Article
Chemistry, Analytical
Yuanbiao Tu, Zhihao Han, Rongbin Pan, Kuncheng Zhou, Ji Tao, Peifei Liu, Ray P. S. Han, Shuaichang Gong, Yueqing Gu
Summary: The novel peptide GB-6 labeled with NIR fluorescent dye and radionuclide technetium-99m showed efficient targeting to pancreatic cancer cells through the gastrin-releasing peptide receptor. It exhibited selective and specific uptake by tumors in vivo, allowing for clear tumor visualization and potential application in molecular-targeted therapy.
ANALYTICAL CHEMISTRY
(2023)
Article
Biochemical Research Methods
Cuicui Li, Lei Kang, Kevin Fan, Carolina A. Ferreira, Kaelyn Becker, Nan Huo, Hanxiao Liu, Yunan Yang, Jonathan W. Engle, Rongfu Wang, Xiaojie Xu, Dawei Jiang, Weibo Cai
Summary: The study investigated the use of Cu-64-NOTA-YY146 for imaging CD146 expressions in breast cancer, demonstrating its potential for diagnosis, prognosis prediction, and monitoring therapeutic response in orthotopic and metastatic tumor models.
BIOCONJUGATE CHEMISTRY
(2021)
Article
Cell Biology
Zicong Gao, Xingxing Han, Yuying Zhu, He Zhang, Ran Tian, Zhiyong Wang, Yanfen Cui, Zhaosong Wang, Ruifang Niu, Fei Zhang
Summary: Our study demonstrates that exosomal EphA2 plays a key role in transferring aggressive phenotype between cancer cells without direct cell-cell contact. The increase of EphA2 in drug-resistant cell-derived exosomes may be an important mechanism of chemotherapy/drug resistance-induced breast cancer progression. Exosomal EphA2 activates ERK1/2 signaling, promoting breast cancer progression through the Ephrin A1-dependent reverse pathway.
CELL DEATH & DISEASE
(2021)
Review
Biochemistry & Molecular Biology
Ping Zhao, Dewei Jiang, Yunchao Huang, Ceshi Chen
Summary: EphA2, a receptor tyrosine kinase overexpressed in human breast cancers, plays important roles in malignant breast progression and has become a promising therapeutic target for breast cancer treatment.
JOURNAL OF GENETICS AND GENOMICS
(2021)
Article
Oncology
Megan C. Madonna, Joy E. Duer, Joyce V. Lee, Jeremy Williams, Baris Avsaroglu, Caigang Zhu, Riley Deutsch, Roujia Wang, Brian T. Crouch, Matthew D. Hirschey, Andrei Goga, Nirmala Ramanujam
Summary: Targeting tumor metabolism is an effective therapeutic approach, with lipids playing a crucial role in certain cancer subtypes, particularly breast cancer. Imaging techniques, such as intra-vital microscopy with fluorescently labeled molecules, provide a dynamic and quantitative way to study metabolic pathways in vivo. Understanding and manipulating lipid uptake in tumors could lead to the development of new drugs that disrupt these metabolic dependencies and hinder tumor growth.
Article
Radiology, Nuclear Medicine & Medical Imaging
Chung Ying Chan, Zijun Chen, Gianluca Destro, Mathew Veal, Doreen Lau, Edward O'Neill, Gemma Dias, Michael Mosley, Veerle Kersemans, Florian Guibbal, Veronique Gouverneur, Bart Cornelissen
Summary: In this study, [F-18]rucaparib, a non-invasive PARP-targeting imaging agent, was developed for PET imaging of pancreatic cancer. The results showed its potential application value.
EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING
(2022)
Article
Immunology
Jin Wang, Xingchen Liu, Junsong Ji, Jianhua Luo, Yuanyu Zhao, Xiaonan Zhou, Jianming Zheng, Meng Guo, Yanfang Liu
Summary: This study describes the construction of a novel orthotopic PDAC model through implantation of tissue slices and discusses the resistance to immunotherapy from the perspective of a PDAC microenvironment. Results show that elimination of MDSCs by NKG2D CAR can rescue impaired CAR-T cell activity.
FRONTIERS IN IMMUNOLOGY
(2022)
Article
Biophysics
Stefan Markovic, Tangi Roussel, Lilach Agemy, Keren Sasson, Dina Preise, Avigdor Scherz, Lucio Frydman
Summary: The study utilizes deuterium metabolic imaging techniques for pancreatic tumor metabolic imaging, showing the ability to detect lactate signal within the tumors, peaking at 60 minutes. Additionally, the water resonance signal continuously increases throughout the experiment and can be imaged in the entire abdomen, particularly in the tumor, kidney, and bladder.
