PRMT1 is a key enzyme that catalyzes asymmetric dimethylation of arginine residues and overexpressed in various cancers and inflammatory diseases. While current PRMT1 inhibitors lack specificity and effectiveness, targeted degradation of PRMT1 offers a potential strategy to treat PRMT1-driven conditions and explore its nonenzymatic roles.

Parkinson’s disease (PD) is a neurodegenerative disorder characterized by the progressive loss of dopaminergic (DA) neurons in the substantia nigra, leading to clinical symptoms such as tremors, rigidity, bradykinesia and postural instability.

Researchers at North China Electric Power University and collaborators have developed novel radiolabels for the membrane-bound monoamine oxidase-B that feature a coumarin core.

Researchers from Fudan University and their collaborators reported the synthesis and preclinical characterization of novel Bruton’s tyrosine kinase (BTK)-targeting proteolysis-targeting chimeras (PROTACs) based on ARQ-531, a potent, reversible, noncovalent BTK inhibitor. 

Tumors with high levels of microsatellite instability (MSI-H), such as some subsets of colorectal, endometrial and gastric cancers, are associated with a hypermutated phenotype and a specific dependency on the WRN gene. Pharmacologic inhibition of WRN has been shown to selectively impair the viability of MSI-H cancer cells, effectively blocking tumor growth while sparing microsatellite-stable (MSS) cells.

Peptide-drug conjugates (PDCs) are emerging as a promising alternative to antibody-drug conjugates (ADCs), offering enhanced tumor penetration and reduced immunogenicity. Carbonic anhydrase IX (CAIX) and epidermal growth factor receptor (EGFR) are both well-validated targets in oncology due to their role in cancer cell survival, invasion and migration.

Mucosa-associated lymphoid tissue lymphoma translocation protein 1 (MALT1) is an important factor from a complex downstream of Bruton tyrosine kinase (BTK) in the B-cell receptor (BCR) signaling pathway.