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In conclusion we have designed and synthesized
2023-11-28
In conclusion, we have designed and synthesized a series of 4-phenyl-thiazole analogues as potent ATX inhibitors. Total twenty-five compounds were synthesized and evaluated for their inhibitory activity on ATX using FS-3 and human plasma assays. Compound was found to be the most potent derivative p
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However there are studies revealing the dark side of
2023-11-28
However, there are studies revealing the “dark side” of autophagy at later stages in cancers, when oncogenes (mainly K-ras and B-raf) are activated and/or tumour suppressors such as PTEN and p53 are inactivated. These studies are based on the use of GEMM and deletions of essential autophagy genes (A
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Growth inhibition assays are the
2023-11-27
Growth-inhibition assays are the most commonly used to identify antifungal small molecules. However, they have several facts that limit their use since many pathogenic fungi grow as filaments making difficult a correlation between growth and OD (optical density). They are not useful for identifying
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br Identification of the croaker mAR cDNA Testosterone
2023-11-27
Identification of the croaker mAR cDNA Testosterone (T) was observed to alter steroidogenesis through a nongenomic mechanism (not blocked by the transcription inhibitor, actinomycin D) in Atlantic croaker ovarian tissues (Braun and Thomas, 2003). This action of T was mimicked by T conjugated to B
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br Perspective AA LA and other PUFAs and
2023-11-27
Perspective AA, LA and other PUFAs and their lipid metabolites play an important role in human diseases. 12/15-LOX which is the metabolic enzyme of them plays an important role in the pathogenesis-related diseases such as atherosclerosis, diabetic nephropathy, neurological diseases and other path
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There are two ways to transport FFAs
2023-11-27
There are two ways to transport FFAs into cells. First by passive diffusion. Second as the putative long-chain fatty anderson kpt transporters are proposed, CD36 the plasma membrane-associated fatty acid-binding protein (FABPpm) and fatty acid transport proteins (FATP) [11], where CD36 is responsib
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In a recent series of studies from our
2023-11-27
In a recent series of studies from our laboratory, to characterize the contractile systems within the rat apoptosis inducer wall, three conditions were identified that led to detrusor activity: spontaneous micro-contractions, electrical field stimulated (EFS) contractions and muscarinic agonist ind
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br Materials and methods br Results
2023-11-27
Materials and methods Results The average body weights for each group of mice over the course of the study are shown in Fig. 2A. The average body weights of the mice in the saline control group and PACAP group increased slightly during the study. In contrast, starting at day 17, the body weigh
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In the late s Solvay Pharmaceuticals discontinued the Phase
2023-11-27
In the late ‘90s, Solvay Pharmaceuticals discontinued the Phase 2 development of a promising potent and highly selective A1AR antagonist based on the pyrrolopyrimidine scaffold, SLV320 [43] (2, Chart 1, also named derenofylline; Ki hA1AR = 1 nM), for the treatment of acute heart failure [24]. In the
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The purpose of this study is to
2023-11-27
The purpose of this Bezafibrate synthesis study is to examine the relationship between ACEs and engagement in treatment among a sample of youth in residential treatment centers (RTCs). It is hypothesized that youth with higher ACE scores will have lower levels of engagement in treatment. In order to
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Inhibitors of mPGES are considered as safe
2023-11-27
Inhibitors of mPGES-1 are considered as safe alternative to NSAIDs in the treatment of chronic inflammatory diseases that are characterized by excessive PGE2 production (Bahia et al., 2014; Khurana and Jachak, 2016; Koeberle et al., 2016; Korotkova and Jakobsson, 2014; Norberg et al., 2013; Psarra e
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In order to improve the methodology of the
2023-11-27
In order to improve the methodology of the synthesis of steroidal derivatives, our goal was the investigation of aza-Michael addition of different N-nucleophiles to 16-dehydropregnenolone in the presence of [DBU][OAc] as catalyst and reaction medium. Michael addition of electron deficient steroidal
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PF also a dual Aurora A
2023-11-27
PF-03814735, also a dual Aurora-A and Aurora-B inhibitor, was administered in a phase I dose escalation study in a 3-weekly Tenatoprazole sale for 5 or 10 consecutive days [69], [70]. To date 25 patients have been included in 7 dose levels (5–100mg/day for 5 days). Using the 5-day schedule the MTD
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The co crystal structure of blebbistatin bound to myosin II
2023-11-24
The co-crystal structure of ()-blebbistatin ()- bound to myosin II (PDB: ) was used to scout for possible favorable interactions with the residues lining the binding pocket. Looking at A, we hypothesized that -oriented hydrophilic moieties (e.g. hydroxymethyl) on C of the blebbistatin scaffold migh
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br ASK in Huntington s disease and other
2023-11-24
ASK1 in Huntington's disease and other polyglutamine diseases The polyglutamine (polyQ) diseases are a group of inherited neurodegenerative disorders caused by the expansion of cytosine-adenine-guanine (CAG) trinucleotide repeats in the coding regions of specific genes, leading to the production
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