Preclinical evaluation of Ga-labeled folic acid conjugates for visualization of inflammatory foci.

Introduction: Folate receptors (FR) have been considered a convenient target for different radiopharmaceuticals in recent years. Multifarious Ga-labeled folate conjugates have been proposed as promising agents for the PET imaging of FR-overexpressing malignant neoplasms. In addition, radiolabeled folate-based conjugates can be effective for imaging non-tumor pathological foci characterized by a pronounced cluster of activated macrophages.

Pentamethine cyanine dyes with alkynyl group as perspective structure for conjugation with targeting moiety.

We report a modified carbocyanine-based asymmetric fluorescent dye, suitable for the azide-alkyne cycloaddition reaction, that possesses promising photochemical properties (Φ = 0,49). As an example of usage of the new fluorophore, it was conjugated to a ligand targeting prostate-specific membrane antigen (PSMA), one of the widely utilized prostate cancer markers.

Structure-activity relationship study of mesyl and busyl phosphoramidate antisense oligonucleotides for unaided and PSMA-mediated uptake into prostate cancer cells.

Phosphorothioate (PS) group is a key component of a majority of FDA approved oligonucleotide drugs that increase stability to nucleases whilst maintaining interactions with many proteins, including RNase H in the case of antisense oligonucleotides (ASOs). At the same time, uniform PS modification increases nonspecific protein binding that can trigger toxicity and pro-inflammatory effects, so discovery and characterization of alternative phosphate mimics for RNA therapeutics is an actual task. Here we evaluated the effects of the introduction of several -alkane sulfonyl phosphoramidate groups such as mesyl (methanesulfonyl) or busyl (1-butanesulfonyl) phosphoramidates into gapmer ASOs on the efficiency and pattern of RNase H cleavage, cellular uptake , and intracellular localization.

Fluorescent Conjugates Based on Prostate-Specific Membrane Antigen Ligands as an Effective Visualization Tool for Prostate Cancer.

Fluorescent dyes are widely used in histological studies and in intraoperative imaging, including surgical treatment of prostate cancer (PC), which is one of the most common types of cancerous tumors among men today. Targeted delivery of fluorescent conjugates greatly improves diagnostic efficiency and allows for timely correct diagnosis. In the case of PC, the protein marker is a prostate-specific membrane antigen (PSMA).