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A range of inhibitors were therefore
2020-01-13

A range of inhibitors were therefore synthesized containing either carboxylic PX-478 2HCl or ester functionality at the ‘tail’ group as well as variations in the ‘head.’ These were assayed in vitro using the DCIP assay for binding affinity against and human DHODH at 50μM, respectively (). Analysi
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Milnacipran HCl We further correlated OPRK and OPRM
2020-01-13

We further correlated OPRK1 and OPRM1 methylation levels with individual characteristics in Xinjiang Han and Uygur controls. Partial correlation analyses showed that OPRK1 methylation was positively correlated with age in Uygur male controls (r=0.72, p=0.001, adjusted by body mass index (BMI), gluco
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The EGFR belongs to the ErbB family of receptor tyrosine
2020-01-13

The EGFR belongs to the ErbB family of receptor tyrosine kinases (RTKs), comprised of four members: EGFR (ErbB1, HER1), HER2 (ErbB2), HER3 (ErbB3) and HER4 (ErbB4) [24]. HER receptors are activated by a group of epidermal growth factor (EGF) ligands and undergo homo- or hetero-dimerization during th
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The expression of EBI has been found
2020-01-13

The expression of EBI2 has been found to be dysregulated in several types of B cell malignancies and is thus reduced in e.g. diffuse large B-cell lymphomas [12] and chronic lymphocytic leukemia [13] and increased in post-transplantation lymphoproliferative disorders (PTLDs) [14]. EBI2 is also highly
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br Effect of DPP Inhibitors on the
2020-01-13

Effect of DPP-4 Inhibitors on the Clinical Course of Heart Failure Four large-scale cardiovascular outcomes trials with DPP-4 inhibitors have been completed, and their findings have been published (Table 1) 31, 32, 33, 34. In 2 studies (with saxagliptin and alogliptin), DPP-4 inhibition was accom
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Boulares group has demonstrated that the NF
2020-01-13

Boulares group [82] has demonstrated that the NF-κB1/p50 NF-κB, a family member of type I NF-κB, is an excellent substrate for DNA-PK, which-dependent phosphorylation of NF-κB1 at serine 20 appears to enhance its binding to DNA as either a homodimer or a heterodimer with p65 NF-κB and the ability of
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Evodiamine The other scenario pertaining to the significance
2020-01-13

The other scenario pertaining to the significance of H2AX phosphorylation is based on the fact that the initiation of DNA fragmentation by CAD facilitates the chromatin condensation that occurs concurrently [15]. Apoptotic DNA fragmentation and chromatin condensation are important for the efficient
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With the recent expanse of technology to evaluate synthetic
2020-01-13

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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Ranolazine The homologous DDRs are composed of an N
2020-01-13

The homologous DDRs are composed of an N-terminal discoidin homology domain, followed by a sequence of ∼220 amino acids unique to the DDRs, a transmembrane domain, a large juxtamembrane domain, and a conserved cytoplasmic tyrosine kinase domain. In a previous study, we demonstrated that DDR activati
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The first transcription factor TF
2020-01-13

The first transcription factor (TF) known to interact with one of the cis-acting GAREs is GAMYB protein, the expression of which is induced by GA in the aleurone ITE receptor of barley (HvGAMYB) (Gubler and Jacobsen, 1992). GAMYB is an important regulator of endosperm functions during seed developme
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As previously stated the most unexpected finding from
2020-01-13

As previously stated, the most unexpected finding from this series of compounds was the identification of a dimethyl isoxazole side chain that gave dramatically improved binding over the parent compounds. Holding this piece of the molecule constant, a series of analogs were made to further understan
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br Materials and methods br
2020-01-13

Materials and methods Results Discussion In the past decade, GWAS have attempted to identify genetic variants that confer risk for many human diseases, whose inherited components remain unexplained (Manolio et al., 2009). In a few cases risk variants identified by GWAS have paved the way fo
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Introduction Determining how genes function together
2020-01-11

Introduction Determining how genes function together as biological systems is a defining challenge of the genomic era. While genome sequences reveal the DNA blueprint of organisms, deciphering how this blueprint leads to biological function is challenging due in large part to the complexity of prot
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br DDR mediated signaling DDRs initiate signaling
2020-01-11

DDR-mediated signaling DDRs initiate signaling pathways in a context and cell type-dependent manner. For instance, DDR1 was reported to activate ERK in vascular smooth muscle Xylazine HCl (Lu et al., 2011), to inhibit ERK in mesangial cells (Curat and Vogel, 2002), and to have no effect on ERK a
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br Allosteric inhibitors In general candidate drugs
2020-01-11

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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