Inhibitor of Wnt receptor 1 suppresses the effects of Wnt1, Wnt3a and β‑catenin on the proliferation and migration of C6 GSCs induced by low‑dose radiation.

The radioresistance of glioma is an important cause of treatment failure and tumor aggressiveness. In the present study, under performed with linear accelerator, the effects of 0.3 and 3.

From hit to lead: Structure-based discovery of naphthalene-1-sulfonamide derivatives as potent and selective inhibitors of fatty acid binding protein 4.

Fatty acid binding protein 4 (FABP4) plays a critical role in metabolism and inflammatory processes and therefore is a potential therapeutic target for immunometabolic diseases such as diabetes and atherosclerosis. Herein, we reported the identification of naphthalene-1-sulfonamide derivatives as novel, potent and selective FABP4 inhibitors by applying a structure-based design strategy. The binding affinities of compounds 16dk, 16do and 16du to FABP4, at the molecular level, are equivalent to or even better than that of BMS309403.

Characterization of naturally occurring pentacyclic triterpenes as novel inhibitors of deubiquitinating protease USP7 with anticancer activity in vitro.

Deubiquitinating protease USP7 is a promising therapeutic target for cancer treatment, and interest in developing USP7 inhibitors has greatly increased. In the present study, we reported a series of natural pentacyclic triterpenes with USP7 inhibitory activity in vitro. Among them, both the ursane triterpenes and oleanane triterpenes were more active than the lupine triterpenes, whereas ursolic acid was the most potent with IC of 7.

Benzbromarone, an old uricosuric drug, inhibits human fatty acid binding protein 4 in vitro and lowers the blood glucose level in db/db mice.

Aim: Fatty acid-binding protein 4 (FABP4) plays an important role in maintaining glucose and lipid homeostasis. The aim of this study was to find new inhibitors of FABP4 for the treatment of type 2 diabetes.

Methods: Human FABP4 protein was expressed, and its inhibitors were detected in 1,8-ANS displacement assay.

The essential role for aromatic cluster in the β3 adrenergic receptor.

Aim: To explore the function of the conserved aromatic cluster F213(5.47), F308(6.51), and F309(6.

Classification of 5-HT(1A) receptor agonists and antagonists using GA-SVM method.

Aim: To construct a reliable computational model for the classification of agonists and antagonists of 5-HT(1A) receptor.

Methods: Support vector machine (SVM), a well-known machine learning method, was employed to build a prediction model, and genetic algorithm (GA) was used to select the most relevant descriptors and to optimize two important parameters, C and r of the SVM model. The overall dataset used in this study comprised 284 ligands of the 5-HT(1A) receptor with diverse structures reported in the literatures.

[The effect of lead exposure in utero on the teeth eruption and enamel development of rat offspring.].

Objective: To investigate the effects of lead exposure at different levels in utero on the teeth eruption and enamel development of rat offsprings.

Methods: 27 pregnant SD rats were divided into three groups randomly: high level lead group (HLG), low level lead group (LLG) and control group with nine rats in each group. The three groups from the gestation day to the end of the gestation were given either deionized water in control group or deionized water containing 200 mg/L Pb2+ as lead acetate through drinking method in high level lead experimental group and 50 mg/L Pb2+ as lead acetate through drinking method in low level lead experimental group.