NMR IN BIOMEDICINE
(2021)
Article
Chemistry, Multidisciplinary
Bin Qu, Yeming Han, Ting Liang, Chao Zhang, Guihua Hou, Feng Gao
Summary: A novel peptide, SD01, was designed and tested for its potential in the diagnosis of TNBC. Compared to another peptide YSA, SD01 showed higher affinity, better imaging, and higher tumor accumulation, making it a promising targeting agent for EphA2.
ARABIAN JOURNAL OF CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Fu-Ling Chang, Cheng-Chung Lee, Keng-Chang Tsai, Tsai-Yu Lin, Chen-Wei Chiang, Shiow-Lin Pan, Yu-Ching Lee
Summary: In this study, a novel antibody-drug conjugate (ADC) specifically targeting EphA2 in pancreatic cancer cells was developed. The ADC showed impressive tumor-killing response, inhibiting tumor cell growth and promoting apoptosis. The results suggest the potential of further developing the ADC to have a broader and more potent therapeutic impact on pancreatic cancer and other EphA2-related cancers.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2023)
Article
Medicine, General & Internal
Ilias Nikas, Constantinos Giaginis, Kalliopi Petrouska, Paraskevi Alexandrou, Artemis Michail, Panagiotis Sarantis, Gerasimos Tsourouflis, Eugene Danas, Alexandros Pergaris, Panagiotis K. Politis, Lydia Nakopoulou, Stamatios Theocharis
Summary: Ongoing research continues to uncover the complex role of ephrin receptors and their ligands in breast cancer pathogenesis. In this study, the clinical significance of EPHA2, EPHA4, and EPHA7 expression in triple-negative breast cancer (TNBC) was investigated. The study found that high expression of EPHA2 was associated with poorer overall survival and disease-free survival, while high expression of EPHA4 was linked to lymph node metastasis. The study suggests that EPHA2 could be a potential prognostic factor for TNBC patients.
Article
Veterinary Sciences
Silvia Elena Santana-Krimskaya, Jorge R. Kawas, Diana Ginette Zarate-Trivino, Yareellys Ramos-Zayas, Cristina Rodriguez-Padilla, Moises Armides Franco-Molina
Summary: Breast cancer is the most common type of cancer worldwide, and triple negative breast cancer is an aggressive subtype. A study has compared the differences between the mammary fat pad orthotopic model and the air pouch heterotopic model in terms of tumor microenvironment factors. The results showed that orthotopic tumors form more metastases, while heterotopic tumors grow larger and have a higher FOXP3 cell infiltrate.
RESEARCH IN VETERINARY SCIENCE
(2022)
Article
Oncology
Gloria Echeverria, Shirong Cai, Yizheng Tu, Jiansu Shao, Emily Powell, Abena B. Redwood, Yan Jiang, Aaron McCoy, Amanda L. Rinkenbaugh, Rosanna Lau, Alexander J. Trevarton, Chunxiao Fu, Rebekah Gould, Elizabeth E. Ravenberg, Lei Huo, Rosalind Candelaria, Lumarie Santiago, Beatriz E. Adrada, Deanna L. Lane, Gaiane M. Rauch, Wei T. Yang, Jason B. White, Jeffrey T. Chang, Stacy L. Moulder, W. Fraser Symmans, Susan G. Hilsenbeck, Helen Piwnica-Worms
Summary: This study established 369 orthotopic PDX models of breast cancer and found that treatment-resistant cancers were more likely to be successfully engrafted. The molecular subtype of breast cancer was not associated with engraftment rate. A statistical model predictive of engraftment was developed based on clinical indicators. These breast cancer models are valuable for clinical treatment and biomarker research.
Article
Biophysics
Xinyu Zhan, Sha Yang, Guorong Huang, Lihua Yang, Yang Zhang, Huiyan Tian, Fengxin Xie, Marc Lamy de la Chapelle, Xiang Yang, Weiling Fu
Summary: The research team developed a THz metamaterial biosensor for exosomal miRNA detection based on DSN-triggered RCA. The biosensor showed high sensitivity and specificity, enabling rapid and accurate miR-21 detection in clinical plasma samples, with the ability to distinguish between pancreatic cancer patients and healthy controls.
BIOSENSORS & BIOELECTRONICS
(2021)
Article
Engineering, Biomedical
Theresa C. Ezenwafor, Vanessa O. Uzonwanne, Jonathan U. A. Madukwe, Said M. Amin, Vitalis C. Anye, John D. Obayemi, Olushola S. Odusanya, Winston O. Soboyejo
Summary: This paper presents a combined experimental and theoretical study on the adhesion between molecular recognition units and receptors on tumor surfaces. The results show that the adhesion forces and energies between high-grade TNBC tissues and Luteinizing Hormone Releasing Hormone (LHRH) or Epherin type A2 (EphA2) are significantly higher than those with normal human breast tissues. These findings have important implications for the development of targeted nanostructures for the detection and treatment of TNBC.
