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Several structural classes of ASK inhibitors mostly from ind
2024-02-21

Several structural Brilliant Blue G of ASK1 inhibitors, mostly from industry but also from academia, have been identified over the last decade. In 2012, Terao et al. (Takeda) reported imidazo[1,2-α]pyridine () as a potent ASK1 inhibitor derived from structure-based drug design. GSK, Merck and Gilead
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br Materials and methods br
2024-02-21

Materials and methods Results Discussion I/R injury is characterized by myocardial damage triggered by the ischemic insult followed by reperfusion injury. While the primary insult depends mainly on the severity and duration of blood flow restriction and the breakdown of ATP-dependent pd1843
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It has been proven that genetic polymorphisms can
2024-02-21

It has been proven that genetic polymorphisms can play an important role in development of hypertension and CVDs. In a Turkish population-based study, it was found that the APLNR gene (rs948847-A445C) polymorphism was not associated with coronary artery disease (CAD), but it was shown to be related
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Despite the absence of disulfide
2024-02-21

Despite the absence of disulfide bonds in its linear structure, KT43C displays antifungal and antibacterial activity. Disulfide bonds are determinants of defensins' integrity and have been reported to increase the antimicrobial activity (Jenssen et al., 2006). However, some linear derivatives of AMP
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br Selective Androgen Receptor Modulators
2024-02-20

Selective Androgen Receptor Modulators (SARMs) The AR and its endogenous ligands, androgens, are important for development and maintenance of muscle and bone, secondary sexual organs, and development of other tissues (Mooradian et al., 1987). Although androgens are important for normal developmen
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br The lipoxygenase pathway in diseases of the nervous syste
2024-02-20

The 12/15-lipoxygenase pathway in diseases of the nervous system Conclusions and future perspectives Arachidonic pracinostat and other polyunsaturated fatty acids, and their lipid metabolites, play very important roles in human health and disease. This review has outlined the functions of 12-
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br Animal models of NAFLD Human research has greatly
2024-02-20

Animal models of NAFLD Human research has greatly shaped our understanding of non-alcoholic fatty liver disease, but several limitations exist in studying the disease processes in humans, such as variations in environmental exposure, pre-existing genetic risk factors, racial and ethnic difference
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HsALDH enzyme has been purified for
2024-02-20

HsALDH enzyme has been purified for the first time in our laboratory from human saliva and has been kinetically characterized using different aromatic substrates [35]. Also, the effect of some common substances frequently encountered by the enzyme in the oral cavity (such as ethanol, hydrogen peroxi
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Our initial approach to identify
2024-02-20

Our initial approach to identify hits was two-pronged and included a high-throughput screening (HTS) campaign of the OSI Gambogic Acid library as well as a virtual screening (VS) campaign, utilizing a publically available crystal structure of ACK1 (PDB code: ). A tolerance for protein flexibility w
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Sperm total motility and hyperactivated motility are mediate
2024-02-20

Sperm total motility and hyperactivated motility are mediated by PLD-dependent LY335979 polymerization [20]. Reduction of PIP2 synthesis inhibited actin polymerization and motility, and increasing PIP2 synthesis enhanced these activities. Furthermore, sperm demonstrating low motility contained low l
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br Conflicts of interest br Acknowledgments br Significance
2024-02-20

Conflicts of interest Acknowledgments Significance Introduction Androgen receptor (AR) plays a paramount role in the onset and progression of prostate cancer (PC) (Burnstein, 2005, Lonergan and Tindall, 2011, Watson et al., 2015). This very facet underlies androgen deprivation therapy (A
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Because of its role in tumor growth proliferation
2024-02-20

Because of its role in tumor growth, proliferation and metastasis, Axl is considered a therapeutic target. Several Axl inhibitors, including low-molecular-weight agents and antibodies, have been reported. Axl inhibition, using low-molecular-weight inhibitors or shRNA knockdown, resulted in reduced t
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Although we have achieved a great deal of success in
2024-02-20

Although we have achieved a great deal of success in the development of tools to understand autophagy in health and disease, highly specific reagents for autophagy manipulation and deep knowledge of autophagy is required to advance the research in therapeutic treatment. Better disease (ischemia) ani
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The canonical binding sites to
2024-02-20

The canonical CGS 35066 to which α2, α3, or α5 contribute are highly similar. Therefore, differences in ligand affinity will not be large even if a ligand makes optimal use of the small differences in the pockets. As a possible alternative approach to achieve separation of compound effects, ligands
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am 580 Protein microarrays represent just one
2024-02-20

Protein microarrays represent just one of a variety of experimental approaches that can be used to generate datasets of relevance to pathway mapping. Other approaches include protein am 580 profiling techniques, such as antibody arrays [29], tissue arrays [30] and 2-dimensional gel electrophoresis
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