Article
Chemistry, Medicinal
Yasheng Zhu, Xiuquan Ye, Hao Shen, Jiaxing Li, Zeyu Cai, Wenjian Min, Yi Hou, Haojie Dong, Yuxing Wu, Liping Wang, Xiao Wang, Yibei Xiao, Peng Yang
Summary: In this study, a novel EGFR inhibitor targeting Osimertinib resistance was identified by virtual screening and compound synthesis. The representative compound showed potent antitumor activity and good pharmacokinetic properties and oral bioavailability.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Hong-Yi Zhao, Xiao-Xiao Xi, Minhang Xin, San-Qi Zhang
Summary: The third-generation EGFR-TKIs have shown significant clinical achievements in NSCLC treatment, but acquired drug resistance remains a major limitation. The development of fourth-generation EGFR-TKIs targeting the triple mutant EGFR with C797S mutation has gained much attention. This review outlines the current panorama of fourth-generation EGFR-TKIs, focusing on their design strategy, binding mode, and antitumor activity. The challenges and prospects of fourth-generation EGFR-TKIs are also discussed.
BIOORGANIC CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Kshipra S. Karnik, Aniket P. Sarkate, Deepak K. Lokwani, Ishudeep S. Narula, Prasad V. L. S. Burra, Pravin S. Wakte
Summary: This study focused on mutations in EGFR enzyme related to non-small cell lung cancer, developing allosteric inhibitors to enhance EGFR binding affinity. Potential EGFR inhibitors were identified through virtual screening and molecular docking.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2021)
Review
Chemistry, Medicinal
Jie He, Zhihui Zhou, Xin Sun, Zunhua Yang, Pengwu Zheng, Shan Xu, Wufu Zhu
Summary: Epidermal growth factor receptor (EGFR) is a crucial target for treating non-small cell lung cancer (NSCLC), with first to third-generation inhibitors showing efficacy but leading to resistance after 9-15 months. Major breakthroughs in understanding the resistance mechanisms of third-generation inhibitors are still lacking. The fourth-generation EGFR-TKIs show promise in overcoming resistance.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Mingguang Zhang, Yang Yang, Yunyun Wang, Jia Wang, Hongyan Wu, Yongqiang Zhu
Summary: In this study, a class of 2-amine-4-oxyphosaniline pyrimidine derivatives were synthesized and evaluated as new noncovalent reversible EGFR inhibitors against L858R/T790M/C797S triple mutant. The most promising compound 7a showed excellent enzymatic inhibitory activity against CTL and effectively inhibited H1975-EGFR L858R/T790M/C797S in cell proliferation assays. Furthermore, compound 7a displayed good metabolic stabilities in liver microsomes and its putative binding mode with ATP was revealed by molecular docking study.
CHEMICAL & PHARMACEUTICAL BULLETIN
(2023)
Article
Chemistry, Medicinal
Li Xu, Bing Xu, Jianshe Wang, Yuan Gao, Xingrui He, Tian Xie, Xiang-Yang Ye
Summary: This paper summarizes the pharmacochemical processes and strategies for overcoming the resistance to Osimertinib caused by the EGFRC797S mutation in non-small cell lung cancer. It serves as a quick information provider for further structural modifications and drug discovery.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Yu-Ze Mao, Xiao-Xiao Xi, Hong-Yi Zhao, Yin-Liang Zhang, San-Qi Zhang
Summary: In order to overcome drug resistance caused by EGFR(C797S) mutation, a series of 2-aminopyrimidine derivatives were designed and synthesized as EGFR(C797S)-TKIs. Among these compounds, A5 and A13 showed significant anti-proliferative activity against the KC-0116 (EGFR(del19/T790M/C797S)) cell line with high selectivity. A5 inhibited EGFR phosphorylation, induced apoptosis, and arrested KC-0116 cells at G2/M phase. Molecular docking results showed that A5 and brigatinib bind to EGFR in a similar pattern.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2023)
Article
Pharmacology & Pharmacy
Jingjing Shi, Shaoyu Hao, Xiantao Liu, Yingying Li, Xin Zheng
Summary: This study found that Feiyiliu Mixture delays osimertinib resistance in EGFR-mutant cell lines and tumor-bearing mice by inhibiting PRC1/Wnt/EGFR pathway activation, reducing proliferation, and promoting apoptosis.
