1.Evaluation on the comprehensive acquired immunodeficiency syndrome intervention program conducting in men who have sex with men population in Inner Mongolia
Lin QU ; Bo TAO ; Jiqiang DAI ; Jingyuan YANG ; Zhuoqiang BAO
Chinese Journal of Infectious Diseases 2011;29(1):30-33
Objective To evaluation the comprehensive acquired immunodeficiency syndrome (AIDS) intervention program conducting in men who have sex with men (MSM) population living in Inner Mongolia Autonomous region. Methods A comprehensive intervention program was carried out among MSM groups in Hohhot and Baotou City. Seven hundred and six and 767 MSM were enrolled for investigation through the snowball method during May 2008 and May to June 2009, respectively.At the same time, 5 mL intravenous blood sample was collected from each subject for human immunodeficiency virus (HIV) detection and intervention effect evaluation. Data were analyzed by x2test. Results After intervention, the awareness rate of HIV/AIDS knowledge increased from 70.7%(499/706) to 81.7%(627/767) (x2 =25. 004, P<0.01 ). The rate of consistent condom use in the last six months increased from 38.0%(254/668) to 45.3% (346/764) (x2=8. 269, P<0. 05). The percentage of subjects who had more than 5 different male sexual partner during the last 6 months significantly decreased from 42.8% to 24.6% (x2 = 55. 348, P<0.01). The median number of sexual partners in MSM decreased from 3 in 2008 to 2 in 2009. The HIV infection rate was 1.7 % in both 2008 and 2009. Conclusion The comprehensive intervention program among MSM population shows positive influence after one year implementation, which is helpful for increasing HIV/AIDS awareness and safe sex behavior in this population.
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).