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In various models histamine has been shown
2022-03-30
In various models, histamine has been shown to induce chemotaxis. This was first appreciated over 40 years’ ago in studies with eosinophils (Clark et al., 1977). At that time, only histamine H1 and histamine H2 receptors were recognized and studies with ligands to these receptors indicated that neit
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Neurotensin br HO and cerebral malaria In a post mortem eval
2022-03-30
HO-1 and cerebral malaria In a post-mortem evaluation of human cerebral (falciparum) malaria, strong HO-1 immunostaining was consistently noted in microglia/macrophages within and surrounding the pathognomonic Durck’s granulomas (Schluesener et al., 2001). As witnessed in cerebral trauma specimen
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HDAC enzymes oppose the effects of HATs by reversing lysine
2022-03-30
HDAC enzymes oppose the effects of HATs by reversing lysine acetylation, an action that restores the positive charge of the lysine thus stabilizing the local chromatin structure. By removing acetyl groups from ε-amino lysines of proteins, HDACs not only alter transcription, but also promote either t
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P Benzoxaborole substituted macrocyclic compounds based on I
2022-03-30
P4-Benzoxaborole-substituted macrocyclic compounds based on ITMN-191 scaffold were prepared using a general scheme as shown in . ITMN-191 was prepared by following a patent procedure. The P4 BOC group was removed by treatment with TFA in dichloromethane to give amine . The coupling of the amine to 6
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br Amino acid usage in cancer br
2022-03-29
Amino 5-Methyl-CTP usage in cancer Perspective High glucose consumption is a common feature of several types of tumor cells. Therefore, so far, in vivo positron emission tomography (PET) imaging with the glucose analog 18F-fluorodeoxyglucose (18F-FDG) has been used to detect various tumors. H
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The discovery that the physiological
2022-03-29
The discovery that the physiological functions of LPI are associated with the activation of specific GPR55 membrane receptor [4] has launched a new era of research on this lysophospholipid. However, the activation of membrane receptors by lysophospholipids is extremely complex due to the multitude o
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The spatial effects of Ebi
2022-03-29
The spatial effects of Ebi2 involve the creation of a moderate bias in CD4+ T cell distribution toward the LN periphery. Is this modest effect meaningful in an evolutionary sense? In this regard, we think the following considerations are relevant. First, asymmetric CD4+ T cell positioning is highly
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br Introduction The amino acid glycine functions as a
2022-03-29
Introduction The amino Suramin hexasodium salt glycine functions as a neurotransmitter in the vertebrate central nervous system: as an inhibitory neurotransmitter and as a co-agonist of the NMDA-subtype of excitatory glutamatergic receptors (Eulenburg et al., 2005). Under a current hypothesis th
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The calculations for the R substrate
2022-03-29
The calculations for the R substrate showed that, like the S substrate, the coordination shell of the Zn neuronal nitric oxide synthase is more symmetric than in the HIC-SG crystal structure. This symmetry indicates that the enzyme could use the same reaction mechanisms as for the S substrate, but w
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br Introduction Verticillium dahliae Kleb is a soil borne
2022-03-29
Introduction Verticillium dahliae (Kleb.) is a soil-borne fungal pathogen that is able to infect hundreds of plant species, and causes vascular wilt disease [1], [2]. In nature, the infection of V. dahliae initiates from the germination of resting structures called microsclerotia [3]. The germina
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Petrat et al could show that even
2022-03-29
Petrat et al. could show, that even a low dosage of 10-mg/kg glycine (133 μmol/kg) has a beneficial effect on the small intestine after I/R. In regard to glycine, β-alanine has a clearly higher EC50 to the GlyR and activates the receptor with an efficiency of only 34.6%.16, 17 Therefore, it can be c
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GK allosteric activators validate the importance of GK from
2022-03-29
GK allosteric activators validate the importance of GK from a therapeutic perspective, but the nature of allosteric activation of GK remains unclear. The GK allosteric activator site, the pocket where GKAs bind, is ~20 Å remote from the active site (Fig. 1A). The allosteric site is the locus of many
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Moreover we examined inhibition of GLI mediated mRNA express
2022-03-29
Moreover, we examined inhibition of GLI-mediated mRNA expression by 1. Colubrinic GSK 4112 (1) inhibited the mRNA production of PTCH in PANC1 cells in the dose-dependent manner. This result clearly shows 1 inhibits GLI-mediated transcription (Fig. 6). Discussion In this study, we identified thre
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In Solloway and colleagues reported that mice with
2022-03-29
In 2015, Solloway and colleagues reported that mice with alpha cell hyperplasia due to inactive hepatic glucagon receptor signaling may most likely be caused by amino keap1 nrf2 dependent mechanisms [11]. The authors then showed these adaptations are regulated by ‘mechanistic target of rapamycin’ (
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Although the ramifications of non additive SAR are context d
2022-03-29
Although the ramifications of non-additive SAR are context-dependent, the knowledge that perturbations in one region of a chemical series are not synergistic with perturbations in another region of the same chemical series is clearly pertinent to any medicinal chemistry effort. In our experience, no
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