Article
Engineering, Biomedical
Ye Feng, Qianqian Liu, Yi Li, Yang Han, Meng Liang, Hao Wang, Qing Yao, Yuli Wang, Meiyan Yang, Zhiping Li, Wei Gong, Yang Yang, Chunsheng Gao
Summary: The study introduces a cell relay-delivery strategy using artificially damaging/aging erythrocytes to hitchhike on circulating monocytes/macrophages for intratumoral accumulation of anticancer drugs, aiming to improve the efficacy of cancer treatment.
BIOACTIVE MATERIALS
(2021)
Article
Oncology
Marjolein Verhoeven, Eline A. M. Ruigrok, Geert J. L. H. van Leenders, Lilian van den Brink, Hayri E. Balcioglu, Wytske M. van Weerden, Simone U. Dalm
Summary: This study demonstrates that GRPR-targeting approaches can complement and improve the current PSMA-targeting strategies in the management of both early and late stage PCa.
FRONTIERS IN ONCOLOGY
(2023)
Article
Nanoscience & Nanotechnology
June Yong Park, Yuseon Shin, Woong Roeck Won, Chaemin Lim, Jae Chang Kim, Kioh Kang, Patihul Husni, Eun Seong Lee, Yu Seok Youn, Kyung Taek Oh
Summary: An AE147 peptide-conjugated nanocarrier system was developed to target metastatic tumors, displaying potential and effective accumulation at tumor metastatic sites.
INTERNATIONAL JOURNAL OF NANOMEDICINE
(2021)
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)
Review
Cell Biology
Jianying Li, Chelsea Bolyard, Gang Xin, Zihai Li
Summary: Targeting the metabolic profiles of tumor-infiltrating myeloid cells is crucial for overcoming immunotherapy resistance in cancer, as metabolic modulation can shift these cells from pro-tumor to anti-tumor phenotypes. Regulating specific metabolic pathways in myeloid cells within the tumor microenvironment holds therapeutic value in enhancing and improving outcomes with cancer immunotherapy.
FRONTIERS IN CELL AND DEVELOPMENTAL BIOLOGY
(2021)
Article
Endocrinology & Metabolism
Brendon Herring, Samuel Jang, Jason Whitt, Kayla Goliwas, Zviadi Aburjania, Vikas Dudeja, Bin Ren, Joel Berry, James Bibb, Andra Frost, Herbert Chen, John Bart Rose, Renata Jaskula-Sztul
Summary: This study proposes the use of an ex vivo 3D flow-perfusion bioreactor system for cultivating and studying patient-derived neuroendocrine tumors (NETs), demonstrating its utility and providing methods for evaluating therapeutic efficacy. The research suggests that the bioreactor system and similar 3D culture models may be valuable tools for culturing patient-derived NETs and monitoring their response to therapy ex vivo.
FRONTIERS IN ENDOCRINOLOGY
(2021)
Review
Cell Biology
Yibing Chen, Huan Jin, Yucen Song, Ting Huang, Jun Cao, Qing Tang, Zhengzhi Zou
Summary: Tumor-associated macrophages play a significant role in tumor progression and treatment resistance in solid tumors, leading to the development of promising immunotherapeutic strategies targeting macrophages. Targeting TAMs in combination with conventional therapies has shown to be effective in treating solid tumors. Challenges, obstacles in clinical trials, and future perspectives for TAMs-targeting therapies in various cancers are also discussed in this review.
JOURNAL OF CELLULAR PHYSIOLOGY
(2021)
Article
Radiology, Nuclear Medicine & Medical Imaging
Ingrid L. Bakker, Alida C. Froberg, Martijn B. Busstra, J. Fred Verzijlbergen, Mark Konijnenberg, Geert J. L. H. van Leenders, Ivo G. Schoots, Erik de Blois, Wytske M. van Weerden, Simone U. Dalm, Theodosia Maina, Berthold A. Nock, Marion de Jong
Summary: The study demonstrated that the GRPr receptor overexpressed in prostate cancer cells is effective for early prostate cancer imaging, with 68Ga-SB3 PET/CT imaging showing tumor lesions and a significant correlation between GRPr expression and tracer uptake.
JOURNAL OF NUCLEAR MEDICINE
(2021)
Article
Chemistry, Multidisciplinary
Rishi Sharma, Kevin Liaw, Anjali Sharma, Ambar Jimenez, Michelle Chang, Sebastian Salazar, Imaan Amlani, Sujatha Kannan, Rangaramanujam M. Kannan
Summary: The research explores the use of sugar moieties conjugated to dendrimers for targeted therapy of glioblastoma and other cancers. Glucose modification significantly enhances targeting of tumor-associated macrophages and microglia, while galactose modification shifts targeting towards galectins on glioblastoma tumor cells.
