Researchers from China Pharmaceutical University have reported the discovery of novel orally bioavailable fms-like tyrosine kinase 3 (FLT3) inhibitors as potential candidates for the treatment of acute myeloid leukemia (AML). Synthesis and optimization of a novel series of FLT3 inhibitors led to the identification of LT-540-717 as the lead candidate.
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.
Vertex Pharmaceuticals Inc. has developed spirocyclic inhibitors of apolipoprotein L1 (APOL1) reported to be useful for the treatment of pancreatic cancer and focal segmental glomerulosclerosis.
Research at Humanwell Healthcare (Group) Co. Ltd. has led to the identification of interleukin-1 receptor-associated kinase 4 (IRAK-4) inhibitors reported to be useful for the treatment of cancer and autoimmune diseases.
Incyte Corp. has patented bicyclic amines acting as cyclin-dependent kinase 12 (CDK12) inhibitors and reported to be useful for the treatment of cancer.
A Shandong Luye Pharmaceutical Co. Ltd. patent discloses serine/threonine-protein kinase PLK1 (STPK13) inhibitors reported to be useful for the treatment of cancer, neurodegeneration, autoimmune disease and viral infections.
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.
Artificial intelligence (AI) continues to entice. On the exhibition floor at the 2023 Congress of the European Academy of Neurology, one company’s booth featured “Mindart” technology. A passersby could answer a short series of prompts, and get a unique image based on the input made by generative AI. Entertainment aside, medically speaking, AI applications “are still research,” Riccardo Soffietti told his audience at one of several sessions devoted to AI. “But obviously, research is the future.”