Article
Pharmacology & Pharmacy
Hua-Tao Wu, Chun-Lan Li, Ze-Xuan Fang, Wen-Jia Chen, Wen-Ting Lin, Jing Liu
Summary: Triple-negative breast cancer (TNBC) is an aggressive type of breast carcinoma with a high risk of metastasis/relapse and cancer-related death. This study investigated the potential utilization of the mTOR signaling pathway for TNBC treatment by targeting it with itraconazole (ITZ) combined with rapamycin. The results showed that the combination of ITZ and rapamycin synergistically inhibited proliferation and motility of TNBC cells, but did not enhance apoptosis. It was observed that ITZ and/or rapamycin arrested cells in G0/G1 phase and prevented G1/S phase transition. The reduced levels of cyclin D1 protein were consistent with G0/G1 phase arrest, especially when combined with rapamycin.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Oncology
Olivia K. Provance, Eric S. Geanes, Asona J. Lui, Anuradha Roy, Sean M. Holloran, Sumedha Gunewardena, Christy R. Hagan, Scott Weir, Joan Lewis-Wambi
Summary: Overexpression of IFITM1 in TNBC promotes tumor progression, but targeting IFITM1 can inhibit cell proliferation and invasion through the NF-kappa B signaling pathway. Parthenolide, identified as an NF kappa B inhibitor, shows potential as a cytotoxic agent for TNBC treatment.
Article
Chemistry, Medicinal
Jian-Jia Liang, Wu-Lin Yu, Liang Yang, Kong-Ming Qin, Yu-Ping Yin, Dan Li, Yuan-Hao Ni, Jing-Jing Yan, Yin-Xian Zhong, Zi-Xin Deng, Kui Hong
Summary: A series of novel derivatives with modification on C24 of MHO7 were synthesized, and compound 4m showed promising antitumor activity against TNBC. It induced apoptosis through the mitochondria pathway and caused cell cycle arrest. In addition, 4m affected the expression of key proteins and inhibited cell metastasis. These findings suggest that modifying C24 of MHO7 is a potential approach for developing new anti-TNBC agents.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Oncology
Daniel Wilhelm Olivier, Etheresia Pretorius, Anna-Mart Engelbrecht
Summary: This study investigated the role of SAA1 in TNBC, focusing on cell cycle regulation, apoptosis, survival signaling, metabolism, and metastasis. Knockdown of SAA1 had varying effects in different cell types, with potential for therapeutic targeting in TNBC.
EXPERIMENTAL CELL RESEARCH
(2021)
Article
Biochemistry & Molecular Biology
Xiaoyan Jiang, Xu Zhi, Peixia Zhang, Zhongmei Zhou, Jinxiang Ye, Yu Gao, Xinye Wang, Chuanyu Yang, Haijun Chen, Rong Liu, Ceshi Chen
Summary: The study identified that the isochromanoindolenine derivative FZU-0025-065 inhibits TNBC by suppressing the AKT signaling pathway, showing potential for TNBC treatment.
INTERNATIONAL JOURNAL OF BIOLOGICAL SCIENCES
(2021)
Article
Plant Sciences
Francis Adu-Amankwaah, Kudzanai Ian Tapfuma, Raeesa Hoosen Hussan, Ndivhuwo Tshililo, Lucinda Baatjies, Maano Valerie Masiphephethu, Lawrence Mabasa, Vuyo Mavumengwana
Summary: Breast cancer is a leading cause of cancer-related deaths in women globally. This study investigated the potential use of nine Fynbos plants in treating breast cancer and found that E. racemosa and S. africana-lutea are promising candidates for further development of therapeutic agents.
SOUTH AFRICAN JOURNAL OF BOTANY
(2022)
Article
Multidisciplinary Sciences
Shijie Wei, Yubao Zhang, Xiaoran Ma, Yan Yao, Qinqin Zhou, Wenfeng Zhang, Chao Zhou, Jing Zhuang
Summary: This study reveals that matrine, an alkaloid from the medicinal plant Sophora flavescens, has strong anticancer effects and can be explored as a new therapeutic agent for triple-negative breast cancer (TNBC). Through bioinformatics analysis and network pharmacology, researchers found that matrine inhibits the PI3K/AKT pathway, suppresses cell proliferation and invasion, induces apoptosis and autophagy, effectively inhibiting the growth and spread of TNBC.
