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V5 peptide Compound containing dimethylglutarimide P cap P p
2022-06-15
Compound containing, dimethylglutarimide P-cap, P propyl group, α-methylbenzyl urea resulted in inhibitor with much improved binding (=0.064μM) and EC=0.3μM. This was an aza-peptide analog with an EC comparable to our first generation clinical candidate . Analog was evaluated for its selectivity
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Famprofazone Unfortunately the approved drugs suffer from
2022-06-15
Unfortunately, the approved drugs suffer from failure in many cases [5,6]. Several mutations occur in the binding site of NS3/4A protease, which affect drug binding and cause drug resistance [13]. It is a big challenge and needs more efforts to be done. This is the reason why research is still conce
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In first wave first generation drugs telaprevir and
2022-06-15
In 2013, first-wave, first-generation drugs telaprevir and boceprevir was the first protease inhibitors (PIs) incorporated in Brazilian Clinical Guidelines for the treatment of patients infected with HCV g 15 sale 1. Based on this 2013 Clinical Guideline, telaprevir could be used for both naïve and
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The experiments reported herein were designed to test
2022-06-15
The experiments reported herein were designed to test whether co-expression of MRP and GSTP1-1 offers a level of protection from certain cytotoxic drugs not achieved by the expression of either protein alone. This was accomplished by stable transfection with expression vectors into MCF7/WT cells, w
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GSK is a critical component of
2022-06-15
GSK-3 is a critical component of the Wnt signaling pathway. The Wnt/beta-catenin signal transduction pathway is important in normal growth and development and is also frequently dysregulated in cancer and other diseases. The Wnt/beta-catenin pathway is finely tuned by both positive and negative inte
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K-7174 br Introduction br Mitochondrial dysfunction and canc
2022-06-14
Introduction Mitochondrial dysfunction and cancer Lactate and succinate as oncometabolites Intracellular actions of lactate and succinate as tumor promoters Cell-surface receptors for lactate and succinate and their role in cancer GPR109A as the receptor for butyrate and β-hydroxybu
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In the present study we conducted
2022-06-14
In the present study, we conducted a search for other possible endogenous ligands for GPR35. We focused on lysophospholipids because of the homology (30%) between GPR35 and GPR55 whose endogenous ligand is lysophosphatidylinositol (LPI) [9], especially 2-arachidonoyl LPI [10]. Notably, the GPR35 gen
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br Acknowledgements br Introduction Aminoacyl
2022-06-14
Acknowledgements Introduction Aminoacyl-tRNA synthetases catalyze the formation of an ester bond between an amino nrf2 inhibitor and the 3′ end of a tRNA in a two-step reaction. First, the amino acid is activated and an enzyme-bound adenylate intermediate is formed. Then, the amino acid is tr
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The vast majority of clinical studies have shown that chroni
2022-06-14
The vast majority of clinical studies have shown that chronic administration of GLP-1R agonists frequently lowers SBP/DBP in diabetic humans, which is consistent with preclinical studies, though the reported reductions are not as potent as those observed in their animal counterparts. In contrast, ac
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In order to test the
2022-06-14
In order to test the influence of the initial depolarization, experiments were performed, where the degree of chloride substitution was varied, either by adding n-Ringer to vascular disrupting agent incubated in a sucrose Ringer or by suspending the cells directly in Ringers identical to the final
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BTZ043 Racemate We show here that FXR is a
2022-06-14
We show here that FXR is a point of convergence of heredity (H) and environmental (E) risk factors for CRC (re the Tomasetti and Vogelstein model). Our studies demonstrate that the APC mutation and high-fat diet independently and cooperatively increase the BA pool that results in the repression of F
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The ultimate success of multimodal
2022-06-14
The ultimate success of multimodal probe in the inflammation imaging will be dependent on simplicity in synthesis (combining various modules without protection/deprotection), ease of optimization of pharmacological properties (linker group with tunable PEG moiety), co-registration of macroscopic and
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On the other hand histone deacetylase
2022-06-14
On the other hand, histone deacetylase inhibitors can accelerate inflammation resolution by promoting the externalization of AnxA1, a main ALX/FPR2 agonist, with concomitant inhibition of cytokine gene expression in mouse macrophages [30]. Thus, our present results provide an additional mechanism, i
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br Other strategies for ferroptosis In addition to ROS gener
2022-06-14
Other strategies for ferroptosis In addition to ROS-generating and GPX4 inactivating nanomaterials, small molecules and genetic manipulation targeting key factors in the ferroptosis pathway have also been tested for their anticancer effects [39,47,48]. Among a myriad of proteins involved in ferro
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Electrochemical techniques have attracted broad
2022-06-13
Electrochemical techniques have attracted broad attention for their outstanding advantages, such as satisfactory sensitivity and convenient operation. Nowadays, nucleic EZLink Sulfo-NHS-LC-Biotin Kit nanostructures such as DNA tetrahedron structure, nucleic acid-mimicking structure, exhibit noticea
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