JOURNAL OF CONTROLLED RELEASE
(2021)
Article
Chemistry, Medicinal
Simon Lindner, Henning Rudolf, Giovanna Palumbo, Rosel Oos, Melissa Antons, Ralph Hubner, Peter Bartenstein, Ralf Schirrmacher, Bjoern Waengler, Carmen Waengler
Summary: This study presents the initial in vivo evaluation of the most potent heterobivalent gastrin-releasing peptide receptor (GRPR) and vasoactive intestinal peptide receptor subtype 1 (VPAC(1)R) bispecific radiotracer and determined its tumor visualization potential via PET/CT imaging. Only [Ga-68]Ga-NODA-GA-PESIN among the monovalent radiotracers could efficiently delineate the tumor, confirming the results.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2021)
Article
Biochemistry & Molecular Biology
Lei Wang, Ivica Jerolim Bratanovic, Zhengxing Zhang, Hsiou-Ting Kuo, Helen Merkens, Jutta Zeisler, Chengcheng Zhang, Ruiyan Tan, Francois Benard, Kuo-Shyan Lin
Summary: With overexpression in various cancers, the gastrin-releasing peptide receptor (GRPR) is a promising target for cancer imaging and therapy. Three Ga-68-labeled agonist tracers, Ga-TacBOMB2, TacBOMB3, and TacBOMB4, were developed and compared with the clinically validated agonist PET tracer, [Ga-68]Ga-AMBA. The results showed that [Ga-68]Ga-TacBOMB2 had comparable tumor uptake but superior tumor-to-background contrast ratios compared to [Ga-68]Ga-AMBA, and both [Ga-68]Ga-TacBOMB2 and [Ga-68]Ga-TacBOMB3 had much lower pancreas uptake than [Ga-68]Ga-AMBA. This suggests that [Thz(14)]Bombesin(7-14) is a promising targeting vector for GRPR-targeting radiopharmaceuticals.
Review
Pharmacology & Pharmacy
Mingming Zhang, Shan Gao, Dongjuan Yang, Yan Fang, Xiaojie Lin, Xuechao Jin, Yuli Liu, Xiu Liu, Kexin Su, Kai Shi
Summary: This review discusses the challenges and mechanisms of nanoparticle infiltration in tumor microenvironment, as well as the strategies for enhancing therapeutic efficacy through adjusting the characteristics and structure of nanoparticles. The comprehensive summary provided in this review aims to guide future research in improving cancer treatment outcomes.
ACTA PHARMACEUTICA SINICA B
(2021)
Article
Biochemistry & Molecular Biology
Md Habban Akhter, Sarwar Beg, Mohammed Tarique, Arshi Malik, Sarah Afaq, Hani Choudhry, Salman Hosawi
Summary: Although nanomedicines fabricated from biocompatible nanocarriers have reduced targeting potential for clinical benefits, over expression of receptors on tumor cells offers opportunity to design functional nanomedicines for specific delivery of therapeutics, alleviating bio-toxicity and unwanted effects.
BIOCHIMICA ET BIOPHYSICA ACTA-GENERAL SUBJECTS
(2021)
Article
Chemistry, Multidisciplinary
Zhiyang Chen, Liang Chen, Yiqun Ma, Yuyi Liu, Qianyi Zhang, Hao Qin, Yu Chen, Bo Tian, Jian Dong
Summary: A nanosystem is designed and fabricated for synergistic sonodynamic-immunometabolic therapy of spinal-metastasized tumors by integrating oxygen-deficient molybdenum oxide (ODM) nanosonosensitizers and R7 peptides. The nanosystem combines sonodynamic therapy with tumor metabolic regulation, achieving concurrent immune activation and immunosuppressive tumor microenvironment remodeling.
ADVANCED MATERIALS
(2023)
Review
Oncology
Aggelos T. Margetis
Summary: Dysregulated metabolism is a fundamental characteristic of carcinogenesis, leading to aggressive features and additional hallmarks. This review provides a comprehensive overview of well-established metabolic changes in tumors and discusses potential therapeutic targets, bridging the gap between basic research and clinical application in oncology. The tumor microenvironment plays a significant role, as extracellular metabolites, pH alterations, and stromal cells interact with malignant cells, influencing tumor-promoting responses, disabling anti-tumor immunity, and promoting treatment resistance.
JOURNAL OF CANCER RESEARCH AND CLINICAL ONCOLOGY
(2023)
Editorial Material
Radiology, Nuclear Medicine & Medical Imaging
Marcus Unterrainer, Simon Lindner, Leonie Beyer, Franz J. Gildehaus, Andrei Todica, Lena M. Mittlmeier, Klaus Jurkschat, Carmen Waengler, Bjoern Waengler, Ralf Schirrmacher, Joerg C. Tonn, Nathalie L. Albert, Peter Bartenstein, Harun Ilhan
Summary: The novel F-18-SiTATE peptide with remarkable imaging properties may help overcome the shortcomings of Ga-68-labeled ligands and foster widespread use of SSTR ligands in imaging for meningioma patients. Compared to Ga-68-labeled ligands, F-18-SiTATE provides important information with comparable quantitative uptake and very good spatial resolution, potentially increasing its utility in clinical practice.
