Synthesis and Application of 1-[F]Fluoro-4-isothiocyanatobenzene for Radiofluorination of Peptides in Aqueous Medium.

Conjugation of radiofluorinated prosthetic groups to primary amines of peptides in an aqueous medium is still considerably challenging. Herein, we report a one-pot cascade synthesis of 1-[F]fluoro-4-isothiocyanatobenzene ([F]), an isothiocyanate-functionalized prosthetic group for radiolabeling of various peptides in aqueous medium. The developed compound [F] was synthesized in >99% radiochemical purity with 22.

Aspects and prospects of preclinical theranostic radiopharmaceutical development.

This article provides an overview of preclinical theranostic radiopharmaceutical development, highlighting aspects of the preclinical development stages that can lead towards a clinical trial. The key stages of theranostic radiopharmaceutical development are outlined, including target selection, tracer development, radiopharmaceutical synthesis, automation and quality control, radiopharmaceutical analysis, selecting a suitable model, preclinical imaging and pharmacokinetic analysis, preclinical therapeutic analysis, dosimetry, toxicity, and preparing for clinical translation. Each stage is described and augmented with examples from the literature.

Synthesis and evaluation of anti-PD-L1-B11 antibody fragments for PET imaging of PD-L1 in breast cancer and melanoma tumor models.

There is a critical need to non-invasively assess the PD-L1 expression in tumors as a predictive biomarker for determining the efficacy of anti-PD-1/PD-L1 immunotherapies. Non-invasive imaging modality like positron emission tomography (PET) can be a powerful tool to assess the PD-L1 expression in the whole body including multiple metastases as a patient selection criterion for the anti-PD-1/PD-L1 immunotherapy. In this study, we synthesized B11-nanobody, B11-scFv and B11-diabody fragments from the full-length anti-PD-L1 B11 IgG.

Synthesis and preliminary evaluation of novel PET probes for GSK-3 imaging.

Non-invasive imaging of GSK-3 expression in the brain will help to understand the role of GSK-3 in disease pathology and progression. Herein, we report the radiosynthesis and evaluation of two novel isonicotinamide based F labeled PET probes, [F]2 and [F]6 for noninvasive imaging of GSK3. Among the developed PET probes, the in vitro blood-brain permeability coefficient of 2 (38 ± 20 × 10 cm/s, n = 3) was found to be better than 6 (8.

A highly efficient deep red-emitting Mn-powered oxyfluoride nanophosphor developed for plant growth and optical thermometric applications.

This research mainly highlighted an intense deep red-emitting and Mn-powered oxyfluoride nanophosphor, MgGeOF:0.01Mn (MGOF:Mn), which was synthesized adopting a scalable synthesis route for commercial temperature sensing and artificial plant growth applications. The electron microscopic analysis confirmed the formation of nanosized particles without any defined shape or size distribution.

Positron Emission Tomography Imaging of Cell Trafficking: A Method of Cell Radiolabeling.

Stem cell and chimeric antigen receptor (CAR) T-cell therapies are emerging as promising therapeutics for organ regeneration and as immunotherapy for various cancers. Despite significant progress having been made in these areas, there is still more to be learned to better understand the pharmacokinetics and pharmacodynamics of the administered therapeutic cells in the living system. For noninvasive, in vivo tracking of cells with positron emission tomography (PET), a novel [Zr]Zr-p-isothiocyanatobenzyl-desferrioxamine ([Zr]Zr-DBN)-mediated cell radiolabeling method has been developed utilizing Zr (t1/2 78.

Radiometals in Imaging and Therapy: Highlighting Two Decades of Research.

The present article highlights the important progress made in the last two decades in the fields of molecular imaging and radionuclide therapy. Advancements in radiometal-based positron emission tomography, single photon emission computerized tomography, and radionuclide therapy are illustrated in terms of their production routes and ease of radiolabeling. Applications in clinical diagnostic and radionuclide therapy are considered, including human studies under clinical trials; their current stages of clinical translations and findings are summarized.

PET and SPECT Imaging of ALS: An Educational Review.

Amyotrophic lateral sclerosis (ALS) is a disease leading to progressive motor degeneration and ultimately death. It is a complex disease that can take a significantly long time to be diagnosed, as other similar pathological conditions must be ruled out for a definite diagnosis of ALS. Noninvasive imaging of ALS has shed light on disease pathology and altered biochemistry in the ALS brain.

A Review of Theranostics: Perspectives on Emerging Approaches and Clinical Advancements.

Theranostics is the combination of two approaches-diagnostics and therapeutics-applied for decades in cancer imaging using radiopharmaceuticals or paired radiopharmaceuticals to image and selectively treat various cancers. The clinical use of theranostics has increased in recent years, with U.S.

Morpho-nutritional status of micronutrient efficient wheat (Triticum aestivum L.) genotypes under changing environments.

In India, where cereal-based meals make up the majority of the daily diet, bread wheat (Triticum aestivum L.) is a key grain crop. Micronutrient deficiencies are a result of the lack of a diverse food culture in the nation.

The role of selenoproteins in neurodevelopment and neurological function: Implications in autism spectrum disorder.

Selenium and selenoproteins play a role in many biological functions, particularly in brain development and function. This review outlines the role of each class of selenoprotein in human brain function. Most selenoproteins play a large antioxidant role within the brain.

Isotopic composition of serum zinc and copper in healthy children and children with autism spectrum disorder in North America.

To better understand zinc and copper regulation and their involvement in various biochemical pathways as it relates to autism spectrum disorder (ASD), isotopic composition of serum zinc and copper were evaluated in both healthy children and children with ASD in North America. No significant difference in isotopic composition of serum zinc or copper with respect to healthy controls and ASD children were identified. However, the isotopic composition of serum copper in boys was found to be enriched in Cu in comparison to previously published healthy adult copper isotopic composition.

