Article
Biochemistry & Molecular Biology
Mireia Pujals, Carla Mayans, Chiara Bellio, Olga Mendez, Emanuela Greco, Roberta Fasani, Merce Alemany-Chavarria, Esther Zamora, Laura Padilla, Francesc Mitjans, Paolo Nuciforo, Francesc Canals, Lara Nonell, Maria Abad, Cristina Saura, Josep Tabernero, Josep Villanueva
Summary: Epithelial/mesenchymal (E/M) plasticity is important in both embryogenesis and tumorigenesis. The role of receptor for advanced glycation end products (RAGE) in triple-negative breast cancer (TNBC) is unclear. This study shows that RAGE signaling maintains the mesenchymal phenotype of aggressive TNBC cells through the expression of SNAIL1 and its crosstalk with the TGF-β pathway. RAGE inhibition promotes epithelial features and reduces migration and invasion capacities. In vivo inhibition of RAGE reduces metastasis incidence and improves survival.
Article
Oncology
Melinda Magna, Gyong Ha Hwang, Alec McIntosh, Katherine Drews-Elger, Masaru Takabatake, Adam Ikeda, Barbara J. Mera, Taekyoung Kwak, Philip Miller, Marc E. Lippman, Barry I. Hudson
Summary: In this study, it was found that small molecule RAGE inhibitors, TTP488 and FPS-ZM1, can impair TNBC metastasis and fundamental mechanisms underlying tumor progression. TTP488 showed greater potency in reducing metastasis and had a stronger effect on metastatic driver pathways. Functional cell assays confirmed that RAGE inhibition impaired TNBC cell adhesion, migration, and invasion.
Article
Genetics & Heredity
Justine Marsolier, Pacome Prompsy, Adeline Durand, Anne-Marie Lyne, Camille Landragin, Amandine Trouchet, Sabrina Tenreira Bento, Almut Eisele, Sophie Foulon, Lea Baudre, Kevin Grosselin, Mylene Bohec, Sylvain Baulande, Ahmed Dahmani, Laura Sourd, Eric Letouze, Anne-Vincent Salomon, Elisabetta Marangoni, Leila Perie, Celine Vallot
Summary: The persistence of drug-resistant cancer cells is a major clinical challenge, particularly in triple-negative breast cancer. This study reveals that the repressive histone mark H3K27me3 plays a crucial role in regulating cell fate and chemotherapy tolerance in cancer cells. Manipulating H3K27me3 levels effectively enhances the potential of cancer cells to tolerate chemotherapy and delays tumor recurrence. These findings underscore the importance of understanding chromatin landscapes in shaping cancer cell response to initial therapy.
Article
Biochemistry & Molecular Biology
Lake-Ee Quek, Michelle van Geldermalsen, Yi Fang Guan, Kanu Wahi, Chelsea Mayoh, Seher Balaban, Angel Pang, Qian Wang, Mark J. Cowley, Kristin K. Brown, Nigel Turner, Andrew J. Hoy, Jeff Holst
Summary: This study reveals that glutamine-indispensable triple-negative breast cancer (TNBC) cells rely on a non-canonical glutamine-to-glutamate overflow, which increases TCA cycle fluxes and replenishes TCA cycle intermediates. The coupling of glucose and glutamine catabolism hampers TNBC cells' ability to oxidize glucose when glutamine is limiting.
Review
Oncology
Dorota Kwapisz
Summary: Triple-negative breast cancer (TNBC) is a subtype of breast cancer with poor prognosis and limited treatment options, but it shows higher immunogenicity, tumor-infiltrating lymphocytes (TILs) enrichment, and programmed cell death ligand 1 (PD-L1) expression which make it more suitable for immune checkpoint blockade therapy. Patients with PD-L1-positive TNBC subgroup may benefit the most from immune checkpoint inhibitor (ICI) treatment, and ICI given as first-line treatment in advanced TNBC shows better results than in later lines of treatment. Exciting results have been seen with pembrolizumab in early-stage TNBC, indicating potential approval in (neo)adjuvant settings in the near future.