CLINICAL NUCLEAR MEDICINE
(2021)
Article
Radiology, Nuclear Medicine & Medical Imaging
Leonie Beyer, Astrid Gosewisch, Simon Lindner, Friederike Voelter, Lena M. Mittlmeier, Reinhold Tiling, Matthias Brendel, Clemens C. Cyran, Marcus Unterrainer, Johannes Ruebenthaler, Christoph J. Auernhammer, Christine Spitzweg, Guido Boening, F. J. Gildehaus, Klaus Jurkschat, Carmen Wangler, Bjoern Wangler, Ralf Schirrmacher, Vera Wenter, Andrei Todica, Peter Bartenstein, Harun Ilhan
Summary: This study demonstrated the high tumor-to-background ratios and comparable effective dose of [F-18]SiTATE-PET/CT in NET patients from 60 to 180 minutes after injection, with the best compromise between image quality and tumor-to-background contrast reached at 120 minutes followed by 60 minutes.
EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING
(2021)
Article
Chemistry, Multidisciplinary
Justin J. Bailey, Melinda Wuest, Tamara Bojovic, Travis Kronemann, Carmen Waengler, Bjoern Waengler, Frank Wuest, Ralf Schirrmacher
Summary: Efforts to produce an F-18-labeled analogue of the PDE5 inhibitor tadalafil for visualizing PDE5 expression in vivo with PET were hindered by quantitative epimerization of the tadalafil C12a stereocenter during late-stage fluorination, resulting in a less active epi-isomer. In vivo microPET images in mice showed that the epimerized radiotracer accumulated rapidly in the liver with minimal uptake in tissues known for PDE5 expression.
Article
Chemistry, Medicinal
Xia Cheng, Ralph Huebner, Valeska von Kiedrowski, Gert Fricker, Ralf Schirrmacher, Carmen Wangler, Bjorn Wangler
Summary: Combining two peptides into a heterobivalent peptidic ligand (HBPL) shows promise in improving tumor visualization in melanoma treatment by targeting two different receptors simultaneously.
Article
Chemistry, Medicinal
Marco Maspero, Clelia Dallanoce, Bjoern Waengler, Carmen Waengler, Ralph Huebner
Summary: In this study, we describe and explain the aberrant behavior in receptor binding profile of a fluorescein-based multimodal imaging agent for gastrin releasing peptide receptor (GRPR) visualization by elucidating a chelating mechanism on sodium ions of its fluorescent dye moiety.
Article
Chemistry, Multidisciplinary
Benedikt Judmann, Diana Braun, Ralf Schirrmacher, Bjoern Wangler, Carmen Wangler, Gert Fricker
Summary: The study suggests that GE11-based monovalent and small homomultivalent radiotracers have limited affinity for EGFR and are not promising for further development as radioligands.
Article
Chemistry, Medicinal
Helen Damerow, Bjoern Waengler, Ralf Schirrmacher, Gert Fricker, Carmen Waengler
Summary: Different chelators can be used to introduce [Ga-68]Ga3+ into receptor-specific peptidic carriers for radiotracer imaging, and the choice of chelating agent significantly affects the in vivo pharmacokinetics of the radiopeptides. A backbone-functionalized variant of the chelator CB-DO2A, CB-DO2A-GA, was developed as a valuable alternative to established chelating agents for Ga-68-radiolabeling of peptides. It was found that CB-DO2A-GA required harsher reaction conditions for Ga-68-incorporation compared to DOTA, NODA-GA, and DOTA-GA.
Article
Pharmacology & Pharmacy
Helen Damerow, Xia Cheng, Valeska von Kiedrowski, Ralf Schirrmacher, Bjoern Waengler, Gert Fricker, Carmen Waengler
Summary: Zr-89 is a highly favorable positron emitter for immuno-PET imaging. Complexation of the Zr-89(4+) ion with desferrioxamine B is commonly used to introduce the ion into antibodies, but the complexes have limited kinetic inertness. Therefore, new chelators, such as DFO* and 3,4,3-(LI-1,2-HOPO), have been developed. Comparisons between these chelators have shown that DFO* is the most suitable candidate for stable Zr-89 labeling of antibodies for clinical translation.
Article
Chemistry, Medicinal
Benedikt Judmann, Bjorn Waengler, Ralf Schirrmacher, Gert Fricker, Carmen Waengler
Summary: This study investigated whether certain peptidic radiotracers can specifically target EGFR-positive tumors. The results showed that these radiotracers failed to demonstrate the ability to specifically target EGFR-positive tumors, suggesting the need for further exploration of alternative radiotracers.
Review
Chemistry, Medicinal
Carolin Jaworski, Petar Iliev, Carmen Waengler, Bjoern Waengler, Brent Page, Ralf Schirrmacher, Justin J. Bailey
Summary: Trk inhibitors are significant in personalized medicine as they target specific genetic alterations, leading to improved treatment outcomes for cancer patients. Efforts are being made to enhance efficacy and reduce toxicity.
EXPERT OPINION ON THERAPEUTIC PATENTS
(2023)