Article
Biochemistry & Molecular Biology
Carla Bazzicalupi, Alessandro Bonardi, Tarita Biver, Marta Ferraroni, Francesco Papi, Matteo Savastano, Paolo Lombardi, Paola Gratteri
Summary: The interaction between a series of berberine derivatives and human telomeric G-quadruplexes was investigated in this study. The results showed the formation of 1:1 complexes between the derivatives and Tel12. The linkers' length had a correlation with the strength of binding and affected the G4 stabilization effect. This study provides important insights into the mechanism of berberine derivatives in inhibiting telomerase activity in malignant cells.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Chemistry, Medicinal
Jonathan Dickerhoff, Nicole Brundridge, Scott A. McLuckey, Danzhou Yang
Summary: The medicinal natural product berberine is actively studied as a G4-ligand, particularly in targeting the MycG4 structure. Recent research has revealed that the binding mode and stoichiometry of berberine to MycG4 in solution differs significantly from the crystal structure, suggesting the importance of validating ligand-DNA interactions in future rational drug design.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Nuno M. M. Moura, Jose A. S. Cavaleiro, Maria Graca P. M. S. Neves, Catarina I. V. Ramos
Summary: As tumours are closely related to the telomerase function and oncogene expression, the structure of enzymes and genes involved are being targeted for new anticancer drugs. The use of ligands to stabilize G4 DNA structures, such as the telomeric DNA sequence, is considered a promising strategy for cancer therapies. This study evaluated the efficacy of three tetracationic opp-dibenzoporphyrins in stabilizing G4 structures, with the free-base porphyrin and its zinc(II) complex showing good affinity and selectivity for the telomeric G4 structure.
Review
Chemistry, Multidisciplinary
Shubhanwita Basak, Soumi Biswas, Jishu Naskar
Summary: Genomic DNA exists in its canonical B-form, but oligonucleotides can adopt various non-canonical secondary structures such as hairpins, cruciforms, triplexes, quadruplexes (G4), and i-motifs. G4s, formed by guanine-rich oligonucleotides, are found in telomeres, promoter oncogenes, immunoglobulin switch regions, and ribosomal DNA. Recent research has linked G4s to various human diseases, including cancer. Stabilizing G4s with designed molecules or drugs can inhibit the transcription of oncogenes and hinder telomere biogenesis, which is crucial in cancer prevention. G4 is an important molecular target for the discovery of anti-cancer drugs. Among the molecules targeting G4, peptides are particularly interesting due to their small size, simple synthetic methodology, low cytotoxicity, and cellular permeability. This review mainly discusses structurally diverse peptides reported between 2000 and 2022, their potential to target non-canonical G-quadruplex (G4) nucleic acid structures, and their biomedical applications.
Article
Chemistry, Multidisciplinary
Ismail A. Elhaty
Summary: The study found that the quinazoline derivative GW2974 has a strong affinity for human telomeric G-quadruplex, and can inhibit telomerase enzyme activity by altering the stability of G-quadruplex DNA.
Article
Biochemistry & Molecular Biology
Yun Dong, Ming-Hao Hu
Summary: A minimalistic fluorescent probe has been developed in this study, which exhibits selective detection and mapping of parallel topology of cellular RNA G4.
BIOORGANIC CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Chuanqi Zhao, Geng Qin, Jingsheng Niu, Zhao Wang, Chunyu Wang, Jinsong Ren, Xiaogang Qu
Summary: Researchers found that specific sequences in the SARS-CoV-2 genome can form G4 structures, and their biofunctions can be regulated by specific compounds, providing new insights for developing novel antiviral drugs against COVID-19.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2021)
Article
Chemistry, Physical
Mengxin Li, Yalong Cong, Yifei Qi, John Z. H. Zhang
Summary: Human telomerase activity in cancer cells is significantly higher than in normal cells, leading to immortal proliferation of cancer cells. Stabilizing G-quadruplexes formed in the guanine-rich sequence is a potential anti-cancer therapy. Berberine, derived from traditional Chinese medicines, has shown promise in stabilizing G-quadruplexes. Molecular dynamics simulations were conducted to investigate the atomic interactions between G-quadruplexes and berberine derivatives. Precise simulation results were obtained by testing various force fields and charge models. The binding energies and analyses demonstrated the stability of G-quadruplexes in the presence of ligands and the higher affinity of berberine derivatives compared to berberine. Van der Waals interactions were identified as the most favorable interactions between the derivatives and the G-quadruplexes. These findings provide crucial insights into the atomic-level binding of G-quadruplexes and their inhibitors.
