An upgraded solid‐phase assembly of chelators (DOTA and NOTA) enabled bacterial uptake studies of radiolabeled peptide DOI Open Access

B. Pati,

Anuj Kumar, Arnab Chowdhury

и другие.

ChemBioChem, Год журнала: 2024, Номер 26(1)

Опубликована: Дек. 11, 2024

Abstract Among popular radio metal chelators, DOTA and NOTA have been remarkably considered in radionuclide therapy imaging studies due to several advantages pharmacology. Here, we developed a practical general method for assembling the solid phase peptide (pseudo‐dilute conditions) using wide range of solvents with easily accessible economical feedstocks, which mitigated unprecedented challenges associated previously reported methods. This upgraded approach enabled an efficient installation these two chelators on various bioactive sequences. Finally, assessed antimicrobial activity DOTA‐ NOTA‐attached Combi peptides B. subtilis , was intact. The authenticity assembled framework by labeling 177 Lu vitro bacterial uptake E. coli S. aureus . Lu‐labeled DOTA‐Combi exhibited promising developing infection agent while negligible hemolysis even at >200 μM. contribution will be valued radiopharmaceuticals operational simplicity economic approaches.

Язык: Английский

Image-guided cancer surgery: a narrative review on imaging modalities and emerging nanotechnology strategies DOI Creative Commons
Barbara Bortot, Alessandro Mangogna, Giovanni Di Lorenzo

и другие.

Journal of Nanobiotechnology, Год журнала: 2023, Номер 21(1)

Опубликована: Май 18, 2023

Abstract Surgical resection is the cornerstone of solid tumour treatment. Current techniques for evaluating margin statuses, such as frozen section, imprint cytology, and intraoperative ultrasound, are helpful. However, an assessment margins that accurate safe clinically necessary. Positive surgical (PSM) have a well-documented negative effect on treatment outcomes survival. As result, imaging methods now practical method reducing PSM rates improving efficiency debulking surgery. Because their unique characteristics, nanoparticles can function contrast agents in image-guided While most applications utilizing nanotechnology preclinical stage, some beginning to reach clinical phase. Here, we list various used surgery, optical imaging, computed tomography, magnetic resonance nuclear medicine current developments potential detect malignancies. In coming years, will see evolution tailored specific types introduction equipment improve accuracy. Although promise producing exogenous molecular has been clearly demonstrated, much work remains be done put it into practice. Graphical

Язык: Английский

Процитировано

32

Synthesis, preclinical, and initial clinical evaluation of integrin αVβ3 and gastrin-releasing peptide receptor (GRPR) dual-targeting radiotracer [68Ga]Ga-RGD-RM26-03 DOI

Xuejun Wen,

Rongxi Wang, Peng‐Fei Xu

и другие.

European Journal of Nuclear Medicine and Molecular Imaging, Год журнала: 2024, Номер 51(7), С. 2023 - 2035

Опубликована: Фев. 20, 2024

Язык: Английский

Процитировано

8

Preclinical evaluation of [13xLa]La-FAP-2286 as a novel theranostic agent for tumors expressing fibroblast activation protein DOI Creative Commons

Ali Shirpour,

Asghar Hadadi,

Samaneh Zolghadri

и другие.

Scientific Reports, Год журнала: 2025, Номер 15(1)

Опубликована: Март 3, 2025

In this study, a novel theranostic radiopharmaceutical, [13xLa]La-FAP-2286, for targeting Fibroblast Activation Protein (FAP)-positive tumors. The pair of 132La (half-life: 4.59 h, 42.1% β⁺) and 135La 18.91 100% EC) was produced via proton bombardment natural barium in 30 MeV cyclotron, achieving high radionuclidic purity (99.9%) radiochemical (RCP > 99%). Stability tests revealed the RCP greater than 91% over 24 h human serum PBS buffer. Cellular studies confirmed binding affinity (KD = 0.51 ± 0.12 nM) effective internalization [13xLa]La-FAP-2286 FAP + tumor cells. Distribution coefficient (log D) measurements demonstrated hydrophilicity complex with value − 3.21 0.14. Imaging biodistribution tumor-bearing mice further targeting, significant uptake observed up to 48 post-injection. These results suggest can be considered candidate applications, offering both practical PET imaging targeted Auger-electron therapy cancer treatment.

