Aurora kinases, a group of serine/threonine protein family, comprise Aurora A, B and C members and are involved in the regulation of cell division and mitosis. Aurora A overexpression correlates with poor prognosis and is considered a therapeutic target for cancer treatments, although the clinical development of Aurora kinase inhibitors has been so far limited by excessive safety issues.
Menin (MEN1)/MLL interaction inhibitors are reported in a Bala Therapeutics Inc. patent as potentially useful for the treatment of cancer and diabetes.
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.
The c-Myc oncogene is overexpressed in a significant proportion of human cancers, including difficult-to-treat triple-negative breast cancers (TNBC). In the pursuit of novel anti-TNBC agents, there is a growing interest in ligands that can stabilize c-Myc promoter G-quadruplex (G4), thereby inhibiting c-Myc expression.
Novel therapeutic strategies are urgently needed to treat glioblastoma, the most aggressive type of primary brain tumor frequently associated with poor survival.
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.
The trophoblast cell surface antigen 2 (TROP2) class chalked mix news by way of Astrazeneca plc and Daiichi Sankyo Co. Ltd. as the pair disclosed phase III data from the closely watched Tropion-Lung 1 trial with datopotamab deruxtecan (dato-dxd) against non-small-cell lung cancer.