FRONTIERS IN PHARMACOLOGY
(2023)
Article
Pharmacology & Pharmacy
Geunho Choi, Daegeun Kim, Junehwan Oh
Summary: This study utilized artificial intelligence to discover potential drugs that can overcome acquired resistance in lung cancer patients, reducing the limitations of the current drug discovery process.
FRONTIERS IN PHARMACOLOGY
(2021)
Article
Chemistry, Medicinal
Jae Eun Jung, Yunseong Jang, Hee Jin Jeong, Sung Joon Kim, Kichul Park, Do Hee Oh, Ahran Yu, Chan Sun Park, Seo-Jung Han
Summary: This study discovered that 3,4-dihydropyrimido[4,5-d]pyrimidin-2(1H)-one and 3,4-dihydropyrido[2,3-d]pyrimidin-2(1H)-one derivatives are potent ENPP1 inhibitors with high microsomal stabilities.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2022)
Review
Chemistry, Multidisciplinary
Mostafa A. Mansour, Asmaa M. AboulMagd, Samar H. Abbas, Hamdy M. Abdel-Rahman, Mohamed Abdel-Aziz
Summary: Lung cancer is the second most common cause of morbidity and mortality among cancer types worldwide, with non-small cell lung cancer (NSCLC) representing the majority of most cases. EGFR TKIs are widely used as targeted therapy for NSCLC, but their efficacy is compromised by acquired mutations, including C797S. The development of next-generation EGFR TKIs that selectively inhibit EGFR triple mutations is of urgent medical need. This review discusses the design of fourth-generation EGFR TKIs, their binding interactions, clinical difficulties, and potential outcomes of treating patients with C797S mutation.
Article
Chemistry, Physical
Asmaa Aboelnaga, Sahar Soror, Ekhlass Nassar, Samia Elabbady, Asmaa M. Fahim
Summary: This study achieved the eco-friendly synthesis of novel bis heterocyclic compounds containing pyridine derivatives using green tools such as ultrasonication energy. The synthesized compounds were analyzed using spectroscopy and evaluated for their antitumor activity, showing promising results against breast and carcinoma cell lines. Molecular docking simulation and theoretical calculations further confirmed the experimental findings.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Biochemistry & Molecular Biology
Iqrar Ahmad, Matin Shaikh, Sanjay Surana, Arabinda Ghosh, Harun Patel
Summary: Third-generation EGFR inhibitors like Osimertinib selectively target EGFR-T790M mutant and have good selectivity for wild-type EGFR. However, after treatment with Osimertinib, a C797S mutation may occur, rendering the tumor undruggable. Recently, trisubstituted imidazoles based on p38 alpha MAPK inhibitors have been developed as fourth-generation EGFR-TKIs to overcome C797S resistance.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2022)
Article
Biochemistry & Molecular Biology
Minnelli Cristina, Laudadio Emiliano, Sorci Leonardo, Sabbatini Giulia, Galeazzi Roberta, Amici Adolfo, Semrau S. Marta, Storici Paola, Rinaldi Samuele, Stipa Pierluigi, Marcaccio Massimo, Mobbili Giovanna
Summary: Inhibition of EGFR is a promising strategy for NSCLC therapy. The C797S mutation causes resistance to osimertinib in EGFR mutants. This study identifies a novel mutant-selective core and discovers compounds that inhibit the phosphorylation of EGFR mutants, providing insights into overcoming resistance mechanisms.
BIOORGANIC CHEMISTRY
(2022)
Review
Chemistry, Medicinal
Asmaa E. Kassab
Summary: The pyrazolo[3,4-d]pyrimidine core is a promising framework for drug design and discovery, mimicking kinase active site hinge region binding contacts. It has a wide range of pharmacological and biological value, particularly as an anticancer agent. This review summarizes the main synthetic routes of pyrazolo[3,4-d]pyrimidines and their recent developments as inhibitors of endothelial growth factor receptors and vascular endothelial growth factor receptors, aiming to guide the design and synthesis of novel pyrazolo[3,4-d]pyrimidine derivatives for clinical use in cancer treatment.
