Construction of the Bioconjugate Py-Macrodipa-PSMA and Its In Vivo Investigations with Large La and Small Sc Radiometal Ions.

To harness radiometals in clinical settings, a chelator forming a stable complex with the metal of interest and targets the desired pathological site is needed. Toward this goal, we previously reported a unique set of chelators that can stably bind to both large and small metal ions, via a conformational switch. Within this chelator class, py-macrodipa is particularly promising based on its ability to stably bind several medicinally valuable radiometals including large La, Bi, and small Sc.

Targeted, Molecular Europium Probes Enable Luminescence-Guided Surgery and 1 Photon Post-Surgical Luminescence Microscopy of Solid Tumors.

Discrete luminescent lanthanide complexes represent a potential alternative to organic chromophores due to their tunability of optical properties, insensitivity to photobleaching, and large pseudo-Stokes shifts. Previously, we demonstrated that the lack of depth penetration of UV excitation required to sensitize discrete terbium and europium complexes can be overcome using Cherenkov radiation emitted by clinically employed radioisotopes in situ. Here, we show that the second-generation europium complexes [Eu(pcta-PEPA)] and [Eu(tacn-pic-PEPA)] (Φ = 57% and 76%, respectively) lower the limit of detection (LoD) to 1 nmol in the presence of 10 μCi of Cherenkov emitting isotopes, F and Ga.

Correction: Radiolabeling and evaluation of lanmodulin with biomedically relevant lanthanide isotopes.

[This corrects the article DOI: 10.1039/D3CB00020F.].

Radiolabeling and evaluation of lanmodulin with biomedically relevant lanthanide isotopes.

Short-lived, radioactive lanthanides comprise an emerging class of radioisotopes attractive for biomedical imaging and therapy applications. To deliver such isotopes to target tissues, they must be appended to entities that target antigens overexpressed on the target cell's surface. However, the thermally sensitive nature of biomolecule-derived targeting vectors requires the incorporation of these isotopes without the use of denaturing temperatures or extreme pH conditions; chelating systems that can capture large radioisotopes under mild conditions are therefore highly desirable.

,-Alkylation Clarifies the Role of - and -Protonated Intermediates in Cyclen-Based Cu Radiopharmaceuticals.

Radioisotopes of Cu, such as Cu and Cu, are alluring targets for imaging (e.g., positron emission tomography, PET) and radiotherapeutic applications.

The expanding role of primary care providers in care of individuals with kidney disease.

An estimated 37 million Americans have chronic kidney disease (CKD). Primary care providers (PCPs) have long played a critical role in detecting CKD and preventing disease progression, particularly in the early stages of the disease. With recent studies demonstrating substantial improvements in kidney outcomes with use of sodium glucose cotransporter 2 (SGLT2) inhibitors, PCPs have an even greater opportunity to improve care of individuals with CKD.

Multiplex and In Vivo Optical Imaging of Discrete Luminescent Lanthanide Complexes Enabled by In Situ Cherenkov Radiation Mediated Energy Transfer.

Recently, we pioneered the application of Cherenkov radiation (CR) of radionuclides for the in situ excitation of discrete Eu(III) and Tb(III) complexes. CR is produced by isotopes decaying under emission of charged particles in dielectric media and exhibits a maximum intensity below 400 nm. We have demonstrated that luminescent lanthanide antenna complexes are ideal acceptors for Cherenkov radiation-mediated energy transfer (CRET).

Establishing Radiolanthanum Chemistry for Targeted Nuclear Medicine Applications.

We report the first targeted nuclear medicine application of the lanthanum radionuclides La. These isotopes represent a matched pair for diagnosis via the positron emissions of La and therapy mediated by the Auger electron emissions of La. We identify two effective chelators, known as DO3Apic and macropa, for these radionuclides.