Detectability of Al18F-NOTA-HER2-BCH PET for Nodal Metastases in Patients With HER2-Positive Breast Cancer.

Purpose: The aim of this study was to compare Al18F-NOTA-HER2-BCH and 18F-FDG for detecting nodal metastases in patients with HER2-positive breast cancer on PET/CT.

Patients And Methods: In this retrospective study, 62 participants with HER2-positive breast cancer underwent both Al18F-NOTA-HER2-BCH and 18F-FDG PET/CT. Participants were pathologically confirmed as HER2-positive (IHC 3+ or IHC 2+ with gene amplification on FISH).

Radioiodinated Nanobody immunoPET probe for in vivo detection of CD147 in pan-cancer.

Background: To develop the extracellular matrix metalloproteinase inducer (CD147)-targeting therapeutic strategies, accurate detection of CD147 expression in tumors is crucial. Owing to their relatively low molecular weights and high affinities, nanobodies (Nbs) may be powerful candidates for cancer diagnosis and therapy. In this study, we developed a novel CD147-targeted nanobody radiotracer, [I]I-NB147, which provides guidance for the noninvasive detection of CD147-overexpressing cancers.

Copper-64 Based PET-Radiopharmaceuticals: Ways to Clinical Translational.

Positron emission tomography (PET) as an advanced noninvasive imaging technique, provides unprecedented insights into the study of physiological and biochemical processes in vivo. Copper-64 (Cu) has a ideal half-life of 12.7 hours, with β+ and β-dual decay modes and abundant coordination chemistry, enabling the development of a wide variety of radiopharmaceuticals for PET imaging and radionuclide therapy.

Construction of [Zr]Zr-Labeled HuL13 for ImmunoPET Imaging of LAG-3 Checkpoint Expression on Tumor-Infiltrating T Cells.

Lymphocyte activation gene 3 (LAG-3) has attracted much attention as a potentially valuable immune checkpoint. Individual identification of LAG-3 expression at screening and during treatment could improve the successful implementation of anti-LAG-3 therapies. HuL13 is a human IgG1 monoclonal antibody that binds to the LAG-3 receptor in T cells.

Construction and Application of a PD-L1-Targeted Multimodal Diagnostic and Dual-Functional Theranostics Nanoprobe.

Background: In recent years, PD-L1 has been primarily utilized as an immune checkpoint marker in cancer immunotherapy. However, due to tumor heterogeneity, the response rate to such therapies often falls short of expectations. In addition to its role in immunotherapy, PD-L1 serves as a specific target on the surface of tumor cells for targeted diagnostic and therapeutic interventions.

An iodine‑labelled Antibody-drug conjugate PET probe for noninvasive monitoring of Nectin-4 expression in urothelial carcinoma.

Background And Purpose: Some kinds of antibody-drug conjugate (ADC) with high affinity to Nectin-4 have demonstrated breakthrough progress in the third-line setting for bladder cancer. However, many patients are still difficult to benefit from treatment based on the heterogeneity of tumour. As the most advanced auxiliary treatment technology, treatment visualization can most intuitively predict the effectiveness of drug treatment, and timely detect the occurrence of drug resistance.

I-labeled anti-CD147 antibody for noninvasive detection of CD147-positive pan-cancers: construction and preclinical studies.

Extracellular matrix metalloproteinase inducer CD147 is a glycoprotein on the cell surface. There is minimal expression of CD147 in normal epithelial and fetal tissues, but it is highly expressed in a number of aggressive tumors. CD147 has been implicated in pan-cancer immunity and progression.

Preparation and Application of a Bioorganic Nanoparticle-Enhanced PDL1-Targeted Small-Molecule Probe.

Programmed death ligand 1 (PDL1) is a specific molecular target for the diagnosis and immunotherapy of solid tumors. PET imaging can be used for noninvasive assessments of PDL1 expression in tumors to aid in therapy selection. The most frequently reported small-molecule radiotracer of PDL1 is limited by low imaging specificity, short residence time, and singular functionality.

Construction and Preclinical Evaluation of a I-Labeled Specific Antibody Targeting PD-L2 in Lung Cancer.

Programmed cell death-ligand 2 (PD-L2) is an important emerging molecule of the immune checkpoint, which is closely related to the prognosis of patients with immune checkpoint inhibitor (ICI) therapy. The quantification of PD-L2 can provide a potential reference for patients who benefit from ICI treatment. In this study, we used iodine isotope (I)-labeled PD-L2 antibody (ATL2) to noninvasively detect PD-L2 expression in mice with human lung adenocarcinoma A549 cell lines.

Preclinical evaluation and first in human study of AlF radiolabeled ODAP-urea-based PSMA targeting ligand for PET imaging of prostate cancer.

Purpose: This study aimed to introduce a novel [F]AlF-labeled ODAP-Urea-based Prostate-specific membrane antigen (PSMA) probe, named [F]AlF-PSMA-137, which was derived from the successful modification of glutamate-like functional group. The preclinically physical and biological characteristics of the probe were analyzed. Polit clinical PET/CT translation was performed to analyze its feasibility in clinical diagnosis of prostate cancer.