ARCHIV DER PHARMAZIE
(2023)
Retraction
Chemistry, Multidisciplinary
Fengfeng Xiao, Bing Cao, Congyu Wang, Xujuan Guo, Mengge Li, Da Xing, Xianglong Hu
Article
Nanoscience & Nanotechnology
Qiubo Hao, Zhixiong Wang, Wei Zhao, Liewei Wen, Wenhui Wang, Siyu Lu, Da Xing, Meixiao Zhan, Xianglong Hu
ACS APPLIED MATERIALS & INTERFACES
(2020)
Article
Chemistry, Physical
Congyu Wang, Wei Zhao, Bing Cao, Zhixiong Wang, Qi Zhou, Siyu Lu, Ligong Lu, Meixiao Zhan, Xianglong Hu
CHEMISTRY OF MATERIALS
(2020)
Article
Materials Science, Ceramics
Xin Yang, Xianglong Hu, Zhean Su, Anhong Shi, Yuanqi Weng, Qizhong Huang
JOURNAL OF ASIAN CERAMIC SOCIETIES
(2020)
Article
Chemistry, Multidisciplinary
Zhixiong Wang, Meixiao Zhan, Weijie Li, Chengyan Chu, Da Xing, Siyu Lu, Xianglong Hu
Summary: The study introduces a photosensitizer-free system that can achieve controlled release of NO in cancer cells, inducing apoptosis. Through photoacoustic technology, the release of nanocapsules and the production of highly cytotoxic peroxynitrite were achieved.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2021)
Article
Engineering, Biomedical
Bing Cao, Xiaoming Lyu, Congyu Wang, Siyu Lu, Da Xing, Xianglong Hu
Article
Engineering, Environmental
Yongbo Zhang, Xu He, Yongteng Zhang, Yanping Zhao, Siyu Lu, Yongjun Peng, Ligong Lu, Xianglong Hu, Meixiao Zhan
Summary: This study introduces a novel immunomodulator nanoparticle that targets tumor cell mitochondria, combined with photothermal therapy and immune checkpoint blockade to enhance antitumor immune response, effectively suppressing tumor recurrence and metastasis.
CHEMICAL ENGINEERING JOURNAL
(2021)
Article
Engineering, Multidisciplinary
Xianglong Hu, Min Huang, Nizao Kong, Fei Han, Ruixuan Tan, Qizhong Huang
Summary: Coating SiC ceramic layer on mesophase pitch-based carbon fibers surface can improve thermal conductivity and electrical insulation, offering a new approach for thermal conductive fillers in electronic packaging.
COMPOSITES PART B-ENGINEERING
(2021)
Article
Polymer Science
Minglong Chen, Xianglong Hu, Shiyong Liu
Summary: Vaccination is a promising method to prevent serious diseases, but the limitations of mRNA vaccines require further research for optimization.
MACROMOLECULAR CHEMISTRY AND PHYSICS
(2022)
Article
Polymer Science
Wenjia Zhang, Xiaoming Lyu, Li Zhang, Wenhui Wang, Qi Shen, Siyu Lu, Ligong Lu, Meixiao Zhan, Xianglong Hu
Summary: This study presents a label-free polyprodrug strategy to formulate doxorubicin nanoparticles, which can take advantage of the photophysical properties of the drug and achieve precise photothermal-chemotherapy.
MACROMOLECULAR RAPID COMMUNICATIONS
(2022)
Article
Chemistry, Multidisciplinary
Qi Zhou, Xiaoming Lyu, Bing Cao, Xueping Liu, Jing Liu, Jiarui Zhao, Siyu Lu, Meixiao Zhan, Xianglong Hu
Summary: Pathogenic microorganisms pose challenges to public health, requiring fast staining and efficient treatment. This study successfully achieved fast imaging and photodynamic treatment of various typical pathogens using a water-soluble AIE-active photosensitizer TPA-PyOH.
