Carbonic anhydrase IX (CAIX) is a transmembrane protein involved in cell proliferation and transformation that is expressed in clear-cell renal cell carcinoma (ccRCC), colorectal cancer (CRC), and other hypoxic tumor types, but has low expression in healthy tissues.
Researchers at Merck & Co. Inc. have presented the discovery of novel selective metabotropic glutamate receptor 2 (mGluR2) negative allosteric modulators (NAMs) as potential PET imaging agents. Synthesis and optimization of a series of analogues of a potent and selective mGluR2 NAM resulted in the identification of compound MK-8056 as a high-affinity mGluR2 NAM (Ki=0.19 nM) with desirable lipophilicity (logD7.0=2.46) and low P-gp susceptibility.
In a study reported in the online edition of Science on Aug. 10, 2023, a group of synthetic biologists from the University of California (UC) San Diego and clinicians from Australia have engineered synthetic bacteria to detect specific DNA sequences in the genomes of colorectal cancer (CRC) cells and organoids. This living cell sensor capable of detecting cancer in the colons of mice has the potential to steer the way to new biosensors capable of identifying various infections, cancers and other diseases.
Fuzionaire Diagnostics Inc. has changed its name to Fuzionaire Theranostics Inc. to better reflect the company’s pipeline of paired fluorine-18 PET diagnostics and radioligand therapies to find and treat cancer.
Characterized by periods of deep and profound depression alternating with periods of excessive mania mood swings with diminished sleep, bipolar spectrum disorder (BSD) affected an estimated 40 million people globally in 2019 in the U.S. with a major part of the problem attributed to delays in diagnosis including a mean time of 5-13 years. These delays in BSD diagnosis exert lifelong impacts including heightened suicide risk, relationship strains, impaired work/education performance, significant financial burdens and increased risk for cardiovascular disease.
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.
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.
Helmholtz Zentrum Dresden Rossendorf has patented 3-((3-([1,1’-biphenyl]-3-ylmethoxy)phenoxy)methyl)benzonitrile derivatives that are radiolabeled compounds targeting programmed cell death 1 ligand 1 (PD-L1; CD274). They are reported to be potentially useful for the diagnosis and/or radionuclide therapy treatment of cancer and SARS-CoV-2.
Researchers from the Mayo Clinic have reported findings from the preclinical evaluation of a novel cardiac targeting peptide (CTP)-based radiotracer – [68Ga]NOTA-CTP – being developed as a myocardial perfusion imaging PET probe.
RSS
