Copper-64 (T_1/2 = 12.7 h) is a positron and beta-emitting isotope, with decay characteristics suitable for both positron emission tomography (PET) imaging and radiotherapy of cancer. Copper-67 (T_1/2 = 61.8 h) is a beta and gamma emitter, appropriate for radiotherapy β-energy and with a half-life suitable for single-photon emission computed tomography (SPECT) imaging. The chemical identities of ⁶⁴Cu and ⁶⁷Cu isotopes allow for convenient use of the same chelating molecules for sequential PET imaging and radiotherapy. A recent breakthrough in ⁶⁷Cu production opened previously unavailable opportunities for a reliable source of ⁶⁷Cu with high specific activity and purity. These new opportunities have reignited interest in the use of copper-containing radiopharmaceuticals for the therapy, diagnosis, and theranostics of various diseases. Herein, we summarize recent (2018–2023) advances in the use of copper-based radiopharmaceuticals for PET, SPECT imaging, radiotherapy, and radioimmunotherapy.

BODIPY chromophores (4,4-difluoro-4-bora-3a,4a-diaza-s-indacene) are one of the most versatile fluorophores which are commonly used in a variety of scientific fields. The combination of excellent photophysical properties with the possibility of easy chemical modification of structure, chemical and photostability determines the application of BODIPY in biomedicine, photocatalysis, analytical chemistry and materials science. This review summarizes approaches to the synthesis and modification of BODIPY, discussing both classical and recently-published synthetic and postfunctionalization approaches. An influence of BODIPY structure and various postfunctionalization methods on photophysical properties of the fluorophores and their potential applications in biomedicine, materials science and biosensorics are also discussed. The bibliography includes 344 references.

Novel triantennary N-acetylgalactosamine derivatives of tris(hydroxymethyl)aminomethane were synthesized and used to form complexes with the asialoglicoprotein receptor expressed on the hepatocellular surface. The equilibrium dissociation constants (K_D) of the complexes of the asialoglicoprotein receptor with the synthesized compounds were measured by surface plasmon resonance spectroscopy. The K_D values were in the subnanomolar range, being 6 orders of magnitude lower than the respective values for the complex of the receptor with the natural N-acetylgalactosamine ligand. The resulting data suggest that the synthesized ligands are promising agents for targeted delivery of various therapeutic agents in hepatocytes.

Alzheimer’s disease (AD) is a worldwide problem due to the lack of effective therapy and accurate methods for timely diagnosis. The complexity of AD’s pathophysiology complicates the development of effective therapeutic agents, as most drugs act on only one therapeutic target, bypassing others. The design and development of multifunctional agents capable of altering metal ion-induced abnormalities, oxidative stress, and toxic beta amyloid (Aβ) aggregates is of interest. Herein, we report the first boron dipyrromethene (BODIPY) based bifunctional copper chelator with clioquinol, BDP-CLQ, capable of both optical detection of Aβ fibrils and copper chelation, with multiple anti-AD properties. Foremost, BDP-CLQ demonstrated a 3-fold and 5-fold fluorescence increase at 650 nm and 565 nm in the presence of Aβ and effective copper chelation (pK_d = 16.6 ± 0.3). In addition, BDP-CLQ demonstrated a potent inhibition of Aβ aggregation, reduction in Aβ-induced stiffness of neuronal cells, and antioxidant activity. BDP-CLQ is the first BODIPY-based fluorescent probe with multiple anti-AD activities, as well as the first clioquinol-based probe capable of Aβ optical visualization. This study demonstrates the prospects of the development of clioquinol-based theranostic probes since this allows combining several promising anti-AD actions in a single molecule and developing multi-targeted drugs.