Towards Effective Targeted Alpha Therapy for Neuroendocrine Tumours: A Review.

This review article explores the evolving landscape of Molecular Radiotherapy (MRT), emphasizing Peptide Receptor Radionuclide Therapy (PRRT) for neuroendocrine tumours (NETs). The primary focus is on the transition from β-emitting radiopharmaceuticals to α-emitting agents in PRRT, offering a critical analysis of the radiobiological basis, clinical applications, and ongoing developments in Targeted Alpha Therapy (TAT). Through an extensive literature review, the article delves into the mechanisms and effectiveness of PRRT in targeting somatostatin subtype 2 receptors, highlighting both its successes and limitations.

Monoclonal Antibodies for Targeted Fluorescence-Guided Surgery: A Review of Applicability across Multiple Solid Tumors.

This study aims to review the status of the clinical use of monoclonal antibodies (mAbs) that have completed or are in ongoing clinical trials for targeted fluorescence-guided surgery (T-FGS) for the intraoperative identification of the tumor margins of extra-hematological solid tumors. For each of them, the targeted antigen, the mAb generic/commercial name and format, and clinical indications are presented, together with utility, doses, and the timing of administration. Based on the current scientific evidence in humans, the top three mAbs that could be prepared in a GMP-compliant bank ready to be delivered for surgical purposes are proposed to speed up the translation to the operating room and produce a few readily available "off-the-shelf" injectable fluorescent probes for safer and more effective solid tumor resection.

Quantum Dot Imaging Agents: Haematopoietic Cell Interactions and Biocompatibility.

Quantum dots (QDs) are semi-conducting nanoparticles that have been developed for a range of biological and non-biological functions. They can be tuned to multiple different emission wavelengths and can have significant benefits over other fluorescent systems. Many studies have utilised QDs with a cadmium-based core; however, these QDs have since been shown to have poor biological compatibility.

Impact of Surface Ligand on the Biocompatibility of InP/ZnS Quantum Dots with Platelets.

InP/ZnS quantum dots (QDs) have received a large focus in recent years as a safer alternative to heavy metal-based QDs. Given their intrinsic fluorescent imaging capabilities, these QDs can be potentially relevant for in vivo platelet imaging. The InP/ZnS QDs are synthesized and their biocompatibility investigated through the use of different phase transfer agents.

ATP-responsive Mn(II)-based contrast agent for MRI.

A novel diacetylpyridylcarbohydrazide-DAPyCOHz-based manganese(II) chelate with dipicolylamine/zinc(II) (DPA/Zn) arms (MnLDPA-Zn2) was developed for adenosine triphosphate (ATP) responsive magnetic resonance imaging (MRI) contrast applications. Compound 2 shows enhanced relaxivity ( = 11.52 mM s) upon selective ATP binding over other phosphates.

Inorganic Chemistry of the Tripodal Picolinate Ligand with Gallium(III) and Radiolabeling with Gallium-68.

We report here the improved synthesis of the tripodal picolinate chelator , with an overall yield of 41% over five steps, in comparison to the previously reported 6% yield. was investigated for its coordination chemistry with Ga(III) and radiolabeling properties with gallium-68 (Ga). The obtained crystal structure for [Ga()] shows that the three picolinate arms coordinate to the Ga(III) ion, fully occupying the octahedral coordination geometry.

Redox double-switch cancer theranostics through Pt(IV) functionalised manganese dioxide nanostructures.

Manganese dioxide (MnO)-based nanostructures have emerged as promising tumour microenvironment (TME) responsive platforms. Herein, we used a one-pot reaction to prepare MnO nanostructures with Pt(IV) prodrugs as redox- (and thus TME-) responsive theranostics for cancer therapy, in which the Pt(IV) complexes act as prodrugs of cisplatin (Pt(II)), a clinical chemotherapeutic drug. The cytotoxicity of these MnO-Pt(IV) probes was evaluated in two and three dimensional (2D and 3D) A549 cell models and found to be as effective as active drug cisplatin in 3D models.

