|
|
|
题名
|
作者
|
年代
|
出处
|
被引量
|
| 1 | Novel dual inhibitor for targeting PIM1 and FGFR1 kinases inhibits colorectal cancer growth in vitro and patient-derived xenografts in vivo显示文摘Colorectal cancer(CRC) is the second most common cause of cancer-related death in the world. The pro-viral integration site for Moloney murine leukemia virus 1(PIM1) is a proto-oncogene and belongs to the serine/threonine kinase family, which are involved in cell proliferation, migration,and apoptosis. Fibroblast growth factor receptor 1(FGFR1) is a tyrosine kinase that has been implicated in cell proliferation, differentiation and migration. Small molecule HCI-48 is a derivative of chalcone, a class of compounds known to possess anti-tumor, anti-inflammatory and antibacterial effects. However,the underlying mechanism of chalcones against colorectal cancer remains unclear. This study reports that HCI-48 mainly targets PIM1 and FGFR1 kinases, thereby eliciting antitumor effects on colorectal cancer growth in vitro and in vivo. HCI-48 inhibited the activity of both PIM1 and FGFR1 kinases in an ATPdependent manner, as revealed by computational docking models. Cell-based assays showed that HCI-48inhibited cell proliferation in CRC cells(HCT-15, DLD1, HCT-116 and SW620), and induced cell cycle arrest in the G2/M phase through modulation of cyclin A2. HCI-48 also induced cellular apoptosis, as evidenced by an increase in the expression of apoptosis biomarkers such as cleaved PARP, cleaved caspase 3 and cleaved caspase 7. Moreover, HCI-48 attenuated the activation of downstream components of the PIM1 and FGFR1 signaling pathways. Using patient-derived xenograft(PDX) murine tumor models,we found that treatment with HCI-48 diminished the PDX tumor growth of implanted CRC tissue expressing high protein levels of PIM1 and FGFR1. This study suggests that the inhibitory effect of HCI-48 on colorectal tumor growth is mainly mediated through the dual-targeting of PIM1 and FGFR1kinases. This work provides a theoretical basis for the future application of HCI-48 in the treatment of clinical CRC. | Fanxiang Yin Ran Zhao Dhilli Rao Gorja Xiaorong Fu Ning Lu Hai Huang Beibei Xu Hanyong Chen Jung-Hyun Shim Kangdong Liu Zhi Li Kyle Vaughn Laster Zigang Dong Mee-Hyun Lee | 2022 | Acta Pharmaceutica Sinica B2022，12，11： | 1 |
| 2 | Reconstruction of intersecting curved solids from 2D orthographic views 显示文摘 | Fu Zigang Zou Beiji Chen Yiming | 2010 | Computer-Aided Design2010，42，9： | 1 |
| 3 | Prediction of Potential Distribution of the Genus Cricotopus(Diptera:Chironomidae)Based on MaxEnt Model显示文摘The prediction of suitable area is a method for predicting the potential distribution by using the maximum entropy model.This study predicted the potential suitable habitats for the genus Cricotopus of Chironomidae in China.The latitude and longitude information of 98 distribution sites of Cricotopus in China and the biological environmental factors and altitude distribution in China were collected,and suitable habitats for Cricotopus were predicted,obtaining the suitable ranges and areas of Cricotopus in China,which is consistent with the known living conditions of Cricotopus.The study on the diversity of Cricotopus and the prediction of its suitable habitats provide a theoretical basis for Cricotopus in water monitoring and paddy fields,as well as basic data for the study on the genus Cricotopus. | Zigang XU Yuanyuan YAO Qing CHEN Panpan XIANG Jingru SHANGGUAN Shiwang LIU Yue FU | 2023 | Agricultural Biotechnology2023，12，6： | 0 |
| 4 | Orbital magnetization of the electron gas on a two-dimensional kagome' lattice under a perpendicular magnetic field显示文摘The orbital magnetization of the electron gas on a two-dimensional kagome' lattice under a perpendicular magnetic field is theoretically investigated.The interplay between the lattice geometry and magnetic field induces nontrivial k-space Chern invariant in the magnetic Brillouin zone,which turns to result in profound effects on the magnetization properties.We show that the Berry-phase term in the magnetization gives a paramagnetic contribution,while the conventional term brought about by the magnetic response of the magnetic Bloch bands produces a diamagnetic contribution.As a result,the superposition of these two components gives rise to a delicate oscillatory structure in the magnetization curve when varying the electron filling factor.The relationship between this oscillatory behavior and the Hofstadter energy spectrum is revealed by selectively discussing the magnetization and its two components at the commensurate fluxes of f = 1/4,1/3,and 1/6,respectively.In particular,we reveal as a typical example the fractal structure in the magnetic oscillations by tuning the commensurate flux around f = 1/4.The finite-temperature effect on the magnetization is also discussed. | YUAN ZiGang WANG ZhiGang FU ZhenGuo LI ShuShen ZHANG Ping | 2012 | Science China(Physics,Mechanics & Astronomy)2012，55，10： | 0 |
您所在的机构暂未开通此部分的功能，请联系管理员