Evaluation of Ga- and Lu-Labeled HZ20 Angiotensin-Converting Enzyme 2-Targeting Peptides for Tumor-Specific Imaging.

Angiotensin-converting enzyme 2 (ACE2) is closely related to tumor formation. We developed the radiolabeled peptide pair Ga/Lu-labeled 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA)-conjugated DX600 (Ga/Lu-HZ20), for the targeting and mapping of ACE2-overexpressing tumors. Ga/Lu-HZ20 was prepared with a routine labeling method.

Noninvasive Mapping of Angiotensin Converting Enzyme-2 in Pigeons Using Micro Positron Emission Tomography.

The ACE2 receptor, as the potential entrance site of SARS-CoV-2-affected cells, plays a crucial role in spreading infection. The DX600 peptide is a competitive inhibitor of ACE2. We previously constructed the Ga-labeled DOTA-DX600 (also known as Ga-HZ20) peptide and confirmed its ACE2 binding ability both in vitro and in vivo.

An Albumin-Binding PSMA Ligand with Higher Tumor Accumulation for PET Imaging of Prostate Cancer.

Prostate-specific membrane antigen (PSMA) is an ideal target for the diagnosis and treatment of prostate cancer. Due to the short half-life in blood, small molecules/peptides are rapidly cleared by the circulatory system. Prolonging the half-life of PSMA probes has been considered as an effective strategy to improve the tumor detection.

Application Analysis of I-PPMN for Enhanced Retention in Tumors of Prostate Cancer Xenograft Mice.

Background: In recent years, nuclear medicine imaging and therapy for prostate cancer have radically changed through the introduction of radiolabeled prostate-specific membrane antigen (PSMA)-binding peptides. However, these small molecular probes have some inherent limitations, including high nephrotoxicity and short circulation time, which limits their utility in biological systems.

Methods And Results: In this study, organic melanin nanoparticles were used to directly label the long half-life radionuclide I (t=100.

SARS-CoV-2 receptor binding domain radio-probe: a non-invasive approach for angiotensin-converting enzyme 2 mapping in mice.

The spike protein of SARS-CoV-2 interacts with angiotensin-converting enzyme 2 (ACE2) of human respiratory epithelial cells, which leads to infection. Furthermore, low-dose radiation has been found to reduce inflammation and aid the curing of COVID-19. The receptor binding domain (RBD), a recombinant spike protein with a His tag at the C-terminus, binds to ACE2 in human body.

First-in-Humans Evaluation of a PD-L1-Binding Peptide PET Radiotracer in Non-Small Cell Lung Cancer Patients.

Ga-NOTA-WL12 is a peptide-based PET imaging agent. We conducted a first-in-human study of Ga-NOTA-WL12 for PET to study the in vivo biodistribution, metabolism, radiation dosimetry, safety, and potential for quantifying programmed death ligand-1 (PD-L1) expression levels in patients with advanced non-small cell lung cancer (NSCLC). In vitro assessment of the PD-L1 expression and cellular uptake of Ga-NOTA-WL12 was performed, followed by in vivo evaluation of Ga-NOTA-WL12 uptake in mouse models with tumors.

Molecular PET/CT Profiling of ACE2 Expression In Vivo: Implications for Infection and Outcome from SARS-CoV-2.

Rapid progress has been made to identify and study the causative agent leading to coronavirus disease 2019 (COVID-19) but many questions including who is most susceptible and what determines severity remain unanswered. Angiotensin-converting enzyme 2 (ACE2) is a key factor in the infection process of severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2). In this study, molecularly specific positron emission tomography imaging agents for targeting ACE2 are first developed, and these novel agents are evaluated in vitro, in preclinical model systems, and in a first-in-human translational ACE2 imaging of healthy volunteers and a SARS-CoV-2 recovered patient (NCT04422457).

Cu-PSMA-BCH: a new radiotracer for delayed PET imaging of prostate cancer.

Purpose: Develop a Cu labeled radiopharmaceutical targeting prostate specific membrane antigen (PSMA) and investigate its application for prostate cancer imaging.

Methods: Cu-PSMA-BCH was prepared and investigated for stability, PSMA specificity, and micro-PET imaging. With the approval of Ethics Committee of Beijing Cancer Hospital (No.

A Highly Specific Multiple Enhancement Theranostic Nanoprobe for PET/MRI/PAI Image-Guided Radioisotope Combined Photothermal Therapy in Prostate Cancer.

An integrated molecular probe for combined tumor-targeted multimodal imaging and therapy in the era of precision medicine requires a multiplexed platform that simultaneously has high targeting specificity, versatile conjugation capability, and biocompatibility. Here, a novel biocompatible melanin nanoprobe (PMNs-II-813) coupled with a highly specific prostate-specific membrane antigen small molecule inhibitor is developed for the targeted multimodal diagnosis and treatment of prostate cancer. The melanin nanoparticles demonstrate photoacoustic imaging and photothermal therapy (PTT) functionalities via strong near-infrared absorption.