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第八届全国化学生物学学术会议

作者： tian-miao ou Yue Wu Jia-heng Tan Lian-quan Gu Zhi-shu Huang School of Pharmaceutical Sciences Sun Yat-sen University

＜正＞G-quadruplexes are unique secondary structure exist in various non-coding region of human genome and exhibit important biological roles in the regulation of gene replication,transcription,and *** derivatives are a modified series of derivatives from natural product cryptolepine and showed great stabilizing ability on G-quadruplex in c-myc promoter in the previous *** I will present our

关键词： G-quadruplex oncogene promoter quindoline derivatives transcription regulation

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5-N-Methylated Quindoline Derivatives as G-Quadruplex Stabilizing Ligands and Potential Inhibitors of Telomerase

5-N-Methylated Quindoline Derivatives as G-Quadruplex Stabil...

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第五届全国化学生物学学术会议

作者： Yu-Jing Lu tian-miao ou Ning Sun Jia-Heng Tan Zhi-Shu Huang~* Lian-Quan Gu~* School of Pharmaceutical Sciences,Sun Yat-sen University,Guangzhou 510275,China

＜正＞A series of 5-N-methylated quindoline derivatives were designed and synthesized to develop potent telomerase *** interaction of these compounds with human telomeric G-quadruplex DNA was investigated via PCR-stop *** compounds as inhibitors of telomerase were also examined through the utilization of modified telomerase repeat amplification

关键词： 5-N-methylated quindoline synthesis telomeric G-quadruplex DNA telomerase inhibitor

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Anti-angiogenic Potentials of Quindoline Derivatives Targeting G-quadruplex Structure in Vascular Endothelial Cell Growth Factor

Anti-angiogenic Potentials of Quindoline Derivatives Targeti...

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第五届全国化学生物学学术会议

作者： tian-miao ou Yu-Jing Lu Ning Sun Xie-Fan Fang Zeng-Yun An Zhi-Shu Huang~* Lian-Quan Gu~* School of Pharmaceutical Sciences,Sun Yat-sen University,Guangzhou 510275,China

＜正＞Vascular endothelial growth factor（VEGF）is probably the most important angiogenesis inducer,and over-expression of VEGF and its receptors promote blood vessel formation which may be related with tumor *** have been reported that specific G-quadruplex structures could be formed by the G-rich sequence within the human VEGF promoter region,raising the possibility

关键词： G-quadruplex VEGF quindoline derivatives anti-angiogenic

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Molecular Dynamics Simulation of a Ligand Binding to G-Quadruplex with Different Binding modes

Molecular Dynamics Simulation of a Ligand Binding to G-Quadr...

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2011年全国药物化学学术会议——药物的源头创新

作者： Jin-Qiang Hou,Shuo-Bin Chen,Jia-Heng Tan,tian-miao ou,Lian-Quan Gu and Zhi-Shu Huang~* School of Pharmaceutical Sciences,Sun Yat-sen University,Guangzhou,510006,People''s Republic of China.

＜正＞G-quadruplexes are higher-order DNA ＆ RNA structures formed from guanine-rich sequences and have recently emerged as a new class of potential molecular targets for anticancer drugs. Understanding the three-dimensional interactions between small-molecule ligands and their G-quadruplex targets in solution is the key for rational drug design and effective G-quadruplex ligand *** ligand design efforts have to date focused in large part on the G-quartet ***,ligands binding to the loop nucleotides were also observed from crystallography *** is still unclear that whether ligand could stably bind to loop nucleotides in solution states and how ligands in such binding mode impact on the stability of G-quadruplex ***,we also aim to elucidate how ligands in distinct binding modes influence the G-quadruplex ***,from crystal structure,different ligand-binding models were built and simulated by molecular dynamics *** on a series of computational analyses, the results suggested that ligand binding to the loop was viable in aqueous solution,which was depended on the particular rearrangement of *** ligands binding to the loops had negative impact on the G-quadruplex stability,whereas the ligands binding to the G-quartets had positive impact on the G-quadruplex ***,the ligands simultaneously binding to the quartets and loops had the best stabilizations effect on the G-quadruplex *** findings can help to understand the structural role of ligands with different binding modes in G-quadruplex stability and assist in the design of selective and effective G-quadruplex ligands.

关键词： Molecular dynamics simulation G-Quadruplex G-quartet Naphthalene diimide derivative

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Discovery of Novel Anti-tumour Agents for Specific Recognizing the G-quadruplex in 5'-Untranslated Region of Human Vascular Endothelial Growth Factor(hVEGF)

Discovery of Novel Anti-tumour Agents for Specific Recognizi...

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第九届全国核糖核酸学术讨论会

作者：王世珂 Yue Wu Xiao-Qin Wang Guo-Tao Kuang Qi Zhang Giulia Biffi Shu-Ling Lin Hui-Yun Liu Jia-Heng Tan Zhi-Shu Huang Lian-Quan Gu tian-miao ou 中山大学药学院 School of Pharmacy Guangdong Medical College Cancer Research UK Cambridge Institute University of CambridgeLi Ka Shing Centre

Angiogenesis is important in tumorigenesis and tumor *** vascular endothelial growth factor(h VEGF)is an angiogenic growth factor that plays a crucial role in tumor *** G-rich region within the 5’-untranslated region(5’-UTR)of h VEGF m RNA can form a‘switchable’RNA G-quadruplex structure that is essential for a cap-independent translation *** firstly screen our small-molecule library for binders of this *** a result,a novel quinazoline derivative compound 1shows a significant specific interaction with the G-tract and destabilizes the Gquadruplex *** experiments results reveal that compound 1 downregulates h VEGF translation,and significantly impedes tumor cells *** also find thatcompound1exhibitsan obvious tumor inhibiting activity in MCF-7 xenograft tumors,which may relate with its ability to reduce h VEGF *** findings provide a new way of h VEGF translational control through interacting with Gquadruplex structure in the 5’UTRby small molecules.