SCIENTIFIC REPORTS
(2023)
Article
Biochemistry & Molecular Biology
Shade' A. Ahmed, Patricia Mendonca, Samia S. Messeha, Karam F. A. Soliman
Summary: This study demonstrates that fucoxanthin has anticancer effects in triple-negative breast cancer cells, with a stronger effect in MDA-MB-231 cells. Fucoxanthin targets VEGF-A and VEGF-C, inhibits cell proliferation and migration, and induces cell cycle arrest and apoptosis.
Article
Biochemistry & Molecular Biology
Mohd Shuaib, Shashank Kumar
Summary: Triple-negative breast cancer (TNBC) is a highly aggressive subtype of breast cancer with relatively unknown pathogenesis. In this study, the researchers investigated the tumor-suppressive role of microRNA (miR)-1250-5p in TNBC cells through various experiments. They found that increased expression of miR-1250-5p in TNBC cells led to decreased cell viability, inhibited G1/S phase transition, induced apoptosis, and reduced epithelial-mesenchymal transition. The results suggest that miR-1250-5p could be a potential therapeutic target for TNBC treatment.
JOURNAL OF CELLULAR BIOCHEMISTRY
(2023)
Article
Oncology
Hetakshi Kurani, Seyedeh Fatemeh Razavipour, Kuzhuvelil B. Harikumar, Matthew Dunworth, Andrew J. Ewald, Apsra Nasir, Gray Pearson, Derek Van Booven, Zhiqun Zhou, Diana Azzam, Claes Wahlestedt, Joyce Slingerland
Summary: This study identified DOT1L as a key regulator of cancer stem cells (CSCs) in triple-negative breast cancer (TNBC). Inhibition of DOT1L suppressed the growth and metastasis of TNBC CSCs, suggesting that DOT1L inhibitors may be a potential therapeutic option for targeting stem cell-enriched TNBC.
CLINICAL CANCER RESEARCH
(2022)
Article
Multidisciplinary Sciences
Abdul S. Qadir, Jean Philippe Guegan, Christophe Ginestier, Assia Chaibi, Alban Bessede, Emmanuelle Charafe-Jauffret, Manon Macario, Vincent Lavoue, Thibault de la Motte Rouge, Calvin Law, Jacob Vilker, Hongbin Wang, Emily Stroup, Matthew J. Schipma, Bryan Bridgeman, Andrea E. Murmann, Zhe Ji, Patrick Legembre, Marcus E. Peter
Summary: The apoptosis inducing receptor CD95/Fas has tumorigenic activities and its expression in tumor cells can suppress NK cell immunity, providing a new target for immune therapy.
Article
Biochemistry & Molecular Biology
Shirley A. R. Sancha, Adriana Gomes, Joana B. Loureiro, Lucilia Saraiva, Maria Jose U. Ferreira
Summary: In this study, phytochemical analysis of Pancratium maritimum revealed the presence of various Amaryllidaceae alkaloids, which exhibited significant growth inhibitory effects against breast cancer cell lines, including triple-negative breast cancer. Among the isolated compounds, the homolycorine-type alkaloid 7 showed promising anti-proliferative activity through induction of apoptosis, modulation of mitochondrial reactive oxygen species, and G2/M cell cycle arrest. Furthermore, compound 7 exhibited synergistic effects when combined with conventional chemotherapeutic drugs.
Article
Nanoscience & Nanotechnology
Lizhen Zhan, Cairong Xiao, Changhao Li, Jinxia Zhai, Fabang Yang, Jinhua Piao, Chengyun NIng, Zhengnan Zhou, Peng Yu, Suijian Qi
Summary: This study demonstrates the inhibitory effects of internal wireless electric stimulation (ES) based on piezoelectric nanoparticles on the proliferation and migration of triple-negative breast cancer (TNBC) cells. Three different barium titanate nanoparticles (BTNPs) with different crystal phases and piezoelectric properties were studied, and varying intensities of internal ES were generated. In vitro and in vivo experiments showed that internal ES from BTNPs significantly reduced the proliferative potential of cancer cells, inhibited cell growth and migration, and resisted tumor growth and metastasis. The results suggest a promising noninvasive therapeutic strategy for TNBC with minimal side effects.
