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The Lysine mutant is located in the tail region of
2021-05-25

The Lysine429 mutant is located in the tail region of 5-HT2A, which is predicted to be unstructured. This region has been shown to interact, in vitro, with PSD95 and leads to differences in signaling (Xia et al., 2003). The ASK motif, a component of the tail region, is also important for regulation
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In this report we evaluate if this
2021-05-25

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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We also discovered important clues to domain binding sites
2021-05-25

We also discovered important clues to domain mm hcl of DGKs and how to exploit these regions for development of DGKα-selective inhibitors. The identification of a probe-modified site at the C1 domain provided the first evidence of a ligand binding site remote from the ATP binding region of DGKs. Al
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Apart from its high affinity the
2021-05-25

Apart from its high affinity, the selection of GW2580 as antifungal lead in our radiotracer development program was motivated by its exceptional selectivity. The observed profound impact of small structural modifications on the selected panel of four kinases tested prompted us to conduct comprehensi
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Introduction The carnitine choline acyltransferase
2021-05-25

Introduction The carnitine/choline acyltransferase family is a family of enzymes that play diverse roles, ranging from (the regulation of) acpt and fuel metabolism in mitochondria and peroxisomes to the generation of the neurotransmitter acetylcholine. In mammals, this family consists of seven tra
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Yang et al investigatedPsoralidin a coumestan derivative iso
2021-05-25

Yang et al. investigatedPsoralidin 39, a coumestan derivative isolated from the seed of Psoralea corylifolia, regarding its effects on IR-induced pulmonary inflammation. Psoralidin 39 inhibited the IR-induced COX- 2 expression and PGE(2) production through regulation of PI3K/Akt and NF-κB pathway. A
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br Acknowledgements br Introduction Endothelial cells consti
2021-05-24

Acknowledgements Introduction Endothelial nibr receptor constitute a unique source of humoral factors that may regulate the functions of other cell types via paracrine or endocrine pathways [1]. Among the many molecules originated from the endothelium, nitric oxide (NO) plays versatile roles i
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What would be the possible off target effects of enhancing
2021-05-24

What would be the possible off-target effects of enhancing Ndfip1 to control T cell responses? Increasing Ndfip1 activity could limit cytokine production in macrophages, where it has been shown to function in mouse BMDMs to degrade Tak1 and downregulate NFκB signaling [108]. Whether Ndfip1 regulates
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Since the interaction between the E and E
2021-05-24

Since the interaction between the E2 and E3 is weak and transient, it has been difficult to identify novel interactions between specific E2/E3 complexes [59], [64]. Here we used a modified bait consisting of the Mulan RING domain fused to one of the four E2s isolated in our screen and expressed in y
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Recent pharmaceutical research in the
2021-05-24

Recent pharmaceutical research in the field of respiratory diseases has sought to make available new agents that specifically and selectively antagonize the actions of cysteinyl–leukotrienes. Such an effort has resulted in the development of two classes of drugs, effective in counteracting Cys-LTs p
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Hymenialdisine the most potent inhibitor of parasite
2021-05-24

Hymenialdisine, the most potent inhibitor of parasite TgCK1 enzymes in vitro has no whole cell anti-parasitic activity (Table 2). Like purvalanol B however, this GLPG0634 also displays poor activity against target enzymes in cultured cells. For example, in vitro IC50 values for inhibition of CDK5/c
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Besides having a remarkable progestogenic effect an addition
2021-05-22

Besides having a remarkable progestogenic effect, an additional characteristic of DRSP is its strong antimineralocorticoid effect and antiandrogenic action [11]. DRSP is characterized by an antimineralocorticoid effect that is stronger when compared to progesterone. The decreasing synthesis of proge
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In the present study we investigated the role
2021-05-22

In the present study, we investigated the role of EP1R after ICH and its mechanism of action. We hypothesized that EP1R activation aggravates ICH injury but that its blockade reduces injury through the Src kinases and the MMP-9 signaling pathway. To test this hypothesis, we examined the effects of s
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A comparative analysis of the cleavage activity of different
2021-05-22

A comparative analysis of the cleavage activity of different forms of the BoNT/A endopeptidase in reduced conditions with SNAPtide and full-length SNAP-25 substrate is summarized in Fig. 5, Fig. 6. The BoNT/A LC was found to be the most active against SNAPtide, a small peptide segment of the SNAP-25
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Nitric oxide NO is synthesized by
2021-05-22

Nitric oxide (NO) is synthesized by conversion of the l-arginine to NO and l-citrulline through reaction which is catalyzed by nitric oxide synthetase (NOS) (Knowles and Moncada, 1994). NO as an important molecule not only play a role as second messenger but also binds to cytochrome c oxidase and de
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