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A new approach to the facile synthesis of 2-substituted-quinazolin-4(3H)-ones

Chinese Chemical Letters 2011年第8期22卷 951-953页

作者： Bin Wang Zeng Li Xiao Ning Wang jia heng tan Lian Quan Gu Zhi Shu Huang School of Pharmaceutical Sciences Sun Yat-sen University Guanzhou 510006 China Department of Chemistry and Lithe Science Xiangnan University Chenzhou 423000 China

A new approach to the facile synthesis of 2-substituted-quinazolin-4（3H）-ones and its derivatives using the condensation reaction of substituted 2-aminobenzamide and orthoesters is reported.

关键词： Quinazolin-4(3H)-ones Synthesis Aminobenzamide Orthoester

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Specific Recognition of Quindoline Derivatives on Promoter G-Quadruplex and the Biological Relevance

Specific Recognition of Quindoline Derivatives on Promoter G...

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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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Inhibiting SHP2 reduces glycolysis, promotes microglial M1 polarization, and alleviates secondary inflammation following spinal cord injury in a mouse model

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Neural Regeneration Research 2025年第3期20卷 858-872页

作者： Xintian Ding Chun Chen heng Zhao Bin Dai Lei Ye Tao Song Shuai Huang jia Wang Tao You Department of Orthopedics The First Affiliated Hospital of USTCDivision of Life Sciences and MedicineUniversity of Science and Technology of ChinaHefeiAnhui ProvinceChina Department of Orthopedics Provincial Hospital Affiliated to Anhui Medical UniversityHefeiAnhui ProvinceChina

Reducing the secondary inflammatory response, which is partly mediated by microglia, is a key focus in the treatment of spinal cord injury. Src homology 2-containing protein tyrosine phosphatase 2(SHP2), encoded by PTPN11, is widely expressed in the human body and plays a role in inflammation through various mechanisms. Therefore, SHP2 is considered a potential target for the treatment of inflammation-related diseases. However, its role in secondary inflammation after spinal cord injury remains unclear. In this study, SHP2 was found to be abundantly expressed in microglia at the site of spinal cord injury. Inhibition of SHP2 expression using siRNA and SHP2 inhibitors attenuated the microglial inflammatory response in an in vitro lipopolysaccharide-induced model of inflammation. Notably, after treatment with SHP2 inhibitors, mice with spinal cord injury exhibited significantly improved hind limb locomotor function and reduced residual urine volume in the bladder. Subsequent in vitro experiments showed that, in microglia stimulated with lipopolysaccharide, inhibiting SHP2 expression promoted M2 polarization and inhibited M1 polarization. Finally, a co-culture experiment was conducted to assess the effect of microglia treated with SHP2 inhibitors on neuronal cells. The results demonstrated that inflammatory factors produced by microglia promoted neuronal apoptosis, while inhibiting SHP2 expression mitigated these effects. Collectively, our findings suggest that SHP2 enhances secondary inflammation and neuronal damage subsequent to spinal cord injury by modulating microglial phenotype. Therefore, inhibiting SHP2 alleviates the inflammatory response in mice with spinal cord injury and promotes functional recovery postinjury.

关键词： apoptosis glycolysis inflammatory response microglia neurons polarization spinal cord injury Src homology 2-containing protein tyrosine phosphatase 2

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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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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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Temporal and spatial regulation of biomimetic vascularization in 3D-printed skeletal muscles

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Bio-Design and Manufacturing 2024年第5期7卷 597-610页

作者： Minxuan jia Tingting Fan tan jia Xin Liu heng Liu Qi Gu Key Laboratory of Organ Regeneration and Reconstruction State Key Laboratory of Membrane BiologyInstitute of ZoologyChinese Academy of SciencesBeijing 100101China Beijing Institute for Stem Cell and Regenerative Medicine Beijing 100101China University of Chinese Academy of Sciences Beijing 100049China State Key Laboratory of Stem Cell and Reproductive Biology Institute of ZoologyChinese Academy of SciencesBeijing 100101China Department of Orthopaedics Beijing Jishuitan HospitalCapital Medical UniversityBeijing 100035China

In the intricate skeletal muscle tissue,the symbiotic relationship between myotubes and their supporting vasculature is pivotal in delivering essential oxygen and *** study explored the complex interplay between skeletal muscle and endothelial cells in the vascularization ofmuscle *** harnessing the capabilities of three-dimensional(3D)bioprinting and modeling,we developed a novel approach involving the co-construction of endothelial and muscle cells,followed by their subsequent *** findings highlight the importance of the interaction dynamics between these two cell ***,introducing endothelial cells during the advanced phases of muscle differentiation enhanced myotube ***,it stimulated the development of the vascular network,paving the way for the early stages of vascularized skeletal muscle *** methodology proposed in this study indicates the potential for constructing large-scale,physiologically aligned skeletal ***,it highlights the need for exploring the delicate equilibrium and mutual interactions between muscle and endothelial *** on the multicell-type interaction model,we can predict promising pathways for constructing even more intricate tissues or organs.

关键词： Skeletal muscle Vascularization 3D bioprinting Cell interaction

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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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