CANCER IMMUNOLOGY IMMUNOTHERAPY
(2021)
Letter
Medicine, General & Internal
Ryan Sun, Lee-Jen Wei
Summary: This article discusses the clinical benefits of pembrolizumab combined with chemotherapy in patients with triple-negative breast cancer. The authors suggest that both hazard values and ratios should be considered when evaluating clinical benefits.
NEW ENGLAND JOURNAL OF MEDICINE
(2022)
Article
Chemistry, Medicinal
Carine M. Abdelmalek, Zexi Hu, Thales Kronenberger, Jenni Kublbeck, Franziska J. M. Kinnen, Salma S. Hesse, Afsin Malik, Mark Kudolo, Raimund Niess, Matthias Gehringer, Lars Zender, Paula A. Witt-Enderby, Darius P. Zlotos, Stefan A. Laufer
Summary: Anticancer drug conjugates that simultaneously target two receptors may overcome the limitations of current cancer treatments. A series of compounds connecting tamoxifen or endoxifen with the EGFR-inhibitor gefitinib exhibit potent anticancer activity in breast cancer cells.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Oncology
Rui Han, Hongxing Yang, Changquan Ling, Lingeng Lu
Summary: In this study, the therapeutic potential of Tiliroside (TS) in triple negative breast cancer (TNBC) was evaluated. The results showed that TS exhibited anti-cancer activity, reduced tumor burden, and improved survival rate in TNBC. Additionally, TS acted as a CAXII inhibitor to suppress TNBC progression.
CANCER CELL INTERNATIONAL
(2022)
Article
Oncology
Kurt W. Evans, Erkan Yuca, Stephen S. Scott, Ming Zhao, Natalia Paez Arango, Christian X. Cruz Pico, Turcin Saridogan, Maryam Shariati, Caleb A. Class, Christopher A. Bristow, Christopher P. Vellano, Xiaofeng Zheng, Ana Maria Gonzalez-Angulo, Xiaoping Su, Coya Tapia, Ken Chen, Argun Akcakanat, Bora Lim, Debu Tripathy, Timothy A. Yap, Maria Emilia Di Francesco, Giulio F. Draetta, Philip Jones, Timothy P. Heffernan, Joseph R. Marszalek, Funda Meric-Bernstam
Summary: Oxidative phosphorylation is a metabolic vulnerability in triple-negative breast cancer, and inhibiting it with IACS-10759 may enhance efficacy of multiple targeted therapies.
Review
Oncology
Shengye Jin, Qin Wang, Hao Wu, Da Pang, Shouping Xu
Summary: Biological therapy, particularly oncolytic viruses (OVs), has shown promising therapeutic effects in various cancers, including triple negative breast cancer (TNBC). TNBC, lacking conventional treatment targets, benefits from the emerging concept of OVs for potential treatment options.
BIOMARKER RESEARCH
(2021)
Review
Medicine, General & Internal
Jieun Lee
Summary: Triple-negative breast cancer (TNBC) is an aggressive type of breast cancer, accounting for 15-20% of cases, with a high rate of recurrence despite chemotherapy. Conventional cytotoxic chemotherapy with anthracyclines and taxanes remains the main treatment option. Achievement of pathologic complete response (pCR) is associated with improved survival outcomes, leading to the shift towards neoadjuvant treatment and investigation of intensified chemotherapy and post-neoadjuvant therapy. This article reviews the current treatment landscape for early TNBC, from standard cytotoxic chemotherapy to immune checkpoint inhibitors, capecitabine, and olaparib.
JOURNAL OF CLINICAL MEDICINE
(2023)
Article
Cell Biology
Giulia Salvadori, Federica Zanardi, Fabio Iannelli, Riccardo Lobefaro, Claudio Vernieri, Valter D. Longo
Summary: The study demonstrates that a fasting-mimicking diet activates starvation escape pathways in TNBC cells and reduces stemness markers in CSCs, leading to decreased cell numbers and improved mouse survival. Additionally, the diet activates different survival/growth pathways in differentiated cancer cells, which can be targeted by drugs to promote tumor regression.
