The TCF4/β-catenin axis is a key driver of tumor growth, where β-catenin has remained resistant to therapy and is traditionally considered an undruggable protein. At the ACS Fall 2025 meeting, Parabilis Medicines Inc. divulged results of work on hyperstabilized α-helical peptides named helicons that directly bind to β-catenin and block its interaction with TCF transcription factors such as TCF4, as well as inhibit the Wnt signaling pathway.
Moma Therapeutics Inc. has released data regarding their Werner syndrome helicase (WRN) inhibitor MOMA-341 for the potential treatment of cancer. MOMA-341 is a potent and selective WRN inhibitor, the action of which is through covalent ligation.
Foresight Therapeutics (Hefei) Co. Ltd. has described Werner syndrome ATP-dependent helicase (WRN; RECQ3; RECQL2) inhibitors reported to be useful for the treatment of cancer.
It is known that phosphatidylinositol 5-phosphate 4-kinase, type II, γ (PIP4K2C) is a lipid kinase tied to poor outcomes in a variety of cancers, such as colorectal (CRC) and breast cancers. In the search for PIP4K2C degraders, researchers from Larkspur Biosciences Inc. discovered LRK-4189, a cereblon-mediated PIP4K2C degrader.
Researchers from China Pharmaceutical University and collaborators have identified various naphthalene and indane derivatives as selective USP7 inhibitors.
Colorectal cancer is among the most common malignant tumor types and the second leading cause of tumor-related deaths worldwide. Tumor necrosis factor α-induced protein 8-like protein 2 (TIPE2) is a protein member of the TIPE family and highly expressed in immune cells. The prognostic impact and the relationship with tumor immunity of TIPE2 plus other immune markers such as CD8, CD20 and CD66b were evaluated in colorectal cancer by researchers from First Affiliated Hospital of Anhui Medical University and collaborators.
Ubiquitin-specific protease 14 (USP14) is known to play important roles in the development and progression of cancer, including colorectal cancer, since it modulates proteasomal function and cellular proteostasis. In the present study, investigators from Zhejiang University and collaborators demonstrated that the USP14 inhibitor AKOS, a Chikungunya virus inhibitor, performed well as a colorectal cancer therapeutic both in vitro and in vivo.
Bayer AG and Kumquat Biosciences Inc. have entered into an exclusive global license and collaboration agreement to develop and commercialize Kumquat’s KRAS G12D inhibitor.
Cadherin 17 (CDH17), a member of the cadherin family protein involved in intestinal development and cell adhesion, is recognized as a potential therapeutic target in gastrointestinal (GI) cancers. Its tumor-specific overexpression and limited presence in normal tissues offer a favorable profile for the development of selective, targeted treatments.
Cardiff Oncology Inc.’s mid-stage and ongoing clinical trial of its PLK1 inhibitor in colorectal cancer produced promising data but the company’s stock lost a quarter of its value on July 30 because of second-quarter losses. The randomized phase II study of onvansertib combined with a standard-of-care treatment in first-line, RAS-mutated metastatic colorectal cancer produced a 49% confirmed objective response rate at the 30-mg dose level compared to 30% in the control arm.
