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.
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.
Recent genome-wide association studies have elucidated a spliced variant (rs72613567:TA) in 17β-hydroxysteroid dehydrogenase 13 (HSD17B13) found to be associated with decreased risk of chronic liver disorders. The presence of this variant also correlates with delayed onset of autoimmune hepatitis in carriers.
Nonalcoholic steatohepatitis (NASH) is the most severe form of nonalcoholic fatty liver disease, where in addition to the accumulation of fat in the liver, there is also chronic inflammation and hepatocyte injury. With no therapy approved yet, selective thyroid hormone receptor-β (THR-β) agonism has yielded good results in ongoing clinical development.
Cyclophilins are a group of proteins involved in cell metabolism and homeostasis. One of the members, CypD, is located in mitochondria and plays an important role as a regulator of mitochondrial permeability transition (mPT) and necrotic cell death resulting in persistent mPT opening that, in turn, leads to hepatic ischemia/reperfusion injury (IRI).
Merck & Co. Inc. has reported the development of a novel monobactam for use in combination with its class A/C β-lactamase inhibitor (BIL) relebactam (MK-7655) in order to achieve the broadest activity against multidrug-resistant (MDR) gram-negative pathogens that express a variety of β-lactamases. The in vitro efficacy of the combination of the monobactam – MSD-045934942 – against a panel of MDR and non-MDR gram-negative bacteria was evaluated using in vitro broth microdilution testing.
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