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Another interesting finding from the present study is that s
2020-06-03
Another interesting finding from the present study is that silencing of ERRγ suppressed the expression of HSD17B1 in extravillous trophoblasts. HSD17B1 is a key enzyme in regulating estrogen activity and has been shown to promote the proliferation and migration of estrogen-dependent breast cancer CG
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Further modifications on the position of compound led
2020-06-03
Further modifications on the 8-position of compound led to compound 4 (8-pCPT-2′--Me-cAMP, a.k.a. 007, ), which is a potent (half-maximal activation of EPAC1 at 2.2µM) and selective (about 100-fold EPAC/PKA selectivity) EPAC agonist. Since the discovery of compound , it has been widely used as a po
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br Introduction Abdominal aortic aneurysm AAA is a daily
2020-06-03
Introduction Abdominal aortic aneurysm (AAA) is a daily concern in vascular surgery, as successful treatment is exclusively achieved by open or endovascular repair. Its prevalence is 2–11% among male smokers, and rupture the major complication, is associated with unacceptably high morbidity and m
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br Introduction Epithelial mesenchymal transition EMT
2020-06-03
Introduction Epithelial-mesenchymal transition (EMT) is a biological process by which epithelial hiv protease inhibitors lose cell polarity and cell-cell adhesion, and gain mesenchymal features with an increase of migratory and invasive properties [1]. EMT is essential for mesoderm formation dur
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br Inhibiting APC C during
2020-06-03
Inhibiting APC/C during Interphase and prior to Anaphase Because ubiquitylation by APC/C triggers cell division, it is essential that APC/C is restrained until cells are prepared for its substrates to be degraded. In addition to regulation by phosphorylation, an additional layer of control comes
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In summary we hypothesize that targeting the A R
2020-06-03
In summary, we hypothesize that targeting the A1R–D1R heterotetramer with heteromer-selective drugs might improve safety and efficacy of the pharmacological therapy for RLS and other motor diseases, resulting in fewer side effects than classical drugs developed for targeting monomeric A1R or D1R.
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br Acknowledgment This work was supported by the Estonian
2020-06-03
Acknowledgment This work was supported by the Estonian Science Foundation (Grant ETF8862). Introduction In higher eukaryotes ionizing-radiation (IR) induced DNA double-strand breaks (DSB) are primarily repaired by the non-homologous end joining (NHEJ) pathway [1]. Ku, a heterodimeric protein
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DNA damage represents a persistent threat to genomic stabili
2020-06-03
DNA damage represents a persistent threat to genomic stability. A critical link exists between DNA mutation, chromosomal rearrangement and cancer development. In myeloid malignancies, various chromosomal translocations and/or mutations increased cellular reactive oxygen species (ROS), followed by DS
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br Oxidoreductase like MEM for prodrug activation br
2020-06-02
Oxidoreductase-like MEM for prodrug activation Future outlook Although MEM-mediated prodrug activation has been performed by different MEMs and prodrugs, and their effectiveness have been proved in vivo, only a few types of MEMs or prodrugs have been explored in prodrug activation until now [2
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EBI remains an orphan GPCR
2020-06-02
EBI2 remains an orphan GPCR and the identity and source of its ligand are yet to be described. Molecular studies of EBI2 have suggested that this receptor has constitutive activity, similar to that observed for many herpesvirus-encoded 7TM receptors (Benned-Jensen and Rosenkilde, 2008, Rosenkilde et
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We elucidated that the ten DGK isozymes have
2020-06-02
We elucidated that the ten DGK isozymes have different relative 1-MGK and 2-MGK activities vs DGK activity under the same conditions. However, because the octylglucoside-mixed micellar assay was developed for DGK, it is not known whether the DGKs exhibit maximum 1-MGK and 2-MGK activities in this as
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This hydrophobic biphenyl tail gave good binding affinity fo
2020-06-02
This hydrophobic biphenyl tail gave good binding affinity for human DHODH enzyme (IC arn 509 synthesis was found to be the main metabolite in human microsomes and it was 100-fold less active against hDHODH than the ester. In an attempt to identify the specific non-covalent binding interactions whi
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The all NTP pyrophosphatase and NUDIX families maintain
2020-06-02
The all-α NTP pyrophosphatase and NUDIX families maintain the deoxynucleotide triphosphate (dNTP) pool balance, limit the incorporation of harmful nucleotides, and represent a promising therapeutic approach to develop anticancer and immunosuppressive agents., , , , Among these housekeeping enzymes
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However not all inhibitory profiles by metals can be
2020-06-02
However, not all inhibitory profiles by metals can be a priori considered artifacts of the methodology used to quantify the activity of such enzymes. Metals can indeed interfere with cholinesterases, and the mechanisms are varied. The inhibitory effect of specific metals may derive from their abilit
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An interesting observation pertinent to the
2020-06-02
An interesting observation pertinent to the immunology of pregnancy comes from a study by Kruse et al., they found that recurrent miscarriage patients with higher serum progesterone levels had lower Th1/Th2 cytokine ratios suggesting that progesterone levels modulate cytokine production patterns. Pr
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