Platelet zinc status regulates prostaglandin-induced signaling, altering thrombus formation.

Background: Approximately 17.3% of the global population exhibits an element of zinc (Zn) deficiency. One symptom of Zn deficiency is increased bleeding through impaired hemostasis.

Insights into the Effect of Magnetic Confinement on the Performance of Magnetic Nanocomposites in Magnetic Hyperthermia and Magnetic Resonance Imaging.

The combination of superparamagnetic iron oxide nanoparticles (SPIONs) and lipid matrices enables the integration of imaging, drug delivery, and therapy functionalities into smart theranostic nanocomposites. SPION confinement creates new interactions primarily among the embedded SPIONs and then between the nanocomposites and the surroundings. Understanding the parameters that rule these interactions in real interacting (nano)systems still represents a challenge, making it difficult to predict or even explain the final (magnetic) behavior of such systems.

, a Chelator for Ga Positron Emission Tomography: Hydroxide Coordination Increases Biological Stability of [Ga][Ga(BnDT3A)(OH)].

The chelator was used to produce a novel Ga complex for positron emission tomography (PET). Unusually, this system is stabilized by a coordinated hydroxide in aqueous solutions above pH 5, which confers sufficient stability for it to be used for PET. complexes Ga in a hexadentate manner, forming a complex with log ([Ga()]) = 18.

Practical Considerations of Dissolved Oxygen Levels for Platelet Function under Hypoxia.

Investigating human platelet function in low-oxygen environments is important in multiple settings, including hypobaric hypoxia (e.g., high altitude), sea level hypoxia-related disease, and thrombus stability.

Smart magnetic resonance imaging-based theranostics for cancer.

Smart theranostics are dynamic platforms that integrate multiple functions, including at least imaging, therapy, and responsiveness, in a single agent. This review showcases a variety of responsive theranostic agents developed specifically for magnetic resonance imaging (MRI), due to the privileged position this non-invasive, non-ionising imaging modality continues to hold within the clinical imaging field. Different MRI smart theranostic designs have been devised in the search for more efficient cancer therapy, and improved diagnostic efficiency, through the increase of the local concentration of therapeutic effectors and MRI signal intensity in pathological tissues.

Scandium calix[]arenes ( = 4, 6, 8): structural, cytotoxicity and ring opening polymerization studies.

Interaction of [Sc(OR)3] (R = iPr or triflate) with p-tert-butylcalix[n]arenes, where n = 4, 6, or 8, affords a number of intriguing structural motifs, which are relatively non-toxic (cytotoxicity evaluated against cell lines HCT116 and HT-29) and a number were capable of the ring opening polymerization (ROP) of cyclohexene oxide.

A Single-Pot Template Reaction Towards a Manganese-Based Contrast Agent.

Manganese-based contrast agents (MnCAs) have emerged as suitable alternatives to gadolinium-based contrast agents (GdCAs). However, due to their kinetic lability and laborious synthetic procedures, only a few MnCAs have found clinical MRI application. In this work, we have employed a highly innovative single-pot template synthetic strategy to develop a MnCA, , and studied the most important physicochemical properties in vitro.

NIR-quantum dots in biomedical imaging and their future.

Fluorescence imaging has gathered interest over the recent years for its real-time response and high sensitivity. Developing probes for this modality has proven to be a challenge. Quantum dots (QDs) are colloidal nanoparticles that possess unique optical and electronic properties due to quantum confinement effects, whose excellent optical properties make them ideal for fluorescence imaging of biological systems.

A Single-Pot Template Reaction Towards a Manganese-Based T Contrast Agent.

Manganese-based contrast agents (MnCAs) have emerged as suitable alternatives to gadolinium-based contrast agents (GdCAs). However, due to their kinetic lability and laborious synthetic procedures, only a few MnCAs have found clinical MRI application. In this work, we have employed a highly innovative single-pot template synthetic strategy to develop a MnCA, MnL , and studied the most important physicochemical properties in vitro.