Evaluation of different Zr-labeled synthons for direct labeling and tracking of white blood cells and stem cells in healthy athymic mice.

Cell based therapies are evolving as an effective new approach to treat various diseases. To understand the safety, efficacy, and mechanism of action of cell-based therapies, it is imperative to follow their biodistribution noninvasively. Positron-emission-tomography (PET)-based non-invasive imaging of cell trafficking offers such a potential.

Governing the crystallographic sites for tuning Eu emission in an apatite oxyfluoride host to be applied for superior white light emitting diodes.

Single white light-emitting phosphors for near-UV-converted white light-emitting diodes (WLEDs) are the best alternatives to tricolour phosphor blends and blue light converted yellow-emitting garnets. Nevertheless, achieving white light with elevated colour rendering (CRI) from a single-phase phosphor activated with a lone activator ion is a major challenge. This study aimed at the generation of white light from a single-phase composition activated only with europium.

Design, Synthesis, and Preliminary Evaluation of [Ga]Ga-NOTA-Insulin as a PET Probe in an Alzheimer's Disease Mouse Model.

Aberrant insulin signaling has been considered one of the risk factors for the development of Alzheimer's disease (AD) and has drawn considerable attention from the research community to further study its role in AD pathophysiology. Herein, we describe the development of an insulin-based novel positron emission tomography (PET) probe, [Ga]Ga-NOTA-insulin, to noninvasively study the role of insulin in AD. The developed PET probe [Ga]Ga-NOTA-insulin showed a significantly higher uptake (0.

A new solid target design for the production of Zr and radiosynthesis of high molar activity [Zr]Zr-DBN.

Due to the advent of various biologics like antibodies, proteins, cells, viruses, and extracellular vesicles as biomarkers for disease diagnosis, progression, and as therapeutics, there exists a need to have a simple and ready to use radiolabeling synthon to enable noninvasive imaging trafficking studies. Previously, we reported [Zr]zirconium--isothiocyanatobenzyl-desferrioxamine ([Zr]Zr-DBN) as a synthon for the radiolabeling of biologics to allow PET imaging of cell trafficking. In this study, we focused on improving the molar activity (A) of [Zr]Zr-DBN, by enhancing Zr production on a low-energy cyclotron and developing a new reverse phase HPLC method to purify [Zr]Zr-DBN.

Dynamic Imaging of Chimeric Antigen Receptor T Cells with [18F]Tetrafluoroborate Positron Emission Tomography/Computed Tomography.

T cells genetically engineered to express chimeric antigen receptors (CAR) have shown unprecedented results in pivotal clinical trials for patients with B cell malignancies or multiple myeloma (MM). However, numerous obstacles limit the efficacy and prohibit the widespread use of CAR T cell therapies due to poor trafficking and infiltration into tumor sites as well as lack of persistence in vivo. Moreover, life-threatening toxicities, such as cytokine release syndrome or neurotoxicity, are major concerns.

Corrigendum: Evaluation of Zn, Cu, and Se Levels in the North American Autism Spectrum Disorder Population.

[This corrects the article DOI: 10.3389/fnmol.2021.

Unusual Increased Blood Pool Activity on 68Ga-DOTATATE PET/CT in a Patient With Metastatic Neuroendocrine Disease.

68Ga-DOTATATE is a well-established, positron-emitting, somatostatin receptor-binding radiopharmaceutical. We present an unusual case of transiently increased blood pool uptake of 68Ga-DOTATATE in a patient with well-differentiated stage IV neuroendocrine tumor, with Ki-67 <2% (WHO grade 1) maintained on lanreotide. During serial 68Ga-DOTATATE PET/CT examinations, increased blood pool accumulation of presumably unbound 68Ga was demonstrated, which could impact the Kenning score and lead to a false treatment response assessment.

Development of a Clinically Relevant Reporter for Chimeric Antigen Receptor T-cell Expansion, Trafficking, and Toxicity.

Although chimeric antigen receptor T (CART)-cell therapy has been successful in treating certain hematologic malignancies, wider adoption of CART-cell therapy is limited because of minimal activity in solid tumors and development of life-threatening toxicities, including cytokine release syndrome (CRS). There is a lack of a robust, clinically relevant imaging platform to monitor expansion and trafficking to tumor sites. To address this, we utilized the sodium iodide symporter (NIS) as a platform to image and track CART cells.

Non-invasive immunoPET imaging of PD-L1 using anti-PD-L1-B11 in breast cancer and melanoma tumor model.

Introduction: Immunotherapy targeting PD-1/PD-L1 immune checkpoint inhibition (ICI) is efficacious in various solid and hematologic malignancies. However, the response rate to PD-1/PD-L1 therapy is only 15-35%. To obtain optimal clinical response to ICI therapies, a reliable assessment of tumor PD-L1 expression is needed to select appropriate patients, and a non-invasive imaging-based assessment of PD-L1 expression is critically needed.

Evaluation of Zn, Cu, and Se Levels in the North American Autism Spectrum Disorder Population.

Metal ion dyshomeostasis and disparate levels of biometals like zinc (Zn), copper (Cu), and selenium (Se) have been implicated as a potential causative factor for Autism Spectrum Disorder (ASD). In this study, we have enrolled 129 children (aged 2-4 years) in North America, of which 64 children had a diagnosis of ASD and 65 were controls. Hair, nail, and blood samples were collected and quantitatively analyzed for Zn, Cu and Se using inductively coupled plasma mass spectrometry (ICP-MS).