Discovery of -(2-Acetamidobenzo[]thiazol-6-yl)-2-phenoxyacetamide Derivatives as Novel Potential BCR-ABL1 Inhibitors Through Structure-Based Virtual Screening.

BCR-ABL1 kinase is a critical driver of chronic myeloid leukemia (CML) pathophysiology. The approval of allosteric inhibitor asciminib brings new hope for overcoming drug resistance caused by mutations in the ATP-binding site. To expand the chemical diversity of BCR-ABL1 kinase inhibitors with positive anti-tumor effect with asciminib, structure-based virtual screening and molecular dynamics simulations were employed to discover novel scaffolds.

Multi-view learning with enhanced multi-weight vector projection support vector machine.

Multi-view learning aims on learning from the data represented by multiple distinct feature sets. Various multi-view support vector machine methods have been successfully applied to classification tasks. However, the existed methods often face the problems of long processing time or weak generalization on some complex datasets.

Comparison on the Electrochemical Corrosion Behavior of Ti6Al4V Alloys Fabricated by Laser Powder Bed Fusion and Casting.

The non-equilibrium solidification process in the additive manufacturing of titanium alloy leads to special microstructures, and the resulting changes in corrosion behavior are worthy of attention. In this paper, the microstructure and electrochemical corrosion behavior of Ti6Al4V alloys prepared using laser powder bed melting (LPBF) and casting are systematically compared. The results show that the LPBF-processed Ti6Al4V alloy is composed of dominant acicular α' martensite within columnar prior β phase, and less β disperses have also been discovered, which is significantly different from the α + β dual-phase structure of cast Ti6Al4V alloy.

Metformin Directly Binds to MMP-9 to Improve Plaque Stability.

Vulnerable atherosclerotic plaque rupture is the principal mechanism that accounts for myocardial infarction and stroke. High matrix metalloproteinase-9 (MMP-9) expression and activity have been proven to lead to plaque instability. Metformin, a first-line treatment for type 2 diabetes, is beneficial to plaque vulnerability.

Galectin-3-centered paracrine network mediates cardiac inflammation and fibrosis upon β-adrenergic insult.

Rapid over-activation of β-adrenergic receptors (β-AR) following acute stress initiates cardiac inflammation and injury by activating interleukin-18 (IL-18), however, the process of inflammation cascades has not been fully illustrated. The present study aimed to determine the mechanisms of cardiac inflammatory amplification following acute sympathetic activation. With bioinformatics analysis, galectin-3 was identified as a potential key downstream effector of β-AR and IL-18 activation.

Composite protective effect of benzotriazole and 2-mercaptobenzothiazole on electroplated copper coating.

Benzotriazole (BTAH) and 2-mercaptobenzothiazole (MBT) are mixed to passivate electroplated copper coatings. The growth process of passive films is comprehensively analyzed from the surface potential, microstructure and chemical composition by potential-time curve, FESEM and XPS. Meanwhile, the corrosion resistance of copper coatings with different passivation treatments is evaluated by potentiodynamic polarization curves and electrochemical impedance spectroscopy.

IMM-H007 attenuates isoprenaline-induced cardiac fibrosis through targeting TGFβ1 signaling pathway.

Upon chronic stress, β-adrenergic receptor activation induces cardiac fibrosis and leads to heart failure. The small molecule compound IMM-H007 has demonstrated protective effects in cardiovascular diseases via activation of AMP-activated protein kinase (AMPK). This study aimed to investigate IMM-H007 effects on cardiac fibrosis induced by β-adrenergic receptor activation.

Paired box 6 inhibits cardiac fibroblast differentiation.

Cardiac fibroblast (CF) differentiation plays a crucial role in cardiac fibrosis, which is a specific manifestation distinguishing pathological cardiac hypertrophy from physiological hypertrophy. The DNA-binding activity of paired box 6 (Pax6) has been shown to be oppositely regulated in physiological and pathological hypertrophy; however, it remains unclear whether Pax6 is involved in CF differentiation during cardiac fibrosis. We found that Pax6 is expressed in the heart of and CFs isolated from adult mice.

Determination of Iron Valence States Around Pits and the Influence of Fe on the Pitting Corrosion of 304 Stainless Steel.

Potassium ferricyanide and potassium ferrocyanide were used to observe and monitor the pitting corrosion of 304 stainless steel (SS) at anodic polarization in situ. The results show that there are Fe ions around the corrosion pit when pitting occurs on 304 SS in NaCl aqueous solution. The effect of Fe surrounded pits on the pitting corrosion was also studied by testing the electrochemical behavior of 304 SS in different Fe/Fe solutions.

Coupling Effects of pH and Dissolved Oxygen on the Corrosion Behavior and Mechanism of X80 Steel in Acidic Soil Simulated Solution.

In an acidic red soil environment, the corrosion mechanism of X80 steel may be closely related to the pH value and oxygen content, but it has not yet formed a systematic understanding. In this paper, the coupling effects of pH and dissolved oxygen on the corrosion behavior and mechanism of X80 steel in an acidic soil simulated solution were further analyzed by electrochemical methods and three-dimensional video microscope. Results showed that the hydrogen reduction reaction was almost the only cathode process in the anoxic and low pH system, and small and dense pits were present on the electrode surface.

α-AR overactivation induces cardiac inflammation through NLRP3 inflammasome activation.

Acute sympathetic stress causes excessive secretion of catecholamines and induces cardiac injuries, which are mainly mediated by β-adrenergic receptors (β-ARs). However, α-adrenergic receptors (α-ARs) are also expressed in the heart and are activated upon acute sympathetic stress. In the present study, we investigated whether α-AR activation induced cardiac inflammation and the underlying mechanisms.

Metformin attenuates renal fibrosis in both AMPKα2-dependent and independent manners.

Metformin is a well-known AMP-activated protein kinase (AMPK) activator, and it has been shown to inhibit organ fibrosis. Whether AMPKα2 mediates metformin protection against renal fibrosis remains unknown. Here, we aimed to investigate the role of the AMPKα2 isoform in mediating the inhibitory effect of metformin on renal fibrosis.

A portable system for on-site quantification of formaldehyde in air based on G-quadruplex halves coupled with A smartphone reader.

A portable colorimetric determination system based on G-quadruplex DNAzyme integrated with a smartphone was developed to quantitatively detect formaldehyde (FA). The method is based on the oxidation of FA by H2O2, which prevents the 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS)–H2O2 reaction catalyzed by G-quadruplex halves. With the addition of FA, the amount of the blue-green-colored free-radical cation (ABTS+) was reduced.

A one-step approach to the large-scale synthesis of functionalized MoS2 nanosheets by ionic liquid assisted grinding.

A prerequisite for exploiting most proposed applications for MoS2 is the availability of water-dispersible functionalized MoS2 nanosheets in large quantities. Here we report one-step synthesis and surface functionalization of MoS2 nanosheets by a facile ionic liquid assisted grinding method in the presence of chitosan. The selected ionic liquid with suitable surface energy could efficiently overcome the van der Waals force between the MoS2 layers.