PHYSICAL CHEMISTRY CHEMICAL PHYSICS
(2023)
Article
Chemistry, Medicinal
Mao-Lin Li, Jing-Mei Yuan, Hao Yuan, Bi-Han Wu, Shi-Liang Huang, Qing-Jiang Li, Tian-Miao Ou, Hong-Gen Wang, Jia-Heng Tan, Ding Li, Shuo-Bin Chen, Zhi-Shu Huang
Summary: Research suggests that drugs targeting G4 structures and improving anti-tumor activity through the introduction of carbohydrates could be a promising option for cancer treatment.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Analytical
Ranran Sun, Xiaomeng Guo, Dawei Yang, Yalin Tang, Jie Lu, Hongxia Sun
Summary: The Cy-1 dye fluorescent probe exhibits over 1000-fold fluorescence enhancement for recognizing c-myc G-quadruplex and shows good specificity in selectively recognizing this structure. These properties make Cy-1 a promising tool for c-myc G-quadruplex recognition in nanotechnology or biology.
Article
Chemistry, Multidisciplinary
Soumi Biswas, Shubhanwita Basak, Satyabrata Samui, Sanjeev Pasadi, K. Muniyappa, Jishu Naskar
Summary: This study describes the co-assembly of a synthetic dendron-like peptide, C-delta 3-(YYEE)-E, with G4 DNA in aqueous buffer containing Na+ ions. Biophysical and molecular docking studies have confirmed the co-assembly phenomenon and the peptide's ability to enhance the thermal stability of G4 DNA. The peptide inhibits telomerase activity and down-regulates oncogenic expression, exhibiting significant cytotoxic effects on cancer cells compared to non-cancer cells.
Article
Biochemistry & Molecular Biology
Suganthi Soundarapandian, Aleyamma Alexander, Archana Sumohan Pillai, Israel V. M. V. Enoch, Sameena Yousuf
Summary: A novel anthraquinonesulfonyl derivative of beta-cyclodextrin was prepared and characterized, showing enhanced fluorescence of ethidium bromide and berberine when encapsulated in the cyclodextrin's cavity. The conjugate displayed selective fluorescence quenching on quadruplex DNAs kit22 and telo24. Binding constants were determined for different molecules encapsulated by the beta-cyclodextrin conjugate, showing varying fluorescence behaviors.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2022)
Article
Pharmacology & Pharmacy
Qiong Huang, Xiao Wang, An Chen, Hua Zhang, Qimeng Yu, Chenfeng Shen, Annoor Awadasseid, Xiaoyin Zhao, Xuqiong Xiong, Yanling Wu, Wen Zhang
Summary: A series of new naphthalimide derivatives have been designed and synthesized, among which compound 7c displayed the strongest anti-tumor activity with the best selectivity for HepG2 cells. It was found that 7c induced HepG2 cell apoptosis, hindered cancer cell migration, and arrested the cell cycle at the G2/M phase. Mechanism studies revealed that 7c selectively induced a G-rich HRCC DNA sequence in the mitochondria to form a G-quadruplex structure, causing mitochondrial dysfunction and ultimately leading to proliferative inhibition and apoptosis of cancer cells.
BIOCHEMICAL PHARMACOLOGY
(2022)
Review
Biochemistry & Molecular Biology
Patricia M. Toro, Marianela Saldias, Gabriela Valenzuela-Barra
Summary: This study provides a comprehensive review of metal compound G4 binders and their structural features that enable them to recognize G-quartets and stabilize DNA G4 structures.
