Researchers from University North Carolina, Chapel Hill have discovered prostate-specific member antigen (PSMA)-targeted agents with reduced salivary gland uptake while maintaining high tumor uptake. Synthesis and subsequent screening of PSMA agents bearing different chelators and targeting ligands led to the identification of two lead agents, NOTA-UNC-PSMA-2 and DOTA-UNC-PSMA-2.
It seems unlikely that American poet and civil rights activist Maya Angelou spent much time thinking about translational research. But two quotes of hers capture the essence of the interplay between bench and bedside: “I did then what I knew how to do. Now that I know better, I do better” and “I’ve learned that I still have a lot to learn.” At the 2023 Annual Congress of the European Academy of Neurology, Mary Reilly described the relationship between bench and bedside as “a continuous circle of translation,” with each cycle beginning with patients and their needs.
Because of its overexpression in many solid tumors, gastrin-releasing peptide receptor (GRPR) represents a promising therapeutic target and imaging marker for cancer. Gastrin-releasing peptide (GRP) and bombesin are the natural ligands for GRPR. To improve in vivo stability, researchers at the University of British Columbia synthesized two 68Ga-labeled GRPR agonists by replacing Val and His sequences in GPR(20-27) and bombesin(7-14) with Tle and NMe-His, respectively.
The fibroblast activation protein (FAP) is a known biomarker expressed on the surface of cancer-associated fibroblasts (CAF), as well as an important target that distinguishes normal fibroblasts from CAF. Researchers from National Yang-Ming University recently reported the discovery and preclinical evaluation of a novel PET tracer, [18F]FEQGP, being developed for the detection of FAB expression in CAF imaging.
Four-repeat (4R)-tauopathies are neurodegenerative diseases whose main hallmarks are brain accumulations of specific protein tau isoforms that lead to syndromes such as progressive supranuclear palsy (PSP) or corticobasal syndrome. There are yet no sensitive-enough PET tracers for 4R-tauopathies.
AC Immune SA has patented 4h-imidazo[1,5-b]pyrazole derivatives and labeled compounds targeting α-synuclein (SNCA). They are reported to be useful for diagnosis of multiple system atrophy, Parkinson’s dementia, Lewy body dementia, Alzheimer’s and Parkinson’s disease, among others.
α-Synucleinopathies constitute a set of neurological disorders including Parkinson’s disease (PD), dementia with Lewy bodies, multiple systems atrophy (MSA), and other rare disorders. The development of positron emission tomography (PET) tracers for imaging α-synuclein aggregates is essential for performing efficient and accurate diagnosis, tracking disease progression and monitoring efficacy of potential therapies.
Previous studies have identified a promising target and potential biomarker for diagnosing and treating gastrointestinal and esophageal cancers: claudin18.2 (CLDN18.2), a tight junction protein overexpressed in these and other solid tumors.
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