Dysregulation of iron homeostasis by TfR-1 renders EZH2 wild type diffuse large B-cell lymphoma resistance to EZH2 inhibition.

EZH2 has been regarded as an efficient target for diffuse large B-cell lymphoma (DLBCL), but the clinical benefits of EZH2 inhibitors (EZH2i) are limited. To date, only EPZ-6438 has been approved by FDA for the treatment of follicular lymphoma and epithelioid sarcoma. We have discovered a novel EZH1/2 inhibitor HH2853 with a better antitumor effect than EPZ-6438 in preclinical studies.

Effect of duloxetine on pain relief after total knee arthroplasty: A meta-analysis of randomized controlled trials.

Background: Postoperative pain is one of the most feared complications of total knee arthroplasty. Recently, randomized controlled trials have compared the efficacy of duloxetine in patients undergoing total knee arthroplasty. However, there is no definite answer as to the efficacy and safety of duloxetine.

Regulation of CCL2 by EZH2 affects tumor-associated macrophages polarization and infiltration in breast cancer.

Tumor associated macrophages (TAMs) play an important role in tumorigenesis, development and anti-cancer drug therapy. However, very few epigenetic compounds have been elucidated to affect tumor growth by educating TAMs in the tumor microenvironment (TME). Herein, we identified that EZH2 performs a crucial role in the regulation of TAMs infiltration and protumoral polarization by interacting with human breast cancer (BC) cells.

SAF-189s, a potent new-generation ROS1 inhibitor, is active against crizotinib-resistant ROS1 mutant-driven tumors.

The ROS1 fusion kinase is an attractive antitumor target. Though with significant clinical efficacy, the well-known first-generation ROS1 inhibitor (ROS1i) crizotinib inevitably developed acquired resistance due to secondary point mutations in the ROS1 kinase. Novel ROS1is effective against mutations conferring secondary crizotinib resistance, especially G2032R, are urgently needed.

AZD9291 inactivates the PRC2 complex to mediate tumor growth inhibition.

Deregulated Polycomb repressive complex 2 (PRC2) is intimately involved in tumorigenesis and progression, making it an invaluable target for epigenetic cancer therapy. Disrupting the EZH2-EED interaction, which is required for PRC2 enzymatic activity, is a promising strategy for cancer treatment. However, this kind of inhibitors are still limited.

[Mechanism of Photochemical Degradation of MC-LR by Pyrite].

Pyrite was used as catalyst to degrade Microcystin-LR (MC-LR) at pH 6.8 under visible light irradiation (>420 nm). X-ray diffraction (XRD) and scanning electron microscope (SEM) characterization showed that pyrite had the layered structure.

Tumor-targeting efficacy of a BF211 prodrug through hydrolysis by fibroblast activation protein-α.

BF211, a bufalin (BF) derivative, exhibits stronger anti-cancer activity than BF but with potential cardiotoxicity. Fibroblast activation protein-α (FAPα) is a membrane-bound protease specifically expressed by carcinoma-associated fibroblasts, thus has been used for the selective delivery of anticancer agents. In this study, we used a FAPα-based prodrug strategy to synthesize a dipeptide (Z-Gly-Pro)-conjugated BF211 prodrug named BF211-03.

Structure-based design and synthesis of imidazo[1,2-a]pyridine derivatives as novel and potent Nek2 inhibitors with in vitro and in vivo antitumor activities.

We present herein the discovery and development of novel and potent Nek2 inhibitors with distinctive in vitro and in vivo antitumor activity based on an imidazo[1,2-a]pyridine scaffold. Our studies identified a nonlinear SAR for activity against both Nek2 and cancer cells. Bioisostere and structure-based design techniques were employed to identify compounds 42c (MBM-17, IC = 3.

Exploring the reactivity of multicomponent photocatalysts: insight into the complex valence band of BiOBr.

The band structure of multicomponent semiconductor photocatalysts, as well as their reactivity distinction under different wavelengths of light, is still unclear. BiOBr, which is a typical multicomponent semiconductor, may have two possible valence-band structures, that is, two discrete valence bands constructed respectively from O 2p and Br 4p orbitals, or one valence band derived from the hybridization of these orbitals. In this work, aqueous photocatalytic hydroxylation is applied as the probe reaction to investigate the nature and reactions of photogenerated holes in BiOBr.

[Study on determination of bovine serum albumin using o-hydroxyphenylfluorone reagent with fluorescence spectrophotometry].

The reaction conditions for the determination of bovine serum albumin (BSA) using o-hydroxyphenylfluorone (o-HPF) as fluorescence probe reagent were studied. In the B-R medium at pH 7.90, o-HPF could react with BSA, producing a stable complex compound which resulted in fluorescent quenching of this binary system.

[Study on the determination of bovine serum albumin using o-hydroxyphenylfluorone reagent with fluorescence spectrophotometry].

The reactions were studied for the determination of bovine serum albumin (BSA) using o-hydroxyphenylfluorone (o-HPF) as fluorescence probe reagent with fluorescence spectrophotometry. In the B-R medium, o-HPF reacts with BSA to form the stable complex compound. The reaction system of o-HPF and BSA was binary system, and the method for the determination of BSA was of good selectivity and stability and simplicity.

[Determination of hydrogen peroxide in rainwater by fluorometry].

The present paper introduces a new method using spectrofluorimetric analysis to determine the concentration of hydrogen peroxide in rainwater. In this method, an oxidation reaction is conducted between o-phenylenediamine (OPDA) and hydrogen peroxide in the buffer medium of NaAc-HAc at pH 4. 48 to form a new product 2,3-diaminophenazine (DAPN).

Photocatalytic degradation of the dye sulforhodamine-B: a comparative study of different light sources.

The photocatalytic degradation of dye pollutant sulforhodamine-B (SRB) in aqueous titanium dioxide (TiO2) dispersions was examined under three lighting regimes: UV light (330 nm450 nm), all investigated at pH=2.5. Total organic carbon (TOC) and chemical oxygen demand (COD(Cr)) assays show that the degradation rate of SRB is much higher when irradiated with UV and sunlight compared with visible light.

[DMF induces apoptosis in human androgen-independent prostate cancer PC3 cells in vitro].

Objective: To evaluate the antiproliferative activity of 3-(2-chlorophenyl)-1-(2-hydroxy-4, 6-dimethoxy-3-((ethyl(methyl) amino) methyl) phenyl) prop-2-en-1-one (DMF) against human androgen-independent prostate cancer PC3 cells in vitro and its underlying mechanisms.

Methods: The cytotoxic effect of DMF on PC3 cells was measured by MTT assay. Induction of apoptosis was assessed by propidium iodide staining and flow cytometric analysis.