关键词： VEGF translational regulation G-quadruplex quinazoline derivative antitumor

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Rational design of novel fusion dyes:specific indicators for G-quadruplex nucleic acids

Rational design of novel fusion dyes:specific indicators for...

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2011年全国药物化学学术会议——药物的源头创新

作者： Jin-Wu Yan,Wen-Jie Ye,Shuo-Bin Chen,Wei-Bin Wu,Jin-Qiang Hou,Jia-Heng Tan~*,tian-miao ou, Lian-Quan Gu,Zhi-Shu Huang School of Pharmaceutical Sciences,Sun Yat-Sen University,Guangzhou 510006,People''s Republic of China

＜正＞G-quadruplexes are unique secondary structures formed by G-rich nucleic acid sequences in many pivotal genomic regions and receiving a great deal of attention as uncovering their important biological *** years,m...

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Disubstituted quinazoline derivatives as a new type of highly selective ligands for telomeric G-quadruplex DNA

Disubstituted quinazoline derivatives as a new type of highl...

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2011年全国药物化学学术会议——药物的源头创新

作者： Zeng Li,tian-miao ou,Jia-Heng Tan,Jin-Hui He,Yi Long,Ding Li,~* Lian-Quan Gu,Zhi-Shu Huang~* School of Pharmaceutical Sciences,Sun Yat-sen University,Guangzhou University City,Waihuan East Road 132,Guangzhou 510006,People''s Republic of China.

＜正＞A series of 2,4-disubstituted quinazoline derivatives with one imitative tetracyclic aromatic plane formed through intramolecular hydrogen bond and two positively charged side chains found to be a new type of highly selective ligand to bind with telomeric G-quadruplex DNA,and their biological properties were reported for the first *** interactions with telomeric

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C-5-methyl-cytosine stabilizing G-quadruplex DNA in bcl-2 promoter

C-5-methyl-cytosine stabilizing G-quadruplex DNA in bcl-2 pr...

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2011年全国药物化学学术会议——药物的源头创新

作者： Jing Lin,Jin-qiang Hou,Han-dan Xiang,Yi-yong Yan,Yu-chao Gu,Jia-heng Tan,Ding Li,Lian-quan Gu, tian-miao ou,and Zhi-shu Huang~* Inistitute of Medicinal Chemistry,School of Pharmaceutical Sciences,Sun Yat-sen University, Guangzhou University City,Waihuan East Road 132,Guangzhou 510006

＜正＞The epigenetic modification of gene-5-C-methylation of cytosine plays significance roles in regulating gene transcription through DNA hypermethylation or ***,the molecular details on how DNA methylated state regulates gene expression is not well understood. In the present work,we hypothesized a potential molecular mechanism for explaining this question,which is associated with the G-quadruplex,a special DNA secondary structure,which in most cases,acts as an impediment to gene ***,we demonstrated that methylation induced a conformational transition of the G-quadruplex formed by the P1 promoter of bcl-2 and increased the stability of this ***,cytosine methylation enhanced G-quadruplex’s competition with duplex formation as well as the ability to arrest the polymerase in *** results suggested that one possible mechanism of cytosine methylation to suppress gene transcription is achieved through stabilizing the blockader-G-quadruplex in the promoters of human genes.

关键词： Cytosine DNA methylation G-quadruplex

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Natural products and their derivatives as G-quadruplex binding ligands

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Science China Chemistry 2013年第10期56卷 1351-1363页

作者： SHAN Chan TAN Jia-Heng ou tian-miao HUANG Zhi-Shu School of Pharmaceutical Sciences Sun Yat-sen University

G-quadruplexes comprise a class of secondary structures that are formed in guanine-rich sequences in eukaryotic genomes and play a crucial role in the regulation of many biological events.G-quadruplexes have become targets for anticancer drugs with high selectivity *** DNA and low cytotoxicity against normal *** products and their derivatives display polymorphism,structural complexity,and potent *** is,therefore,reasonable to seek ligands targeting G-quadruplexes from natural ***,many successful examples have been reported,showing ligands with excellent anticancer *** this review,we summarized the development of research on natural products and derivatives that target G-quadruplex structures in an effort to guide future studies.

关键词： G-quadruplex binding ligands natural products derivatives

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Face Age Estimation Based on CSLBP and Lightweight Convolutional Neural Network

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Computers, Materials & Continua 2021年第11期69卷 2203-2216页

作者： Yang Wang Ying tian ou tian School of Computer Science and Software Engineering University of Science&Technology LiaoningAnshan114051China Medical and Health Sciences University of WollongongNSW2522Australia

As the use of facial attributes continues to expand,research into facial age estimation is also *** face images are easily affected by factors including illumination and occlusion,the age estimation of faces is a challenging *** paper proposes a face age estimation algorithm based on lightweight convolutional neural network in view of the complexity of the environment and the limitations of device computing *** face age estimation based on Soft Stagewise Regression Network(SSR-Net)and facial images,this paper employs the Center Symmetric Local Binary Pattern(CSLBP)method to obtain the feature image and then combines the face image and the feature image as network input *** feature images to the convolutional neural network can improve the accuracy as well as increase the network model *** experimental results on IMDB-WIKI and MORPH 2 datasets show that the lightweight convolutional neural network method proposed in this paper reduces model complexity and increases the accuracy of face age estimations.

关键词： Face age estimation lightweight convolutional neural network CSLBP SSR-Net

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