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In early a collaborative effort between the group
2022-05-19

In early 2017, a collaborative effort between the group that pioneered the above described evidence of platinum-induced PUFA chemotherapy resistance and a group that has contributed to much of the known molecular pharmacology of FFA4, revealed that the molecular target of 16:4(n-3), which affords ch
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br Materials and methods br Results br Discussion The
2022-05-19

Materials and methods Results Discussion The distribution of FFA1 and FFA4 expressed in normal tissues is distinguishable. FFA1 is expressed in the restricted organ, such as pancreatic beta glycogen synthase kinase 3 [18]. In contrast, FFA4 is highly expressed in the lung, gastrointestinal
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br Introduction br Results br
2022-05-19

Introduction Results Discussion Experimental Acknowledgment Introduction Endocannabinoids, N-arachidonoylethanolamine (AEA) and 2-arachidonoylglycerol (2-AG) have been found in most mammalian tissues and they stimulate cannabinoid CB1 and CB2 receptor activity thereby modulating se
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br Material and methods br Results br Discussion It is
2022-05-19

Material and methods Results Discussion It is challenging to discriminate between HIV monoinfection and HIV-1/2 dual infection in settings where both viruses co-exist, due to cross-reactivity in serological tests. Thus, the gold standard for detection of HIV-1/2 dual infection is through NA
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Multi targeting agents are of major interest in modern drug
2022-05-19

Multi-targeting agents are of major interest in modern drug design and discovery. Design of such compounds can be applied to H3R antagonists for the purpose of achieving optimum efficiency as performed for some preclinical candidates such as recently for contilisant (Bautista-Aguilera et al., 2017;
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In the previous study concerning HO mediated inhibtion
2022-05-19

In the previous study concerning HO-1-mediated inhibtion of HCV replication, the mechanism underlying IFN-α/β indcuction by HO-1 involved in HO-1-catalyzed heme metabolic product, biliverdin (Zhu et al., 2010; Lehmann et al., 2010). However, in the present study SnPP, an inhibitor of HO-1 enzymatic
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Among the isoforms of heme oxygenases HO
2022-05-19

Among the 3 isoforms of heme oxygenases (HO-1, HO-2, and HO-3), HO-1 expression is inducible, and it catalyzes the degradation of heme to biliverdin, carbon monoxide (CO) and free Fe. The Fe is then stored in ferritin, limiting its ability to participate as a catalyst through the Fenton reaction and
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G protein coupled receptor kinases GRKs
2022-05-18

G protein-coupled receptor kinases (GRKs) are another group of kinases whose limited substrate repertoire is associated with an extensive binding interface. GRKs phosphorylate activated G protein-coupled receptors (GPCRs) at multiple sites, promoting binding of arrestin proteins to mediate receptor
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Indeed GSTP mRNA appears to be already highly stable in
2022-05-18

Indeed GSTP1-1 mRNA appears to be already highly stable in K562 leukemia zingerone australia with a half-live of more then 40h which is even further increasing to 92h after hemin treatment and erythroid differentiation. Previous reports quantified GST mRNA half-lives which depend on the cellular mo
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We also examined possible involvement of the
2022-05-18

We also examined possible involvement of the NF-κB signaling pathway in GSK-3 inhibitor-induced suppression of PGE2 production, whereas GSK-3 inhibitors did not have a significant effect on IκB phosphorylation/degradation or NF-κB nuclear translocation. These results are consistent with a previous p
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Our synthetic approach to GPR antagonists was designed so th
2022-05-18

Our synthetic approach to GPR55 antagonists was designed so that many different structures could be accessed to rapidly explore initial SAR, along with validating or modifying our current model (). The synthesis begins with the coupling of a carboxylic human leukocyte elastase to 4-piperidone by fi
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Although it is currently unknown
2022-05-18

Although it is currently unknown why the longer splice variant found in the human has not been found in any other species, similar results have been reported for other receptors, including the PQ 401 receptor receptor splice variant ERbeta2 identified in human and primate, but not other species (Si
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br Conflict of interest br CRediT
2022-05-18

Conflict of interest CRediT authorship contribution statement Magdalena Olga Ciechanowska: Conceptualization, Data curation, Investigation, Methodology, Project administration, Writing - original draft. Magdalena Łapot: Formal analysis, Investigation, Methodology. Marek Kowalczyk: Writing - re
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Herein we report the discovery of AM AM
2022-05-18

Herein, we report the discovery of AM-3189 (). AM-3189 maintains the in vivo efficacy of AMG 837 while displaying a superior pharmacokinetic profile and minimal CNS exposure. As we reported previously, activity on the GPR40 receptor varies significantly with substitution at the β-carbon relative to
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The ion conduction pathway reported herein accounts for all
2022-05-18

The ion conduction pathway reported herein accounts for all known functional properties of EAAT/GltPh anion channels. Simulations reveal unitary current amplitudes and ion selectivities (Figures 3C and 3D) that resemble experimental results (Melzer et al., 2003, Wadiche and Kavanaugh, 1998). The cal
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