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Since both the Ub and
2020-03-02
Since both the Ub and ISG15 systems are crucial for the innate immune response, many prokaryotic and viral pathogens have evolved ways to hijack them in order to create a “window-of-opportunity” for efficient replication. Several viral and bacterial proteins have been found to directly target these
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A set of small molecule LigI inhibitors were
2020-03-02
A set of small molecule LigI inhibitors were identified through an in silico structure-based screen, using the atomic resolution structure of LigI complexed with nicked DNA [[18], [26]]. This screen yielded inhibitors that were selective for LigI (L82), inhibited both LigI and LigIII (L67) and inhib
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The authors gratefully acknowledge financial support
2020-03-02
The authors gratefully acknowledge financial support from the State of São Paulo Research Foundation (FAPESP, Fundação de Amparo à Pesquisa do Estado de São Paulo), grants 2013/07600-3 and 2013/25658-9, and the National Council for Scientific and Technological Development (CNPq, Conselho Nacional de
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Currently according to Mielke and
2020-03-02
Currently, according to Mielke and colleagues [103], drugs with US Food and Drug Administration (FDA) approval for Alzheimer therapy include the following: galantamine (Razadyn®, 4aS,6R,8aS-5,6,9,10,11,12- hexahydro- 3-methoxy- 11-methyl- 4aH [1], benzofuro[3a,3,2-ef] [2] benzazepin- 6-ol), rivastig
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Semantics play an important role in
2020-02-28
Semantics play an important role in software component-based development as they improve components identification, selection and integration through, among others, the use of ontologies (Kaur and Mishra, 2017). Analogously, they allow to improve discovery, composition and reuse in the context of We
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br The estrogen receptors History and discovery In Elwood
2020-02-28
The estrogen receptors: History and discovery In 1958, Elwood Jensen discovered the estrogen receptor, the first receptor ever encountered for any hormone, by showing that reproductive female tissues were able to uptake estrogen from the circulation by binding to proteins. He later demonstrated t
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fda approved vegf inhibitor EP is the major receptor to
2020-02-28
EP4 is the major receptor to mediate PGE2-induced inflammatory pain. EP4 is upregulated by fda approved vegf inhibitor in DRG neurons [16]. Intrathecal injection of the EP4 agonist produced pain responses [25]. Either systemic or local injection of EP4 antagonists relieves inflammatory pain [3], [1
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cancer The prospects of the use of this novel approach for
2020-02-28
The prospects of the use of this novel approach for the selective local thermo-activation of enzymes include biomedical and biotechnological applications. As NPs could be engineered to gain access to cancer through the endosomal compartment [47] or through non-endocytotic pathways [48], [49], [50] o
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Another enzyme class that has emerged
2020-02-28
Another enzyme class that has emerged as a potential alternative to P450s are the so-called ‘unspecific peroxygenases’ (UPOs). They also contain a heme but are extracellularly expressed fungal enzymes that are often more stable than P450 monooxygenases. Importantly, UPOs use H2O2 instead of O2 as th
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br Experimental Procedures br Author Contributions br Acknow
2020-02-28
Experimental Procedures Author Contributions Acknowledgments Introduction The intestinal mucosal barrier surface is constantly exposed to food antigens, beneficial microbes, pathogens, and a multitude of other environmental stimuli (Turner, 2009). Innate lymphoid akt inhibitors (ILCs) a
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Previous studies revealed the expression
2020-02-28
Previous studies revealed the expression of the CCR3 receptor in neurons and its neuroprotective function using mice lacking CCR3 expression (Wainwright et al., 2009). The regulation of CCR3 receptor expression in the microglia and astrocytes was shown in neurological disorders and has been demonstr
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br Materials and Methods br Results br
2020-02-28
Materials and Methods Results Discussion Even though T cell checkpoint inhibitors alone have achieved impressive clinical benefit in some cancers, their application as single agents has had limited efficacy (Hamid et al., 2013; Wolchok et al., 2013). The resistance to immunotherapy is in pa
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Compounds were screened for their activity against the hERG
2020-02-28
Compounds were screened for their activity against the hERG channel, with the 2,3-Cl compounds more active here than the 2,4-F compounds. The homopiperazine examples (, , , ) showed increased hERG activity relative to the corresponding piperazines. The cell data for the 6,7-dimethoxyquinoline compo
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An AmDH is engineered by mutating two conserved amino
2020-02-28
An AmDH is engineered by mutating two conserved amino RG2833 residues in the active site of an amino acid dehydrogenase (AADH). Starting from the leucine dehydrogenase (LeuDH) from Bacillus stearothermophilus, substituting a serine and leucine at the K68 and N261 positions, respectively, resulted i
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YO-01027 synthesis Our comparison of all ER iso forms
2020-02-28
Our comparison of all ERα (iso)forms with ERβ immunostaining suggests that overall ERβ expression is lower than that of ERα isoforms. This contrasts the so far reported data for ERs in the lung, but is not a paradox; in pathology routine, ER positivity is defined stricto senso by nuclear WT ERs. As
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