Tunable NIR-II emitting silver chalcogenide quantum dots using thio/selenourea precursors: preparation of an MRI/NIR-II multimodal imaging agent.

Aqueous-stable, Cd- and Pb-free colloidal quantum dots with fluorescence properties in the second near-infrared region (NIR-II, 1000-1400) are highly desirable for non-invasive deep-tissue optical imaging and biosensing. The low band-gap semiconductor, silver chalcogenide, offers a non-toxic and stable alternative to existing Pd, As, Hg and Cd-based NIR-II colloidal quantum dots (QDs). We report facile access to NIR-II emission windows with Ag2X (X = S, Se) QDs using easy-to-prepare thio/selenourea precursors and their analogues.

Synthesis of a porphyrin with histidine-like chelate: an efficient path towards molecular PDT/SPECT theranostics.

The goal of "personalised" medicine has seen a growing interest in the development of theranostic agents. Bifunctional, and targeted-trifunctional, theranostic water-soluble porphyrins with a histidine-like chelating group have been synthesised via copper-catalysed azide-alkyne cycloaddition (CuAAC) "click" chemistry in high yield and purity. They are capable of photodynamic treatment and [99mTc(CO)3]+ complexation for single-photon emission computed tomography (SPECT) imaging, with a radiochemical yield of >95%.

The use of yttrium in medical imaging and therapy: historical background and future perspectives.

Yttrium is a chemically versatile rare earth element that finds use in a range of applications including lasers and superconductors. In medicine, yttrium-based materials are used in medical lasers and biomedical implants. This is extended through the array of available yttrium isotopes to enable roles for Y complexes as radiopharmaceuticals and Y tracers for positron emission tomography (PET) imaging.

Metallostar Assemblies Based on Dithiocarbamates for Use as MRI Contrast Agents.

Two different octadentate gadolinium chelates based on DO3A and DOTAGA chelates (hydration number = 1) have been used to prepare a series of bi-, tri-, and tetrametallic d-f mixed-metal complexes. The piperazine-based dithiocarbamate linker ensures that rotation of the gadolinium chelates is restricted, leading to enhanced relaxivity () values, which increase with the overall mass and number of gadolinium units. The value (at 10 MHz, 25 °C) per gadolinium unit rises from 5.

Evaluation of a Bispidine-Based Chelator for Gallium-68 and of the Porphyrin Conjugate as PET/PDT Theranostic Agent.

In this study a bispidine ligand has been applied to the complexation of gallium(III) and radiolabelled with gallium-68 for the first time. Despite its 5-coordinate nature, the resulting complex is stable in serum for over two hours, demonstrating a ligand system well matched to the imaging window of gallium-68 positron emission tomography (PET). To show the versatility of the bispidine ligand and its potential use in PET, the bifunctional chelator was conjugated to a porphyrin, producing a PET/PDT-theranostic, which showed the same level of stability to serum as the non-conjugated gallium-68 complex.

Water-Soluble Rhenium Phosphine Complexes Incorporating the PhC(X) Motif (X = O, NH): Structural and Cytotoxicity Studies.

Reaction of [ReOCl(PPh)] or [ReOI(PPh)] with 2,2'-diphenylglycine (dpgH) in refluxing ethanol afforded the air-stable complex [ReO(dpgH)(dpg)(PPh)] (). Treatment of [ReO(OEt)I(PPh)] with 1,2,3-triaza-7-phosphaadamantane (PTA) afforded the complex [ReO(OEt)I(PTA)] (). Reaction of [ReOI(PTA)] with dpgH led to the isolation of the complex [Re(NCPh)I(PTA)]·0.

Combined Magnetic Resonance Imaging and Photodynamic Therapy Using Polyfunctionalised Nanoparticles Bearing Robust Gadolinium Surface Units.

A robust dithiocarbamate tether allows novel gadolinium units based on DOTAGA (q=1) to be attached to the surface of gold nanoparticles (2.6-4.1 nm diameter) along with functional units offering biocompatibility, targeting and photodynamic therapy.