4篇
您的检索式：作者名="Sunliang Cui"
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| 1 | Discovery of a small molecule inhibitor of cullin neddylation that triggers ER stress to induce autophagy显示文摘Protein neddylation is catalyzed by a three-enzyme cascade,namely an E1 NEDD8-activating enzyme(NAE),one of two E2 NEDD8 conjugation enzymes and one of several E3 NEDD8 ligases.The physiological substrates of neddylation are the family members of cullin,the scaffold component of cullin RING ligases(CRLs).Currently,a potent E1 inhibitor,MLN4924,also known as pevonedistat,is in several clinical trials for anti-cancer therapy.Here we report the discovery,through virtual screening and structural modifications,of a small molecule compound HA-1141 that directly binds to NAE in both in vitro and in vivo assays and effectively inhibits neddylation of cullins 1 e5.Surprisingly,unlike MLN4924,HA-1141 also triggers non-canonical endoplasmic reticulum(ER)stress and PKR-mediated terminal integrated stress response(ISR)to activate ATF4 at an early stage,and to inhibit protein synthesis and mTORC1 activity at a later stage,eventually leading to autophagy induction.Biologically,HA-1141 suppresses growth and survival of cultured lung cancer cells and tumor growth in in vivo xenograft lung cancer models at a well-tolerated dose.Taken together,our study has identified a small molecule compound with the dual activities of blocking neddylation and triggering ER stress,leading to growth suppression of cancer cells. | Yanan Li Chaorong Wang Tiantian Xu Peichen Pan Qing Yu Lei Xu Xiufang Xiong Tingjun Hou Sunliang Cui Yi Sun | 2021 | Acta Pharmaceutica Sinica B2021，11，11： | 1 |
| 2 | Molecular iodine-catalyzed one-pot synthesis of substituted quinolines from imines and aldehydes显示文摘 | Lin Xufeng Cui Sunliang Wang Yanguang | 2006 | Tetrahedron Lett2006，47，18： | 1 |
| 3 | Oxoarylation of ynamides with N-aryl hydroxamic acids显示文摘Ynamides are electron-rich alkynes with unique reactivities and act as flexible building blocks in organic synthesis.Therefore,the investigation for transformation of ynamides with exceptional selectivity and efficiency is attractive and interesting.Herein,we report an oxoarylation of ynamides with N-aryl hydroxamic acids.In the presence of catalytic Cu(OTf)_(2),both the terminal and internal ynamides could undergo an addition/[3,3] sigmatropic rearrangement cascade with N-aryl hydroxamic acids to achieve oxoarylation,along with providing selective entry to(ortho-amino)arylacetamides and oxindoles.Moreover,deuterium-labelling reaction and gram-scale reaction were conducted to probe the mechanism and showcase the scalability. | Changwei Chen Hongyu Zhang Gang Xu Sunliang Cui | 2021 | Chinese Chemical Letters2021，32，8： | 0 |
| 4 | BF_3-promoted annulation of azonaphthalenes and ynamides for synthesis of benzo[e]indoles显示文摘A novel BF_(3)-promoted [3+2] annulation of azonaphthalenes and ynamides is described.This protocol provides a modular and efficient entry to functionalized amino benzo[e]indole derivatives smoothly. | Changwei Chen Sunliang Cui | 2021 | Chinese Chemical Letters2021，32，1： | 0 |
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