ACS APPLIED MATERIALS & INTERFACES
(2022)
Article
Cell Biology
Mengna Zhang, Lingxian Zhang, Ajun Geng, Xiao Li, Yu Zhou, Liming Xu, Yi Arial Zeng, Jinpeng Li, Cheguo Cai
Summary: In this study, the researchers investigated the function of cyclin-dependent kinase 14 (CDK14) in mammary development and breast cancer progression. The results showed that CDK14 is expressed in mammary basal cells and elevated in triple negative breast cancer (TNBC). CDK14 knockdown or inhibition was found to suppress mammary regeneration and the progression of TNBC.
Article
Pharmacology & Pharmacy
Leide Laura Figueiredo Maciel, Marina Barreto Silva, Rafaela Oliveira Moreira, Ana Paula Cardoso, Christiane Fernandes, Adolfo Horn Jr, Joao Carlos de Aquino Almeida, Milton Masahiko Kanashiro
Summary: This study investigated the antineoplastic activity of two platinum complexes containing alpha- and beta-naphthyl groups. The results showed that one of the platinum complexes exhibited higher cytotoxicity against all cancer cell lines tested and lower cytotoxicity against normal peripheral blood mononuclear cells. Further investigations revealed that this complex induced cell death by apoptosis and was associated with mitochondrial membrane depolarization, elevated levels of reactive oxygen species (ROS), and caspase activation.
Article
Chemistry, Medicinal
Mengmeng Wang, Puneet Srivastava, Chao Liu, Robert Snoeck, Graciela Andrei, Steven De Jonghe, Piet Herdewijn
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2018)
Article
Chemistry, Analytical
Su-Xiang Feng, Xian-He Li, Meng-Meng Wang, Rui Hao, Meng-Meng Li, Lei Zhang, Zhe Wang
JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
(2018)
Article
Biochemistry & Molecular Biology
Weizhi Ge, Zhongquan Liu, Yu Sun, Tianpeng Wang, Hongyu Guo, Xinyi Chen, Shengzu Li, Mengmeng Wang, Yue Chen, Yahui Ding, Quan Zhang
BIOORGANIC CHEMISTRY
(2019)
Article
Biochemistry & Molecular Biology
Yao-Yun Fan, Vahid Farrokhi, Teresa Caiazzo, Mengmeng Wang, Denise M. O'Hara, Hendrik Neubert
Article
Chemistry, Medicinal
Yahui Ding, Shengzu Li, Weizhi Ge, Zhongquan Liu, Xuhai Zhang, Mengmeng Wang, Tianyang Chen, Yue Chen, Quan Zhang
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2019)
Article
Medicine, Research & Experimental
Yingying Ke, Mengmeng Wang, Yage Li, Zengfu Shan, Wangyang Mi, Peipei Yuan, Weisheng Feng, Xiaoke Zheng
BIOMEDICINE & PHARMACOTHERAPY
(2020)
Article
Pharmacology & Pharmacy
Mengmeng Wang, Zhuqing Liu, Shoushan Hu, Xianchun Duan, Yanyan Zhang, Can Peng, Daiyin Peng, Lan Han
FRONTIERS IN PHARMACOLOGY
(2020)
Article
Medicine, Research & Experimental
Mengmeng Wang, Bingdi Cui, Man Gong, Qiuyan Liu, Xingxu Zhuo, Jiangnan Lv, Lianhe Yang, Xiaoqian Liu, Zhimin Wang, Liping Dai
Summary: Arctium lappa leaves attenuate AS-induced cholesterol accumulation by regulating the AMPK-mediated PPARG/LXR alpha pathway and promoting cholesterol efflux.
BIOMEDICINE & PHARMACOTHERAPY
(2022)
Article
Pharmacology & Pharmacy
Zihan Guo, Yunlan Ding, Mengmeng Wang, Jiyong Liu, Qing Zhai, Qiong Du
Summary: This study investigated the safety profile of trastuzumab deruxtecan using various medical data sources. The results showed that trastuzumab deruxtecan was well tolerated, but attention should be paid to interstitial lung disease and decreased ejection fraction.
