1.Clinical effect of navigation assisted neuroendoscope hard channel technology with the assistance for treating hypertensive cerebral hemorrhage in basal ganglia region
Hanxun YAO ; Xuewei XIA ; Jing XIAO ; Wenbo WANG
Chongqing Medicine 2018;47(8):1055-1057
Objective To investigate the effect of navigation assisted neuroendoscope hard channel technology for treating hypertensive cerebral hemorrhage in basal ganglia region.Methods Eighty-two inpatients with hypertensive cerebral hemorrhage in basal ganglia region treated in this hospital were selected as the study subjects,among them 37 cases adopted the neuroendoscope hard channel technology and 45 cases adopted the small bone window craniotomy.The operation time,intraoperative bleeding vol-ume,hematoma clearance rate,postoperative complication occurrence rate and NIHSS score at postoperative 3 months were com-pared between the two groups.Results Compared with the bone window group,the operative time in the endoscopic group was lon-ger and the hematoma clearance rate was higher,intracranial rebleeding occurrence rate was lower and the short term prognosis was better(P<0.05).The aspects of intraoperative bleeding volume and other postoperative complications had no statistically signifi-cant difference between the two groups(P> 0.05).Conclusion The navigation assisted neuroendoscope hard channel technology can improve the cure rate in the patients with hypertensive cerebral hemorrhage in basal ganglia region.
2.Synthesis of selective PAK4 inhibitors for lung metastasis of lung cancer and melanoma cells.
Peilu SONG ; Fan ZHAO ; Dahong LI ; Jiqiang QU ; Miao YAO ; Yuan SU ; Hanxun WANG ; Miaomiao ZHOU ; Yujie WANG ; Yinli GAO ; Feng LI ; Dongmei ZHAO ; Fengjiao ZHANG ; Yu RAO ; Mingyu XIA ; Haitao LI ; Jian WANG ; Maosheng CHENG
Acta Pharmaceutica Sinica B 2022;12(6):2905-2922
The p21 activated kinase 4 (PAK4) is serine/threonine protein kinase that is critical for cancer progression. Guided by X-ray crystallography and structure-based optimization, we report a novel subseries of C-3-substituted 6-ethynyl-1H-indole derivatives that display high potential and specificity towards group II PAKs. Among these inhibitors, compound 55 exhibited excellent inhibitory activity and kinase selectivity, displayed superior anti-migratory and anti-invasive properties against the lung cancer cell line A549 and the melanoma cell line B16. Compound 55 exhibited potent in vivo antitumor metastatic efficacy, with over 80% and 90% inhibition of lung metastasis in A549 or B16-BL6 lung metastasis models, respectively. Further mechanistic studies demonstrated that compound 55 mitigated TGF-β1-induced epithelial-mesenchymal transition (EMT).