CURRENT MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Dandan Zhang, Guiqing Xu, Jie Zhao, Yue Wang, Xiaofang Wu, Xing He, Wei Li, Shuting Zhang, Shouning Yang, Chunhua Ma, Yuqin Jiang, Qingjie Ding
Summary: BTK inhibitors are promising drugs for hematological tumors treatment with high selectivity and reduced side effects. Designed range of inhibitors showed potent activity in vitro and can be further developed.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Yong Rao, Hong Liu, Lin Gao, Hong Yu, Jia-Heng Tan, Tian-Miao Ou, Shi-Liang Huang, Lian-Quan Gu, Ji-Ming Ye, Zhi-Shu Huang
BIOORGANIC & MEDICINAL CHEMISTRY
(2015)
Review
Chemistry, Medicinal
Jun Qiu, Mingxue Wang, Yan Zhang, Ping Zeng, Tian-Miao Ou, Jia-Heng Tan, Shi-Liang Huang, Lin-Kun An, Honggen Wang, Lian-Quan Gu, Zhi-Shu Huang, Ding Li
CURRENT TOPICS IN MEDICINAL CHEMISTRY
(2015)
Article
Chemistry, Medicinal
Xiao-Qin Wang, Chun-Li Xia, Shuo-Bin Chen, Jia-Heng Tan, Tian-Miao Ou, Shi-Liang Huang, Ding Li, Lian-Quan Gu, Zhi-Shu Huang
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2015)
Article
Chemistry, Medicinal
Bing-Lei Yao, Yan-Wen Mai, Shuo-Bin Chen, Hua-Ting Xie, Pei-Fen Yao, Tian-Miao Ou, Jia-Heng Tan, Hong-Gen Wang, Ding Li, Shi-Liang Huang, Lian-Quan Gu, Zhi-Shu Huang
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2015)
Article
Chemistry, Medicinal
Yong Rao, Hong Liu, Lin Gao, Hong Yu, Tian-Miao Ou, Jia-Heng Tan, Shi-Liang Huang, Hong-Gen Wang, Ding Li, Lian-Quan Gu, Ji-Ming Ye, Zhi-Shu Huang
JOURNAL OF MEDICINAL CHEMISTRY
(2015)
Article
Chemistry, Medicinal
Peng-Hui Li, Ping Zeng, Shuo-Bin Chen, Pei-Fen Yao, Yan-Wen Mai, Jia-Heng Tan, Tian-Miao Ou, Shi-Liang Huang, Ding Li, Lian-Quan Gu, Zhi-Shu Huang
JOURNAL OF MEDICINAL CHEMISTRY
(2016)
Article
Chemistry, Medicinal
Jie Dai, Zhen-Quan Liu, Xiao-Qin Wang, Jing Lin, Pei-Fen Yao, Shi-Liang Huang, Tian-Miao Ou, Jia-Heng Tan, Ding Li, Lian-Quan Gu, Zhi-Shu Huang
JOURNAL OF MEDICINAL CHEMISTRY
(2015)
Article
Chemistry, Medicinal
Chun-Li Xia, Ning Wang, Qian-Liang Guo, Zhen-Quan Liu, Jia-Qiang Wu, Shi-Liang Huang, Tian-Miao Ou, Jia-Heng Tan, Hong-Gen Wang, Ding Li, Zhi-Shu Huang
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2017)
Article
Chemistry, Multidisciplinary
Hua-Ting Xie, Du-Chao Zhou, Yan-Wen Mai, Lian Huo, Pei-Fen Yao, Shi-Liang Huang, Hong-Gen Wang, Zhi-Shu Huang, Lian-Quan Gu
Article
Biochemistry & Molecular Biology
Jinggong Liu, Jun Qiu, Mingxue Wang, Ling Wang, Lijuan Su, Jinbo Gao, Qiong Gu, Jun Xu, Shi-Liang Huang, Lian-Quan Gu, Zhi-Shu Huang, Ding Li
BIOCHIMICA ET BIOPHYSICA ACTA-GENERAL SUBJECTS
(2014)
Article
Biochemistry & Molecular Biology
Zeng Li, Bin Wang, Jin-Qiang Hou, Shi-Liang Huang, Tian-Miao Ou, Jia-Heng Tan, Lin-Kun An, Ding Li, Lian-Quan Gu, Zhi-Shu Huang
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2013)
Article
Biochemical Research Methods
Yan-Ping Li, Xiang Weng, Fang-Xian Ning, Jie-Bin Ou, Jin-Qiang Hou, Hai-Bin Luo, Ding Li, Zhi-Shu Huang, Shi-Liang Huang, Lian-Quan Gu
JOURNAL OF MOLECULAR GRAPHICS & MODELLING
(2013)
Article
Chemistry, Organic
Shi-Tian Zhuo, Chun-Yan Li, Ming-Hao Hu, Shuo-Bin Chen, Pei-Fen Yao, Shi-Liang Huang, Tian-Miao Ou, Jia-Heng Tan, Lin-Kun An, Ding Li, Lian-Quan Gu, Zhi-Shu Huang
ORGANIC & BIOMOLECULAR CHEMISTRY
(2013)
Article
Biochemistry & Molecular Biology
Jie-Bin Ou, Wei-Hao Huang, Xing-Zi Liu, Guo-Yao Dai, Lu Wang, Zhi-Shu Huang, Shi-Liang Huang
Summary: MSN8C, a novel catalytic inhibitor of human DNA topoisomerase II, has been found to induce tumor regression and differs from VP-16(etoposide). In vitro studies showed that MSN8C had significant antiproliferative activity against eleven human tumor cell lines, with particular efficacy against the Topo II-resistant HL-60/MX2 cell line. The resistance factor (RF) of MSN8C for Topo II in HL-60/MX2 versus HL-60 was 1.7, much lower than traditional Topo II poisons. In addition, MSN8C has shown promising antitumor efficacy and low toxicity in an A549 tumor xenograft model.