FRONTIERS IN CHEMISTRY
(2021)
Article
Biotechnology & Applied Microbiology
Zishuai An, Bing Cao, Junzhe Zhang, Baihong Zhang, Chengqian Zhou, Xianglong Hu, Wenli Chen
Summary: Nanomaterials have been widely studied for their potential to become the new generation of nanocarriers in gene transfection. This study focuses on the application of Poly (2-(N,N-dimethylamino) ethyl methacrylate) (PDMAEMA) as a gene carrier in plant cells. The results show that PDMAEMA has the ability to efficiently deliver DNA in plant cells with lower cytotoxicity compared to polyethylenimine (PEI). This work provides new ideas and more effective methods for plant transformation.
FRONTIERS IN BIOENGINEERING AND BIOTECHNOLOGY
(2022)
Article
Chemistry, Multidisciplinary
Zhixiong Wang, Meixiao Zhan, Xianglong Hu
Summary: Pulsed laser can generate the photoacoustic effect, which is widely used for disease diagnosis with excellent contrast, high penetrability, and sensitivity. Increasing the energy of pulsed laser can promote drug release, enhance therapeutic efficacy, and produce reactive species.
CHEMISTRY-A EUROPEAN JOURNAL
(2022)
Article
Polymer Science
Qiang-Qiang Shi, Xin Zhou, Jie Xu, Ning Wang, Jia-Lin Zhang, Xiang-Long Hu, Shi-Yong Liu
Summary: Compared with spherical micelles, rod/worm-like micelles have extended blood circulation duration and exhibit favorable cellular uptake behavior. The controllable fabrication of narrowly dispersed nanorods in aqueous media is challenging. A methodology of thermal annealing was developed for the fabrication of helical nanorods and a series of nanorods with different lengths. In addition, supramolecular self-assembly by amphiphilic dendritic oligourethane readily fabricated diverse uniform nanorods in aqueous media.
CHINESE JOURNAL OF POLYMER SCIENCE
(2023)
Article
Optics
Li Shichin, Wang Xu, Zhang Penghui, Xin Wenhui, Hua DengXin, Hu Xianglong, Song Yuehui
Summary: In this study, a multichannel pure rotational Raman lidar spectroscopic system is proposed and designed to accurately measure atmospheric temperature profiles using the pure rotational Raman spectroscopy technique. The system effectively filters out background noise by using FPI and low-order diffraction gratings, and successfully achieves absolute detection of atmospheric temperature profiles.
CHINESE JOURNAL OF LASERS-ZHONGGUO JIGUANG
(2022)
Article
Chemistry, Multidisciplinary
Qian Wu, Yubo Cui, Guifeng Xia, Jinlong Yang, Shuming Du, Xinhong Xiong, Li Yang, Dong Xu, Xu Deng, Jiaxi Cui
Summary: Passive daytime radiative cooling (PDRC) technology, while promising for global spacing cooling, faces limitations in practical application due to reduced cooling effectiveness caused by wear and dirt contamination. Researchers have developed a renewable armor structure using fluorinated hollow glass microspheres to enhance the anti-fouling and cooling properties of PDRC coatings. The coatings exhibit high solar reflectance and thermal emittance, leading to significant temperature reduction below ambient temperature.
CHINESE CHEMICAL LETTERS
(2024)
Article
Chemistry, Multidisciplinary
Qiang Bei, Bei Zhang, Kaifeng Wang, Shiming Zhang, Guichuan Xing, Clement Cabanetos
Summary: The power conversion efficiency (PCE) of organic solar cells (OSCs) has reached 20% in recent years, thanks to the advantages of organic photoactive materials. Benzothiadiazole (BT) has attracted significant research attention as a building block of OSCs. OSCs based on BT structure have shown diversity, and the increasing PCE values indicate a promising future for OSCs. This review analyzes the progress made in the last decades, focusing on effective BT small-molecules and BT polymers for OSCs. The structure-property relationships, donor-acceptor matching criteria, and morphology control approaches are discussed. The remaining challenges and a personal perspective on the future advancement of OSCs are summarized.
