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In addition to EGFR other receptor tyrosine kinases RTKs
2020-02-04
In addition to EGFR, other receptor tyrosine kinases (RTKs) also play roles in the tumor progression under hypoxia, especially hepatocyte growth factor receptor (cMet) (Le et al., 2012). Our data suggested that unlike EGFR, hypoxia had no apparent effect on cMet aminolevulinic acid (data not shown),
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We also found downregulation of TRIM
2020-02-04
We also found downregulation of TRIM32 in the hearts of dilated and hypertrophic cardiomyopathy patients in addition to TAC and phenylephrine treated mice [51]. TRIM32 and Dysbindin are known to interact in skeletal muscle, and we could confirm this interaction in cardiomyocytes as well. In cardiomy
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br Results br Discussion The ubiquitin system has
2020-02-04
Results Discussion The ubiquitin system has in recent years become an exciting area for drug discovery (Cohen and Tcherpakov, 2010), as multiple enzymatic steps within the ubiquitylation process are druggable. The potential of targeting the ubiquitin-proteasome pathway was first demonstrated i
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eletriptan Acknowledgments br Introduction Diabetes mellitus
2020-02-04
Acknowledgments Introduction Diabetes mellitus (DM) is a multifactorial disease [1] associated with serious comorbidities. This condition has recently reached epidemic proportions, as its occurrence has exponentially increased in the general population. Over 400 million people worldwide were est
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Introduction Nucleic acids are polyanionic and their negativ
2020-02-04
Introduction Nucleic acids are polyanionic and their negatively charged nucleotides allow the binding of cationic dyes, such as acridine orange (3,6-dimethylaminoacridine). Acridine orange (AO) was first synthesized in 1889, but its ability to bind nucleic acids was only reported in 1940, with grea
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Introduction Fish commonly employ pheromones to regulate a v
2020-02-03
Introduction Fish commonly employ pheromones to regulate a variety of functions including reproductive communication [1]. Reproductive pheromones induce both primer effects, such as changes in the endocrine or physiological state of conspecifics, and releaser effects such as rapid behavioral respon
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Using the juxtarenal PPE the induction of juxta
2020-02-03
Using the juxtarenal PPE, the induction of juxta- and suprarenal aneurysms is described herein (Fig. 3A). The infra-/suprarenal part of the 1,3-PBIT dihydrobromide receptor can now be investigated separately, taking into account different embryological backgrounds and varying reactivity to differin
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carboxypeptidase dihydroxycholesterol OHC was recently ident
2020-02-03
7α,25-dihydroxycholesterol (7α,25-OHC) was recently identified by classic analytical methods as a high-affinity ligand for EBI2 (Hannedouche et al., 2011; Liu et al., 2011). 7α,25-OHC was previously identified as an intermediate in the alternate pathway of hepatic bile carboxypeptidase synthesis (R
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br Results and discussion br Conclusion We
2020-02-03
Results and discussion Conclusion We have constructed a series of potent and greatly selective DPP-4 inhibitors with pyrazolo[1,5-a]pyrimidin-7(4H)-one core surrogates. The modification of the core led us to b2 which has IC50 of 80 nM and > 1000 fold selectivity over DPP-8 and DPP-9. We utiliz
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na inhibitor br Experimental section br Notes br PDB ID code
2020-02-03
Experimental section Notes PDB ID codes The atomic coordinates and structure factors of hDHODH in complex with compounds 4 (PDB id: 5MVC), 5 (PDB id: 5MVD) and 6 (PDB id: 5MUT) have been deposited in the RCSB Protein Data Bank. Acknowledgements This research was financially supported by
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Wu et al explored the anti inflammatory mechanisms by which
2020-02-03
Wu et al. explored the anti-inflammatory mechanisms by which osthole 35 acted on HepG2 cells cultured in a differentiated medium from cultured 3T3-L1 preadipocyte cells. HepG2 cells, a human liver cell line, were treated with various concentrations of osthole 35 in differentiated media from cultured
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To simulate the inhibition of the enzyme by organophosphorus
2020-02-03
To simulate the inhibition of the enzyme by organophosphorus, carbamate insecticides or nerve agents, a reversible cholinesterase inhibitor physostigmine was used for most experiments for safety reasons. However, the results of the measurements were verified using the soman organophosphate, which is
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Covalent inhibitors are well suited for targeting the
2020-02-03
Covalent inhibitors are well suited for targeting the E1 diltiazem hydrochloride receptor of Ubl modifications. Because the E1 enzymes in Ubl modifications, such as the SUMO E1 and Atg7, have a slow turnover rate (Boggio et al., 2004), prolonged inhibition can be achieved without requiring compounds
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Support for Cloninger s personality theory comes also from m
2020-02-03
Support for Cloninger\'s personality theory comes also from molecular genetic studies. Given the high heritability of personality it is plausible that gene variants explain variance in RD. In Gefitinib to endocrine studies, which relate hormone levels mostly in the periphery (blood, saliva, urine) t
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Mitochondrial depolarization induced by DHODH inhibition Fig
2020-02-03
Mitochondrial depolarization induced by DHODH inhibition (Figure 5A) may also contribute to the selective effects of DHODH inhibitors on KRAS mutant cells. If so, the effect may arise more from pro-apoptotic effects of mitochondrial depolarization (Lemasters et al., 1998) than from impaired oxidativ
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