JOURNAL OF CLINICAL PHARMACY AND THERAPEUTICS
(2022)
Article
Pharmacology & Pharmacy
Yifang Wu, Mengmeng Wang, Yufan Li, Hongmei Xia, Yongfeng Cheng, Chang Liu, Ying Xia, Yu Wang, Yan Yue, Xiaoman Cheng, Zili Xie
Summary: Formulating docetaxel (DTX) in a slow-release emulsion with good stability prepared through self-assembly and high-speed electric stirring presents challenges but promising results in terms of controlled release. The addition of DTX in different phases of the emulsion affects its in vitro release rates and demonstrates antioxidant potential.
Article
Pharmacology & Pharmacy
Shuohan Huang, Zihan Guo, Mengmeng Wang, Youjun She, Xuan Ye, Qing Zhai, Jiyong Liu, Qiong Du
Summary: This study analyzed data from the FDA Adverse Event Reporting System and found that BRAF and MEK inhibitor combination therapy is associated with an increased risk of ocular adverse events. Multiple ocular adverse events were identified, including some unexpected ones, and differences in the profiles of these events were found among different combination therapies.
EXPERT OPINION ON DRUG SAFETY
(2023)
Article
Chemistry, Medicinal
Mengmeng Wang, Yingying Ke, Yangyang Wang, Tong Liu, Yage Li, Zengfu Shan, Wangyang Mi, Ning Zhou, Weisheng Feng, Xiaoke Zheng
Summary: The study found that Rehmanniae Radix Praeparata (PRR) may help in improving metabolic function in rats with cold syndrome by activating the AMPK signaling pathway. Further research is needed to understand the heat-warming properties of PRR.
PHARMACOGNOSY MAGAZINE
(2021)
Article
Pharmacology & Pharmacy
Jie Huang, Ronghuan Yu, Qiong Wang, Hongqun Chen, Bin Hu, Mengmeng Wang, Junjie Mao, Baoqing Wang
Summary: Metagenomics next generation sequencing of alveolar lavage fluid can improve the early detection rate of pathogens, achieve accurate and individualized treatment, shorten the length of hospital stay, and reduce mortality for patients with unexplained pulmonary infection.
INDIAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2021)
Article
Integrative & Complementary Medicine
Chen Fang-Fang, Wang Meng-Meng, Xia Wen-Wen, Peng Dai-Yin, Han Lan
CHINESE JOURNAL OF NATURAL MEDICINES
(2020)
Article
Chemistry, Medicinal
Shuang Mei, Su Jiang, Yuting Wang, Han Jing, Peng Yang, Miao-Miao Niu, Jindong Li, Kai Yuan, Yan Zhang
Summary: This study identifies a dual-targeting peptide, AP-1, that effectively inhibits variants of concern (VOCs) of SARS-CoV-2 without impairing host cell viability. The findings suggest that AP-1 could be a promising broad-spectrum agent for treating emerging VOCs of SARS-CoV-2.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Hyeonjun Lee, Ju Yeon Lee, Hyunsoo Jang, Hye Young Cho, Minhee Kang, Sang Hyun Bae, Suin Kim, Eunji Kim, Jaebong Jang, Jin Young Kim, Young Ho Jeon
Summary: By using liquid chromatography-tandem mass spectrometry and nuclear magnetic resonance experiments, we identified new chemical moieties that bind to the target sites of the protein of interest, allowing for reversible binding and protein degradation. This method has the potential to expand the application of PROTAC technology.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Yingying Li, Xiyou Du, Xinru Kong, Yuelin Fang, Zhijing He, Dongzhu Liu, Hang Wu, Jianbo Ji, Xiaoye Yang, Lei Ye, Guangxi Zhai
Summary: This study proposes a novel nanoplatform based on the autophagy cascade to overcome the obstacles in chemo-immunotherapy. The platform combines chemotherapy and starvation therapy to initiate pro-death autophagy and enhance antigen presentation, while also remodeling the immunosuppressive tumor microenvironment. Furthermore, the study discovers a new therapeutic direction for the respiration inhibitor 3-bromopyruvic acid (3BP) in cancer treatment. Overall, this study offers an opportunity to improve antitumor efficacy and boost immune responses.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Bingsi Wang, Mingxu Ma, Yusen Dai, Pengfei Yu, Liang Ye, Wenyan Wang, Chunjie Sha, Huijie Yang, Yingjie Yang, Yunjing Zhu, Lin Dong, Shujuan Wei, Linlin Wang, Jingwei Tian, Hongbo Wang
