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br The Farnesoid X receptor FXR identification and ligands
2022-05-05

The Farnesoid X receptor (FXR): identification and ligands The Farnesoid X receptor (FXR) belongs to a family of proteins called Nuclear Receptors (NRs). NRs are a class of ligand-activated transcription factors, which transactivate networks of target genes, thereby mediating a wide range of phys
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During the course of our optimization of the
2022-05-05

During the course of our optimization of the diarylsulfonamide chemotype as FFA4 agonists, we identified xanthene as a potent and selective antagonist of FFA4 (). Xanthene was able to block the agonist induced intracellular Ca response elicited by both linoleic rad51 and compound in competition
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br Introduction Thrombosis is one of the leading causes
2022-05-05

Introduction Thrombosis is one of the leading causes of deaths in the cardiovascular diseases such as myocardial infarction (MI), unstable ARRY334543 mg and acute coronary syndrome (ACS) in developed countries [1], [2]. It is estimated that venous thromboembolism (VTE) afflicts about 1 million (
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hydrazide Structurally HMTs can be broadly categorized into
2022-05-05

Structurally, HMTs can be broadly categorized into three functional enzymatic families, the SET (Suppressor of variegation, Enhancer of zeste, Trithorax)-domain- containing methyltransferases, the non-SET DOT1-like (DOT1L) lysine methyltransferases, the PRDM family, containing a PR (PRDI-BF1-RIZ1 ho
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Work is presently underway to unveil
2022-05-04

Work is presently underway to unveil mechanisms whereby SAHA-dependent restoration of cardiomyocyte autophagic flux is protective. Another interesting question pertains to mechanisms whereby class I and class II HDAC inhibitors induce autophagy. It has been demonstrated that TSA reduces transverse a
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The replacement of the P butyl
2022-05-04

The replacement of the P-butyl urea cap with sulfonamide derived cap had a profound effect on binding. Compound obtained by the replacement of -butyl urea P cap of compound with sulfonamide demonstrated a =34nM, a fifteen folds improvement in potency. Similarly replacement of P-butyl cap in the P
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It is interesting that SEC significantly
2022-05-04

It is interesting that SEC significantly inhibited cell migration and EMT in PC3 cells expressing a low RKIP level and HEK293T RKIP−/− cells, while had no effect on HEK293T RKIP+/+ cells. These observations can be interpreted that the RKIP-ANXA7 association may block SEC-induced ANXA7 GTPase activat
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The diversity of biological properties and interactions of G
2022-05-04

The 5823 of biological properties and interactions of GSK-3 have been reviewed recently (, , , , ). The interactions of GSK-3 in the signaling pathways induced by nutraceuticals is covered in the review by ) in this special issue of . GSK-3 is a frequent target of many nutraceuticals such as curcum
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br Conclusions br Conflicts of Interest br Introduction
2022-05-04

Conclusions Conflicts of Interest Introduction Myalgic encephalomyelitis/chronic fatigue syndrome (ME/CFS) is a chronic multisystem illness of unconfirmed cause. ME/CFS has largely been diagnosed from Fukuda CFS criteria and/or the Canadian ME/CFS criteria. The Institute of Medicine in 2015
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The atherosclerosis development requires additional pro infl
2022-05-04

The atherosclerosis development requires additional pro-inflammatory response in the vascular tissue, promoting increased levels of adhesion molecules such as VCAM-1 (vascular cell adhesion molecule-1) and ICAM-1 (intercellular adhesion molecule-1). Cytokines such as TNF-α and IL-1β are able to upre
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Continuing studies of endocannabinoid ligands at GPR
2022-05-04

Continuing studies of endocannabinoid ligands at GPR55 reveal that virodhamine (O-arachidonylethanolamine) and AEA can act as a partial agonists at GPR55; at high micromolar concentrations can inhibit β-arrestin recruitment (Sharir et al., 2012). It is likely that there are allosteric as well as or
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Through a large scale phylogenetic
2022-05-04

Through a large-scale phylogenetic analysis of UDG superfamily in more than 1000 completely sequenced genomes, it is shown that family 3 DL-Dithiothreitol synthesis can be separated into two clades with the traditional family 3 SMUG1 as one of them (Fig. 1) [31]. UDG enzymes in another clade are pr
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The following are the supplementary data related to this
2022-05-04

The following are the supplementary data related to this article. Author contribution Conflict of interest Introduction Thrombosis (arterial and venous) is a major cause of vascular obstructive diseases including myocardial infarction, cerebral infarction and pulmonary embolism. Glycoprote
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Heterocysts provide the required microoxic environment for
2022-05-04

Heterocysts provide the required microoxic environment for the oxygen-sensitive N2-fixing nitrogenase enzyme complex. This environment is formed during heterocyst development. Developing heterocysts inactivate photosystem II and degrade antenna pigments, thereby decreasing oxygenic photosynthesis (F
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Recent data from an investigation conducted with beta cell
2022-05-04

Recent data from an investigation conducted with beta-cell cultures and animals suggest that FFAR1 gene HO-3867 receptor is modulated by stimulation of peroxisome proliferator-activated receptor gamma (PPARG) [10]. Intriguingly, in 2001 we had demonstrated effects of the PPARG Pro12Ala single nucle
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