Dopamine D3 receptors play a relevant role in the CNS modulating neurological activity, and its dysfunction is linked to disorders such as schizophrenia, drug abuse or Parkinson’s disease. There is a need for blood-brain barrier (BBB)-penetrant D3 receptor radiotracers with high brain uptake to be used for neurological and neuropsychiatric disease diagnosis.
A Cytosite Biopharma Inc. patent describes prodrugs of granzyme B-targeting compounds reported to be useful as granzyme B-imaging agents for the diagnosis of cancer.
Despite the success of CAR T-cell therapies for cancer immunotherapy, only a small percent of patients have a significant clinical response, and it is difficult to distinguish responders from nonresponders at an early stage with current imaging techniques.
Given the high prevalence of chronic kidney disease and the impact of renal fibrosis on the prognosis of these patients, there is a need for novel diagnostic tools to be able to detect pathological changes earlier and thus avoid progression to later stages of the disease.
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.
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