CHINESE CHEMICAL LETTERS
(2024)
Article
Chemistry, Multidisciplinary
Rong He, Dandan Tang, Ningge Xu, Heng Liu, Kun Dou, Xuejun Zhou, Fabiao Yu
Summary: Nasopharyngeal carcinoma (NPC) is a common malignant tumor of the head and neck, with a high incidence in China and Southeast Asian countries. In this study, a novel near-infrared fluorescent probe, SNAFL-GSH, was designed and synthesized for the detection of glutathione (GSH). The probe showed selective detection of GSH and the ability to distinguish normal and cancer cells. It has great potential for application in the diagnosis and evaluation of NPC.
CHINESE CHEMICAL LETTERS
(2024)
Article
Chemistry, Multidisciplinary
Zhukang Guo, Baijiang Jin, Yile Fang, Lian Jin, Song Li, Yan Deng, Zhu Chen, Hui Chen, Yuanying Zhang, Rabia Usman, Nongyue He
Summary: This study isolated primary cells that can be stably passaged from spontaneous tumors of genetically engineered pancreatic ductal adenocarcinoma model mice and used an autonomously developed automated screening instrument for efficient nucleic acid aptamer screening. The obtained aptamers were affinity verified at the cellular level. The study also investigated the impact of cell growth environment difference on the recognition ability of aptamers and confirmed the targeting ability and drug loading ability of the aptamer.
CHINESE CHEMICAL LETTERS
(2024)
Article
Chemistry, Multidisciplinary
Zhongshan Yang, Qiqi Zhang, Hui Song, Xin Chen, Jiwei Cui, Yanhui Sun, Lequan Liu, Jinhua Ye
Summary: Methane chemistry is a significant area of research in catalysis. Converting methane into value-added chemicals is desirable but challenging due to its high C-H bonding energy and lack of pi bonding or unpaired electrons. Photocatalytic partial oxidation of methane to liquid oxygenates is a promising technology for achieving high efficiency and selectivity under mild conditions. The choice and activation of oxidants are crucial for its performance.
CHINESE CHEMICAL LETTERS
(2024)
Article
Chemistry, Multidisciplinary
Peng Shan, Jing Liao, Jiayi Li, Chengyan Wang, Jie Zhou, Linqiang Mei, Yunlu Dai, Qiang Wang, Wenyan Yin
Summary: This study reports an oral radioprotectant Gel@GYY that combines a gelatin-based hydrogel and a pH-responsive hydrogen sulfide donor. Gel@GYY has excellent adhesion and sustained release properties, allowing it to release H2S in the gastrointestinal tract and effectively scavenge free radicals induced by radiation. It also reduces inflammation and has biodegradable properties.
CHINESE CHEMICAL LETTERS
(2024)
Article
Chemistry, Multidisciplinary
Lu Liu, Ziyi Liu, Jingnan Cui, Guiling Ning, Weitao Gong
Summary: The development of new metal-free heterogeneous catalysts has been the subject of extensive research. In this study, a new Troger's base (TB)-derived porous organic polymer (POPs) was designed and prepared by integrating multifunctional monomers. The resulting polymer, which combines the advantages of pillar[5]arene macrocycle and TB moiety, exhibited enhanced catalytic performance in Knoevenagel condensation and CO2 conversion, serving as an effective metal-free catalyst. This work provides a new strategy for fabricating metal-free heterogeneous catalysts based on macrocyclic POPs.
CHINESE CHEMICAL LETTERS
(2024)
Article
Chemistry, Multidisciplinary
Leyong Zhou, Changyin Yang, Weitao Dou, Tongxia Jin, Haibo Yang, Lin Xu
Summary: This review summarizes the application of micro/nanofluidic techniques in constructing supramolecular assemblies of different scales, and highlights the advantages of these techniques over conventional synthesis methods. Furthermore, it emphasizes the potential of micro/nanofluidic systems in improving our understanding of supramolecular self-assembly processes.
