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br Allosteric inhibitors In general candidate drugs that bin
2019-10-24
Allosteric inhibitors In general, candidate drugs that bind to a GPCR at a site that is distinct (allosteric site) from the binding site of the endogenous agonist (orthosteric site) are attracting increasing attention 39, 42, 58. Allosteric modulators display saturability of their effect, probe d
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Impulsive burying and freezing behaviors in response to aver
2019-10-24
Impulsive burying and freezing behaviors in response to aversive stimuli may represent attempts to avoid novel and/or aversive stimuli. These behaviors can be assessed utilizing the marble burying and conditioned fear tasks, respectively. For example, Wistar rats in proestrus and ovariectomized rats
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br Materials and methods br Acknowledgments br Introduction
2019-10-23
Materials and methods Acknowledgments Introduction Proton pumps convert the energy of high-energy compounds into the GPCR Compound Library of protons across biomembranes. They play two physiological roles: pH regulation and the formation of proton-motive forces in their membranes. The simp
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Finally the identification of predictive biomarkers of respo
2019-10-23
Finally, the identification of predictive biomarkers of response will also allow the more recently discovered CDK inhibitors to be explored in particular genetically-defined contexts, for example by building on recent observations that KRAS mutant tumors are highly sensitive to CDK1 inhibition, and
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RNA seq results also support the similarity
2019-10-23
RNA-seq results also support the similarity between ESC- and YS-derived B-1 progenitors. Bmi1 expression, known as an important gene for self-renewal ability in stem cells, was reduced in ESC-derived B cells compared with YS-derived B cells, and Bmi1 overexpression improved the engraftment of ESC-de
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gbr properties Little information is available regarding the
2019-10-23
Little information is available regarding the expression of the different EP receptor subtypes on human monocytic cells, particularly those that are involved in downregulating cytokine production. The receptors are controlled by the respective genes for each receptor i.e. PTGER1–PTGER4 for EP1–EP4 r
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The discoidin domain receptors DDR and DDR are receptor tyro
2019-10-23
The discoidin domain receptors, DDR1 and DDR2, are receptor tyrosine kinases (RTKs) that are stimulated by collagen in the extracellular matrix (ECM). Unlike most other RTKs, they form ligand-independent stable dimers that are non-covalently linked. This ECM activation induces receptor phosphorylati
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The DNA damage response DDR is
2019-10-23
The DNA damage response (DDR) is a cellular mechanism that protects against DNA damage induced by endogenous and exogenous factors, it includes changes in cellular processes such as AZ191 australia regulation, DNA damage repair, apoptosis and chromatin remodeling. In recent years, the DDR has been r
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Furan analogs and N methylpyrrole analogs had completely dif
2019-10-22
Furan analogs and N-methylpyrrole analogs had completely different SARs. For example, replacement of the furan-2-sulfonyl moiety of 6 with the furan-3-sulfonyl moiety resulted in 8 with a decreased EP1 h89 affinity and an increased antagonist activity, while the corresponding chemical modification
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Whichever interactions are formed between the DS
2019-10-22
Whichever interactions are formed between the DS domains and the collagen ligand, they are expected to lead to structural changes within the DDR dimer that are propagated across the cell membrane to result in DDR autophosphorylation (Noordeen et al., 2006). Tight coupling of the extracellular confor
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It is particularly notable that CYP D appears
2019-10-22
It is particularly notable that CYP2D6 appears to be the most stable of the major CYP450 pfk australia in its expression over time in vitro and appears to be least affected by culture conditions and sample to sample variability (i.e., CYP2D6 expression is remarkably consistent over time and between
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br GPCRs form heterotetramers In addition to
2019-10-22
GPCRs form heterotetramers In addition to homodimers and heterodimers, for several family A receptor heteromers, experimental evidence supports the presence of higher order rearrangements as tetrameric structures, comprised of two different homodimers, each able to signal with its preferred G pro
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With the recent expanse of
2019-10-22
With the recent expanse of technology to evaluate synthetic lethality, new combinations with DHODH inhibitors may be uncovered (O\'Neil, Bailey, & Hieter, 2017). Many oncogenic backgrounds share synthetic lethality with DHODH. Cells with mutant PTEN have increased glutamine metabolism and are sensit
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Interferon IFN induces formation of
2019-10-22
Interferon (IFN)-γ induces formation of a heterotetrameric, IFN-gamma-activated inhibitor of translation (GAIT) complex in human monocytic SR 2595 (Mazumder et al., 2003a, Sampath et al., 2004). The complex binds a bipartite stem-loop element in the 3′UTR of vascular endothelial growth factor (VEGF
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An important strength of our
2019-10-22
An important strength of our study is the use of an elastic net regression model to select the variable and construct the model, which performed ideally in terms of both predictive accuracy and sparsity for the high-dimensional datasets [16]. As a result, the apparent predictive effect of multiple c
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