JOURNAL OF THE MECHANICAL BEHAVIOR OF BIOMEDICAL MATERIALS
(2022)
Article
Biochemistry & Molecular Biology
Carlo Baggio, Parima Udompholkul, Luca Gambini, Jennifer Jossart, Ahmed F. Salem, Maria Hakansson, J. Jefferson P. Perry, Maurizio Pellecchia
CHEMICAL BIOLOGY & DRUG DESIGN
(2020)
Article
Biochemistry & Molecular Biology
Elisa Barile, Carlo Baggio, Luca Gambini, Sergey A. Shiryaev, Alex Y. Strongin, Maurizio Pellecchia
Article
Chemistry, Medicinal
Luca Gambini, Parima Udompholkul, Ahmed F. Salem, Carlo Baggio, Maurizio Pellecchia
Editorial Material
Biochemistry & Molecular Biology
Michael Guetschow, Jean Jacques Vanden Eynde, Josef Jampilek, CongBao Kang, Arduino A. Mangoni, Paola Fossa, Rafik Karaman, Andrea Trabocchi, Peter J. H. Scott, Johannes Reynisson, Simona Rapposelli, Stefania Galdiero, Jean-Yves Winum, Chiara Brullo, Katalin Prokai-Tatrai, Arun K. Sharma, Matthieu Schapira, Yasu-Taka Azuma, Laura Cerchia, Mariana Spetea, Giangiacomo Torri, Simona Collina, Athina Geronikaki, Alfonso T. Garcia-Sosa, M. Helena Vasconcelos, Maria Emilia Sousa, Ivan Kosalec, Tiziano Tuccinardi, Iola F. Duarte, Jorge A. R. Salvador, Massimo Bertinaria, Maurizio Pellecchia, Jussara Amato, Giulio Rastelli, Paula A. C. Gomes, Rita C. Guedes, Jean-Marc Sabatier, Ana Estevez-Braun, Bruno Pagano, Stefano Mangani, Rino Ragno, George Kokotos, Margherita Brindisi, Florenci V. Gonzalez, Fernanda Borges, Mariarosaria Miloso, Jarkko Rautio, Diego Munoz-Torrero
Article
Chemistry, Medicinal
Ahmed F. Salem, Luca Gambini, Parima Udompholkul, Carlo Baggio, Maurizio Pellecchia
Article
Chemistry, Medicinal
Luca Gambini, Parima Udompholkul, Carlo Baggio, Aruljothi Muralidharan, Nikola Kenjic, Zahra Assar, J. Jefferson P. Perry, Maurizio Pellecchia
Summary: By targeting Lys residues with structure-based design of covalent inhibitors, we have identified a potential novel route for designing potent and selective PPIs inhibitors, as evidenced by the design, synthesis, and characterizations of the first Lys-covalent BH3 peptide in our study. This approach could pave the way for the development of novel pro-apoptotic agents targeting specific protein-protein interactions.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Carlo Baggio, Anna Kulinich, Cassandra N. Dennys, Rochelle Rodrigo, Kathrin Meyer, Iryna Ethell, Maurizio Pellecchia
Summary: The study utilized an innovative NMR-guided screening and ligand design approach to derive low-molecular-weight ligands capable of mimicking interactions elicited by ephrin ligands. These agents demonstrated nanomolar affinity, activated receptors in cellular assays with motor neurons, and provided significant motor neuron protection from ALS patient-derived astrocytes. Structural studies on the complex between the ligand-binding domain and the most active agent offered insights into the agents' mechanism at a molecular level, forming a strong foundation for potential treatment of ALS and other human diseases.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Parima Udompholkul, Carlo Baggio, Luca Gambini, Giulia Alboreggia, Maurizio Pellecchia
Summary: The study describes the derivation and characterization of a potent ML-IAP Lys-covalent inhibitor with cellular activity, which can serve as a pharmacological tool to validate ML-IAP as a drug target and facilitate the development of ML-IAP-targeted therapeutics.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Multidisciplinary Sciences
Cassandra Dennys, Carlo Baggio, Rochelle Rodrigo, Florence Roussel, Anna Kulinich, Sarah Heintzman, Ashley Fox, Stephen J. Kolb, Pamela J. Shaw, Iryna M. Ethell, Maurizio Pellecchia, Kathrin C. Meyer
Summary: Amyotrophic lateral sclerosis (ALS) is a degenerative disease. EphA4 agonistic agents have the potential to be a promising therapeutic strategy for ALS.
Article
Chemistry, Medicinal
Carlo Baggio, Parima Udompholkul, Luca Gambini, Maurizio Pellecchia
Summary: This study discovered a novel agent, targefrin, that binds to EphA2-LBD and shows promising anti-cancer effects in cell-based assays and a mouse model.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Carlo Baggio, Jalene V. Velazquez, Marco Fragai, Tara M. Nordgren, Maurizio Pellecchia
JOURNAL OF MEDICINAL CHEMISTRY
(2020)