Letter
Medicine, General & Internal
Shuvadeep Ganguly, Ajay Gogia
Summary: In the KEYNOTE-522 trial, the addition of Pembrolizumab to neoadjuvant chemotherapy improved pathological complete response rate in early triple-negative breast cancer patients and also improved event-free survival. However, this improvement was predominantly observed in patients who did not achieve a pathological complete response.
NEW ENGLAND JOURNAL OF MEDICINE
(2022)
Article
Biochemistry & Molecular Biology
Jankiben R. Patel, Prasad Thangavelu, Renee M. Terrell, Bridg'ette Israel, Arindam Basu Sarkar, A. Michael Davidson, Kun Zhang, Rahul Khupse, Syreeta L. Tilghman
Summary: A novel allosteric inhibitor targeting the PLK1 T-loop was developed and shown to have anti-proliferative and anti-migratory properties in triple-negative breast cancer cells. The inhibitor caused cell cycle arrest and increased p21 expression, suggesting its potential as a promising approach for TNBC treatment.
Article
Oncology
Felipe Batalini, Niya Xiong, Nabihah Tayob, Madeline Polak, Julia Eismann, Lewis C. Cantley, Geoffrey Shapiro, Viktor Adalsteinsson, Eric P. Winer, Panagiotis A. Konstantinopoulos, Alan D'Andrea, Elizabeth M. Swisher, Ursula A. Matulonis, Gerburg M. Wulf, Erica L. Mayer
Summary: This study aimed to evaluate the safety and recommended dose of olaparib in combination with alpelisib in patients with breast cancer, and explore its effects on different subtypes. The results showed that this combination therapy was tolerable for pre-treated TNBC patients and demonstrated activity in non-BRCA mutant patients. Analysis of circulating-free DNA also provided important prognostic information.
CLINICAL CANCER RESEARCH
(2022)
Article
Chemistry, Multidisciplinary
Xiuhong Lu, Wen Wang, Qian Dong, Xiaolong Bao, Xianfeng Lin, Weixing Zhang, Xiaochun Dong, Weili Zhao
CHEMICAL COMMUNICATIONS
(2015)
Article
Chemistry, Medicinal
Xiuhong Lu, Yuanqiu Peng, Chenglin Wang, Jun Yang, Xiaolong Bao, Qian Dong, Weili Zhao, Wenfu Tan, Xiaochun Dong
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2017)
Article
Radiology, Nuclear Medicine & Medical Imaging
Weiyan Zhou, Weiqi Bao, Donglang Jiang, Yanyan Kong, Fengchun Hua, Xiuhong Lu, Yihui Guan
NUCLEAR MEDICINE AND BIOLOGY
(2018)
Article
Chemistry, Multidisciplinary
Xiuhong Lu, Zhongjian Chen, Xiaochun Dong, Weili Zhao
Editorial Material
Chemistry, Multidisciplinary
Xiuhong Lu, Guangyu Lin, Xiaochun Dong, Weili Zhao, Zhongjian Chen
Article
Chemistry, Organic
Yongsheng Zhang, Jincheng Wang, Zhenjiao Yang, Zeng Zhang, Xiaoyan He, Guoliang Chen, Gang Huang, Xiuhong Lu
Summary: In this study, an in situ neocuproine-copper complex formation method was reported for the synthesis of diimine and reduction of alkynes. The method shows a broad functional group tolerance and substrate adaptability, as well as advantages of safety and high efficiency. Furthermore, it provides a useful complementary method to traditional catalytic hydrogenation for reducing nitro, benzyl, boc, and sulfur containing alkynes.
JOURNAL OF ORGANIC CHEMISTRY
(2021)
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)
