate 30% of patients who suffer from epilepsy [1]. Temporal lobe epilepsy (TLE) is one of the most common partial seizures and the common cause of DRE
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DDX belongs to the DEAD
2019-12-13
DDX3 belongs to the DEAD-box family of proteins, ATP-dependent RNA helicases characterized by the presence of a highly conserved helicase core domain [13]. This catalytic core is composed of two RecA-like domains containing motifs involved in ATP binding/hydrolysis, RNA binding and helicase activit
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Recent studies show that the expression and
2019-12-13
Recent studies show that the expression and function of some ion channels such as voltage-gated potassium channels, sodium channels and calcium channels are closely related to the proliferation, migration, and invasion of tumor cells [40], [41], [42]. Firstly, the expression of ion channels is chang
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WAY-100635 The assembly and maturation of invadopodia can be
2019-12-13
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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Our present data show that neuroleptics can affect CYP A
2019-12-12
Our present data show that neuroleptics can affect CYP3A via a direct interaction with the enzyme and a significant indirect mechanism (enzyme regulation) produced in vivo. The obtained results revealed interactions of the neuroleptics (added in vitro to control liver microsomes, Model I) with rat C
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In vivo study showed that the CYP A activity
2019-12-12
In vivo study showed that the CYP3A activity was increased, when morroniside (10, 30 and 90 mg/kg, i.g.) was daily for seven consecutive days. Further, RT-PCR analysis showed that the induction of mRNA energy metabolism by morroniside (10, 30 and 90 mg/kg, i.g.) was 1.13-, 1.43- and 1.79-fold higher
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Deregulated Wnt signaling either due
2019-12-12
Deregulated Wnt signaling, either due to pathway mutations or otherwise aberrant pathway activity, is common in CLL [81], [82]. In addition to targets described above, alvocidib also inhibits glycogen synthase kinase 3 (GSK3)-β at higher nanomolar concentrations [37]. Despite intuition and experimen
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Epigenetic silencing of genes that determine tumor
2019-12-12
Epigenetic silencing of genes that determine tumor invasiveness, growth patterns of tumors, and tumor-cell apoptosis12, 29 may also affect the expression of drug-metabolizing enzymes, thereby providing an additional genetic mechanism in pharmacogenomics. Trisomy 8 that contains wild-type GGH could b
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