Язык: Английский

Процитировано

0

Physiologically based radiopharmacokinetic (PBRPK) modeling to simulate and analyze radiopharmaceutical therapies: studies of non-linearities, multi-bolus injections, and albumin binding DOI Creative Commons

Ali Fele‐Paranj,

Babak Saboury,

Carlos Uribe

и другие.

EJNMMI Radiopharmacy and Chemistry, Год журнала: 2024, Номер 9(1)

Опубликована: Янв. 22, 2024

Abstract Background We aimed to develop a publicly shared computational physiologically based pharmacokinetic (PBPK) model reliably simulate and analyze radiopharmaceutical therapies (RPTs), including probing of hot-cold ligand competitions as well alternative injection scenarios drug designs, towards optimal therapies. Results To handle the complexity PBPK models (over 150 differential equations), scalable modeling notation called “reaction graph” is introduced, enabling easy inclusion various interactions. refer this radiopharmacokinetic (PBRPK) modeling, fine-tuned specifically for radiopharmaceuticals. As three important applications, we used our PBRPK (1) study effect competition between hot cold species on delivered doses tumors organs at risk. In addition, (2) evaluated an paradigm utilizing multi-bolus injections in RPTs instead prevalent single injections. Finally, (3) impact varying albumin-binding affinities by ligands, implications RPTs. found that labeled unlabeled ligands can lead non-linear relations injected activity dose particular organ, sense doubling does not necessarily result doubled organ (a false intuition from external beam radiotherapy). observed fractionating higher payload delivery organs, though tumor. By contrast, out increased such delivering more tumors, be attributed several factors allows us probe. Conclusions Advanced enables simulation analysis variety intervention design scenarios,

Язык: Английский

Процитировано

3

An Overview of Structural Framework and Classification of Theranostic Radiopharmaceuticals DOI
Jasleen Kaur, Monalisa Mukherjee

ChemistrySelect, Год журнала: 2024, Номер 9(38)

Опубликована: Окт. 1, 2024

Abstract Radiopharmaceuticals constitute the backbone of nuclear medicine research and have been commonly used in diagnostic imaging radionuclide therapy. In past, there has a strong emphasis on meticulous design development radiotheranostics for targeted molecular therapy different types tumors. Theranostic radiopharmaceuticals offer synergistic advantages simultaneous all one molecule. Owing to their successful pre‐clinical clinical applications, many new theranostic explored recent years. This review aims provide comprehensive overview structural framework radiopharmaceuticals. this review, we primarily focused chelating agents, linkers, radionuclides potential radiotheranostics. addition, also summarizes classification categories such as nano‐radiotheranostics along with applications. The developments applications small molecule‐based radiotheranostics, antibody‐based peptide‐based nanoparticle‐based reviewed inspiring efforts towards efficient

Язык: Английский

Процитировано

0

An upgraded solid‐phase assembly of chelators (DOTA and NOTA) enabled bacterial uptake studies of radiolabeled peptide DOI Open Access

B. Pati,

Anuj Kumar, Arnab Chowdhury

и другие.

ChemBioChem, Год журнала: 2024, Номер 26(1)

Опубликована: Дек. 11, 2024

Abstract Among popular radio metal chelators, DOTA and NOTA have been remarkably considered in radionuclide therapy imaging studies due to several advantages pharmacology. Here, we developed a practical general method for assembling the solid phase peptide (pseudo‐dilute conditions) using wide range of solvents with easily accessible economical feedstocks, which mitigated unprecedented challenges associated previously reported methods. This upgraded approach enabled an efficient installation these two chelators on various bioactive sequences. Finally, assessed antimicrobial activity DOTA‐ NOTA‐attached Combi peptides B. subtilis , was intact. The authenticity assembled framework by labeling 177 Lu vitro bacterial uptake E. coli S. aureus . Lu‐labeled DOTA‐Combi exhibited promising developing infection agent while negligible hemolysis even at >200 μM. contribution will be valued radiopharmaceuticals operational simplicity economic approaches.

Язык: Английский

Процитировано

0