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The receptor binding assay used in our previous study demons
2022-05-11
The receptor binding assay used in our previous study demonstrated that propofol competitively binds to FPR1, thus blocking the downstream signal transduction of FPR1 and inhibiting neutrophil immune activities [8]. In this study, we assessed the pharmacological action of fMMYALF in the presence of
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FPR activation stimulates multiple signal transduction pathw
2022-05-11
FPR1 activation stimulates multiple signal transduction pathways responsible for various neutrophil functions, such as adhesion, chemotaxis, phagocytosis, Z-LEHD-FMK of secretory granules, and superoxide anion radical (O2) production, which contribute to the physiological inflammatory response asso
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In addition the interplay of membrane
2022-05-11
In addition the interplay of membrane curvature induced tension at the fusion pore and Thalidomide induced tension across the PM seems to be a worthwhile target for investigation. The roles of dynamin and myosin II and especially their spatial and temporal dynamics during activity warrant further r
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BMP signals play pivotal roles in
2022-05-10
BMP signals play pivotal roles in the various processes of chondrogenesis [12], [13]. At early stages of chondrogenesis, BMP signaling regulates the differentiation of mesenchymal Tamoxifen into chondrocytes via the induction of Sox9[29]. The loss of Noggin, a BMP antagonist, results in the overgro
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Multiple subsets of Breg cells in mice have been
2022-05-10
Multiple subsets of Breg cells in mice have been identified that could suppress the T cell-mediated response. However, a lack of consensus surface markers for Breg cells made it difficult to judge whether Breg cells are a special B cell subset or whether all flumethasone have an immuno-regulatory f
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The HCV NS A protease consists of two subunits NS
2022-05-10
The HCV NS3/4A protease consists of two subunits, NS3 and NS4A. NS3 comprises an N-terminal serine protease domain and a C-terminal RNA helicase domain [12]. NS4A acts as a cofactor, which ties the holoenzyme complex to an intracellular membrane compartment. The presence of the central region of NS4
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According to literature RASs V M T S Q K
2022-05-10
According to literature, RASs V36M, T54S, Q80K and R155K are considered primary resistance mutations to different PIs. RASs V36M and R155K can reduce susceptibility to recently approved PIs simeprevir, paritaprevir and grazoprevir [18], [31], [32]. T54S is associated to resistance for first-wave tel
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Whilst it has long been appreciated that Rho family GTPases
2022-05-10
Whilst it has long been appreciated that Rho-family GTPases are able to signal directly to focal adhesions, it is also becoming increasingly clear that they can achieve this indirectly, through their influence on the extracellular matrix to which the integrins bind. Cdc42 and RhoA have long been kno
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br Introduction The Ras superfamily of small GTPases
2022-05-10
Introduction The Ras superfamily of small GTPases is composed of more than 150 protein members involved in a wide variety of biological processes, such as proliferation, differentiation, cytoskeletal organization, and protein trafficking [1]. The Ras superfamily proteins act as molecular switches
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Based on these findings we set out to identify GPR
2022-05-10
Based on these findings, we set out to identify GPR109A agonists capable of biasing the receptor's signaling towards the functional anti-lipolytic and presumed therapeutic response, and away from the flushing side-effect pathways. Indeed, using recombinantly expressed GPR109A, two classes of compoun
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Several investigators including ourselves have
2022-05-10
Several investigators including ourselves have previously shown, that allogeneic HLA-DPB1 class II-alleles are powerful leukemia rejection factor xa inhibitor for CD4 T-cell therapy following allogeneic hematopoietic stem cell transplantation (Herr et al., 2017, Rutten et al., 2008, Stevanovic et a
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In summary we discovered azaindole substituted
2022-05-10
In summary, we discovered 7-azaindole substituted -hydroxypyridone as a potent zinc-binding GLO1 inhibitor (IC=11nM) through lead generation from HTS and structure-based inhibitor design. The X-ray cocrystal structure and the comparison of binding energies with the indole counterpart revealed that
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Herein we report the discovery of
2022-05-10
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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br Introduction Glucokinase GCK hexokinase IV
2022-05-09
Introduction Glucokinase (GCK, hexokinase IV) is a monomeric enzyme that catalyzes the ATP-dependent conversion of glucose to glucose 6-phosphate, the first and rate-limiting step of glycolysis in the liver and pancreas [1,2]. GCK was first discovered in the early 1960's, and shortly thereafter
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12-O-tetradecanoyl phorbol-13-acetate Introduction Parkinson
2022-05-09
Introduction Parkinson's Disease (PD) is a neurodegenerative disease affecting approximately 5–6 million individuals worldwide [1]. This number is expected to escalate to ∼10 million by the year 2030 as the world's population rapidly ages [2]. In the United States, more than 1 million individuals h
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