Researchers from Peking University (PKU) recently presented the discovery and preclinical evaluation of a novel small-molecule inhibitor of pan-αv integrin, C19-9-21, being developed for the treatment of prostate cancer.
Researchers from Washington University in St. Louis and affiliated organizations have provided details on the discovery and preclinical evaluation of [64Cu]NODAGA-PEG4-SL-022-GGS, a novel small peptide imaging agent for evaluating CD38 expression.
Researchers from the University of North Carolina, Chapel Hill and affiliated organizations have reported the development and preclinical evaluation of [18F]F-ZW-cinacalcet, a novel PET agent targeting the calcium-sensing receptor (CaSR) for parathyroid imaging.
Researchers from Duke University presented the discovery and preclinical evaluation of [211At]YF-2, a next-generation prostate-specific membrane antigen (PSMA)-targeted radiopharmaceutical.
Actinium-226 (226Ac) has been previously proposed as a potential surrogate isotope for the development of 225Ac radiopharmaceuticals for targeted alpha therapy (TAT). The benefits of 226Ac include its theoretically superior therapeutic potency as well as a short half-life of its progeny, expected to minimize the toxicities. Researchers from TRIUMF, University of British Columbia and affiliated organizations recently reported the discovery of a novel matched 225/226Ac-radiopharmaceutical pair, [225Ac]crown-TATE and [226Ac]crown-TATE, and conducted studies aiming to compare the radiation dosimetry of these candidates.
Researchers from Stanford University and affiliated organizations have provided details on the discovery and preclinical evaluation of [11C]MGX-10S, a novel PET tracer for GPR84, which is a G protein-coupled receptor (GPCR) expressed predominately on myeloid cells.
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.
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.
Cholemic nephropathy (CN) is an acute renal dysfunction that occurs after high bile acid (BA) levels provoke epithelial cell damage and tubular obstruction in the kidneys.
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.
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