Despite the approval of numerous antibody-drug conjugates (ADCs), their therapeutic index remains limited by off-target toxicity resulting from linker instability. To address this challenge, the development of novel ADCs with improved plasma stability and reduced systemic toxicity is critically needed.

Ningbo Newbay Medical Technology Co. Ltd. has identified helicase bicycle amide derivatives acting as DNA polymerase θ (POLθ, POLQ) inhibitors reported to be useful for the treatment of cancer.

Healzen Therapeutics Co. Ltd. has patented new proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase-binding moiety covalently linked to a mitogen-activated protein kinase kinase kinase kinase 1 (MAP4K1; HPK1; MEKKK1)-targeting moiety via a linker. They are reported to be useful for the treatment of cancer, hematological and autoimmune diseases.

MYC is a key regulator of RNA Polymerase I (Pol I) transcription, promoting rRNA synthesis both directly and indirectly. MYC overexpression is common in many cancer types, where it drives increased ribosome biogenesis to support uncontrolled cell growth and proliferation.

Haisco Pharmaceutical Group Co. Ltd. has identified new proteolysis targeting chimeras (PROTACs) comprising an E3 ubiquitin ligase binding ligand coupled to probable global transcription activator SNF2L2 (SMARCA2; BAF190B; SNF2-α)-targeting agent through a linker acting as SMARCA2 degradation inducers and thus reported to be useful for the treatment of lung cancer.

An Anavo Therapeutics BV patent describes new thiophene and thiazole derivatives acting as protein phosphatase 1D (PP-2Cdelta; WIP1) inhibitors.