Summary: Breast cancer is a common malignant tumor in women, and drug resistance remains a clinical challenge. In this study, a novel compound, G-5b, was developed with potent antagonistic and degradation activities comparable to the current drug fulvestrant. G-5b also showed improved stability and solubility. Mechanistically, G-5b engages the proteasome pathway to degrade ER, inhibiting the ER signaling pathway and inducing apoptosis and cell cycle arrest. In animal models, G-5b exhibited superior pharmacokinetics and pharmacodynamics properties. Overall, G-5b is a promising long-acting SERD worthy of further investigation and optimization.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Karoline B. Waitman, Larissa C. de Almeida, Marina C. Primi, Jorge A. E. G. Carlos, Claudia Ruiz, Thales Kronenberger, Stefan Laufer, Marcia Ines Goettert, Antti Poso, Sandra V. Vassiliades, Vinicius A. M. de Souza, Monica F. Z. J. Toledo, Neuza M. A. Hassimotto, Michael D. Cameron, Thomas D. Bannister, Leticia Costa-Lotufo, Joa o A. Machado-Neto, Mauricio T. Tavares, Roberto Parise-Filho
Summary: A series of hybrid inhibitors combining pharmacophores of known kinase inhibitors and benzohydroxamate HDAC inhibitors were synthesized and evaluated for their anticancer activity and pharmacokinetic properties. Compounds 4d-f exhibited promising cytotoxicity against hematological cells and moderate activity against solid tumor models. Compound 4d showed potent inhibition of multiple kinase targets and had stable interactions with HDAC and members of the JAK family. These compounds showed selective cytotoxicity with minimal effects on non-tumorigenic cells and favorable pharmacokinetic profiles.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Michal Sulik, Diana Fontinha, Dietmar Steverding, Szymon Sobczak, Michal Antoszczak, Miguel Prudencio, Adam Huczynski
Summary: This study describes the synthesis of the first-in-class ivermectin derivatives obtained through derivatization of the C13 position, along with the unexpected rearrangement of the macrolide ring. These derivatives show potential for antiparasitic activity and are important for the development of new antiparasitic agents.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Jun Liu, Qiu-Xian Chen, Wen-Fu Wu, Dong Wang, Si -Yu Zhao, Jia-Hao Li, Yi-Qun Chang, Shao-Gao Zeng, Jia-Yi Hu, Yu-Jie Li, Jia-Xin Du, Shu-Meng Jiao, Hai-Chuan Xiao, Qiang Zhang, Jun Xu, Jian-Fu Zhao, Hai -Bo Zhou, Yong-Heng Wang, Jian Zou, Ping-Hua Sun
Summary: A new anti-infective drug strategy has been discovered to attenuate virulence and modulate inflammation caused by drug-resistant Pseudomonas aeruginosa infections. Compound 5f inhibits biofilm formation, macrophage migration, and inflammatory response induced by P. aeruginosa, showing potential as a novel candidate against drug-resistant infections.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Liuzeng Chen, Ke Wang, Lingyun Wang, Wei Wang, Lifan Wang, Jia Li, Xiaohan Liu, Mengya Wang, Banfeng Ruan
Summary: In this study, a series of novel anti-inflammatory compounds were designed and synthesized based on the natural product pterostilbene skeleton. Among them, compound 8 showed the highest activity and exhibited its effects through inhibition of pro-inflammatory cytokines by blocking the NF-KB/MAPK signaling pathway. Compound 8 also demonstrated a good relieving effect on acute colitis in mice and showed good safety in acute toxicity experiments.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Si-Min Liang, Gui-Bin Liang, Hui-Ling Wang, Hong Jiang, Xian-Li Ma, Jian-Hua Wei, Ri-Zhen Huang, Ye Zhang
Summary: A series of novel multi-target antitumor agents were designed, synthesized, and evaluated. Some compounds exhibited significant antitumor activity and one compound showed excellent efficacy, limited toxicity, and low resistance. Further mechanism studies revealed that the compound exerted antitumor effects through multiple pathways.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)