CHINESE CHEMICAL LETTERS
(2024)
Article
Chemistry, Multidisciplinary
Yanchao Jin, Suixiaochen Chen, Peiwen Huang, Xiongjian Chen, Chun-Yan Lin, Li-Ping Li, Xiao Chen, Rui Ding, Jianxi Liu, Riyao Chen
Summary: In this study, magnesium and coconut shell carbon were used to disinfect water by adsorbing copper(II) and converting dissolved oxygen to hydrogen peroxide through Mg corrosion. The copper was enriched on the carbon surface and efficiently catalyzed the hydrogen peroxide to inactivate E.coli. The process showed promising disinfection performance both in laboratory experiments and real wastewater treatment.
CHINESE CHEMICAL LETTERS
(2024)
Article
Chemistry, Multidisciplinary
Haihong Lai, Zehong Chen, Hao Zhuo, Yijie Hu, Xuan Zhao, Jiwang Yi, Hongzhi Zheng, Ge Shi, Yifan Tong, Ling Meng, Xinwen Peng, Linxin Zhong
Summary: By altering the pyrolysis route of cellulose nanofiber, the structural defects of carbon aerogels can be reduced, leading to improved compressibility and stress retention, as well as higher stress sensor sensitivity and temperature coefficient.
CHINESE CHEMICAL LETTERS
(2024)
Article
Chemistry, Multidisciplinary
Lina Guo, Jinsong Ding, Wenhu Zhou
Summary: Bacteria-based tumor therapy has resurfaced due to the revolution of tumor immunotherapy, offering unique solutions for traditional tumor treatments. Bacteria with active tropism can selectively colonize tumor sites and suppress tumor growth through various mechanisms, making them attractive tools for tumor treatment. This critical review introduces recent advances in bacteria-based tumor therapy, including bacterial properties, their benefits for tumor therapy, anti-tumor mechanisms, challenges, and future perspectives.
CHINESE CHEMICAL LETTERS
(2024)
Article
Chemistry, Multidisciplinary
Lan Liang, Chuanbin Wang, Xukai Lu, Yunan Sun, Beibei Yan, Ning Li, Guanyi Chen, Li'an Hou
Summary: This study investigates the interactions between phenol and benzaldehyde in the ECH process through experiments and theoretical calculations. The results show that phenol can accelerate the conversion of benzaldehyde, while benzaldehyde inhibits the conversion of phenol. The research provides a theoretical basis for the application of ECH in practical bio-oil upgrading.
CHINESE CHEMICAL LETTERS
(2024)
Article
Chemistry, Multidisciplinary
Pengcheng Fan, Yuhao He, Junan Pan, Ning Sun, Qiyu Zhang, Chen Gu, Kang Chen, Weinan Yin, Longlu Wang
Summary: This study focuses on the recent progress in hydrogen evolution reaction (HER) based on photothermal effect. It introduces the main pathways of photothermal conversions applied in H2 evolution, summarizes the functions of the photothermal effect, and presents a method to improve the catalytic system through thermal means. The study also discusses the challenges and outlook in this promising area.
CHINESE CHEMICAL LETTERS
(2024)
Article
Chemistry, Multidisciplinary
Leiduo Lai, Hongyu Zhou, Yichen Hong, Mengfan Luo, Yang Shi, Heng Zhang, Zhaokun Xiong, Gang Yao, Bo Lai
Summary: In this study, a facile ammonia reduction strategy was proposed and a novel FeVO3-x catalyst was synthesized for the activation of peroxymonosulfate (PMS) to degrade the pharmaceutical carbamazepine (CBZ). The results showed that the system could rapidly degrade CBZ and generate various active species involved in the degradation process.
CHINESE CHEMICAL LETTERS
(2024)
Article
Chemistry, Multidisciplinary
Tangxin Xiao, Xiuxiu Li, Liangliang Zhang, Kai Diao, Zheng-Yi Li, Xiao-Qiang Sun, Leyong Wang
Summary: This study presents the construction of a supramolecular light harvesting system based on sequential energy transfer. The system demonstrates tunable fluorescence emission through self-assembly of polymers into nanoparticles, achieving efficient two-step light harvesting.
CHINESE CHEMICAL LETTERS
(2024)