Discovery of a highly selective KIT kinase primary V559D mutant inhibitor for gastrointestinal stromal tumors (GISTs).

KIT kinase V559D mutation is the most prevalent primary gain-of-function mutation in Gastrointestinal Stromal Tumors (GISTs). Here we reported a highly selective KIT V559D inhibitor CHMFL-KIT-031, which displayed about 10-20 fold selectivity over KIT wt in the biochemical assay (IC: 28 nM over 168 nM; Kd: 266 nM versus 6640 nM) and in cell (EC: 176 nM versus 2000 nM for pY703) examination. It also displayed 15∼400-fold selectivity over other primary mutants such as L576P and secondary mutants including T670I, V654A (ATP binding pocket) as well as N822K and D816V (activation loop).

Effects of hyperbaric oxygen therapy on open tibial fractures in rabbits after transient seawater immersion.

Objective: To explore the effect and mechanism of hyperbaric oxygen (HBO₂) therapy of open tibial fractures in rabbits after transient seawater immersion.

Methods: Forty-eight (48) New Zealand rabbits were randomly and averagely divided into an HBO₂ therapy group (Group A) and a control group (Group B). All rabbits were subjected to unilateral open tibial fractures, while immersed in artificial seawater (20-22 °C) for three hours prior to debridement and external fixation.

FPR2 promotes invasion and metastasis of gastric cancer cells and predicts the prognosis of patients.

Formyl peptide receptor 2 (FPR2), a classical chemoattractant receptor of G-protein-coupled receptors, is reported to be involved in invasion and metastasis of some cancers, but the role of FPR2 in gastric cancer (GC) has not yet been elucidated. In this study, we found that the levels of FPR2 expression in GC were positively correlated with invasion depth, lymph node metastasis and negatively correlated with the patients' overall survival. Multivariate analysis indicated that FPR2 expression was an independent prognostic marker for GC patients.

Seawater immersion aggravates sciatic nerve injury in rats.

The aim of the present study was investigate the impact of seawater immersion on peripheral nerve injury and the underlying mechanisms. A total of 234 specific pathogen-free Sprague-Dawley male rats were randomly divided into a sham group, injury control group and seawater immersion + injury group. The Sciatic Functional Index (SFI) was used to assess nerve function for 6 weeks after injury.

Minimally invasive treatment of clavicular fractures with cannulated screw.

Objective: To evaluate minimally invasive treatment of clavicular fractures with cannulated screw.

Methods: Data of 65 patients who had undergone minimally invasive treatment with cannulated screws for clavicular fractures from April 2009 to October 2010 were retrospectively analyzed and compared with those of 65 patients with clavicular fractures who had been treated by the same surgeons with plates. In the study group, there were 41 males and 24 females, aged from 19-67 years (mean, 35.

Solitary necrotic nodule of the liver: a report of two cases and review of the literature.

To investigate the clinicopathological characteristics and possible causes of solitary necrotic nodule of the liver (SNN), two cases of SNN of the liver were studied with clinicopathological data, immunohistochemistry, and histochemistry staining. The patients had no specific symptoms, with negative results for the serum tumor markers. CT and ultrasound all showed low-density lesion.