Article
Clinical Neurology
Peng Zhai, Chun-Li Xia, Jia-Heng Tan, Ding Li, Tian-Miao Ou, Shi-Liang Huang, Lian-Quan Gu, Zhi-Shu Huang
CURRENT ALZHEIMER RESEARCH
(2015)
Article
Chemistry, Medicinal
Shibin Zhao, Julian Maceren, Mia Chung, Samantha Stone, Raphael Geiben, Melissa L. Boby, Bradley S. Sherborne, Derek S. Tan
Summary: Antibiotic resistance is a major threat to public health, with Gram-negative bacteria presenting unique challenges due to their low permeability and efflux pumps. Limited understanding of the chemical rules for overcoming these barriers hinders antibacterial drug discovery. Efforts to address this issue, such as screening compound libraries and using cheminformatic analysis, have led to the design of sulfamidoadenosines with diverse substituents, showing potential utility in accumulation in Escherichia coli.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Jichun Li, Qing Li, Shuai Xia, Jiahuang Tu, Longbo Zheng, Qian Wang, Shibo Jiang, Chao Wang
Summary: This study successfully developed a short peptide mimetic as a MERS-CoV fusion inhibitor by reproducing the key recognition features of the HR2 helix. The resulting 23-mer lipopeptide showed comparable inhibitory effect to the 36-mer HR2 peptide HR2P-M2. This has important implications for developing short peptide-based antiviral agents to treat MERS-CoV infection.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Krista Jaunsleine, Linda Supe, Jana Spura, Sten van Beek, Anna Sandstrom, Jessica Olsen, Carina Halleskog, Tore Bengtsson, Ilga Mutule, Benjamin Pelcman
Summary: Beta(2)-adrenergic receptor agonists can stimulate glucose uptake by skeletal muscle cells and are therefore potential treatments for type 2 diabetes. The chirality of compounds has a significant impact on the activity of these agonists. This study found that certain synthesized compounds showed higher glucose uptake activity. These findings provide important information for the design of novel beta(2)AR agonists for T2D treatment.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Xin Xu, Jia Chen, Guan Wang, Xiaojuan Zhang, Qiang Li, Xiaobo Zhou, Fengying Guo, Min Li
Summary: The study focuses on EZH2, a promising therapeutic target for various types of cancers. Researchers designed and synthesized a series of novel derivatives aiming to enhance the EZH2 inhibition activity. Among them, compound 28 displayed potent EZH2 inhibition activity and showed high anti-proliferative effects in lymphoma cell lines and xenograft mouse models. The study suggests that compound 28 has potential as a therapeutic candidate for EZH2-associated cancers.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Wei Zhang, Wei Liu, Ya-Dong Zhao, Li-Zi Xing, Ji Xu, Rui-Jun Li, Yun-Xiao Zhang
Summary: This study developed a series of aromatic amide derivatives based on Rhein and investigated their inhibitory activity against alpha-Syn aggregation. Two of these compounds showed promising potential in treating Parkinson's disease by stabilizing alpha-Syn's conformation and disassembling alpha-Syn oligomers and fibrils.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Mani Sharma, S. S. S. S. Sudha Ambadipudi, Neeraj Kumar Chouhan, V. Lakshma Nayak, Srihari Pabbaraja, Sai Balaji Andugulapati, Ramakrishna Sistla
Summary: Therapeutically active lipids in drug delivery systems can enhance the safety and efficacy of treatment. The liposome formulation created using synthesized biologically active lipids showed additive anti-cancer effects and reduced tumorigenic potential.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
