Gan & Lee Pharmaceuticals Co. Ltd. has prepared and tested proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase binding moiety covalently linked to an estrogen receptor α(ER-α; ESR1) targeting moiety via a linker reported to be useful for the treatment of cancer.

Work at Dark Blue Therapeutics Ltd. has led to the development of new proteolysis targeting chimera (PROTAC) compounds comprising a E3 ubiquitin ligase-binding moiety coupled to a protein ENL (MLLT1; YEATS1) and/or protein AF-9 (MLLT3; AF9)-targeting moiety through a linker. They are reported to be useful for the treatment of cancer.

Researchers from Stanford School of Medicine and Yonsei University College of Medicine reported the discovery and preclinical characterization of novel KLHDC2-mediated CDK6-selective degraders.

Triana Biomedicines Inc. has divulged protein/nucleic acid degraders acting as cyclin-dependent kinase 2 (CDK2) degraders reported to be useful for the treatment of cancer.

Linkcure Therapeutics has synthesized molecular glue degraders acting as zinc finger protein 803 (ZNF803; WIZ) degradation inducers reported to be useful for the treatment of sickle cell anemia and β-thalassemia.

Enodia Therapeutics SAS has raised €20.7 million ($25 million) in seed financing to advance its work developing novel small-molecule therapies for targeted protein degradation at the point of synthesis.

Ascentage Pharma Group International has obtained IND approval from the FDA for its BTK-targeted protein degrader APG-3288. A phase I study will be conducted in patients with relapsed or refractory B-cell malignancies.

Convergen (Suzhou) Pharmaceutical Co. Ltd. has described proteolysis targeting chimera (PROTAC) compounds comprising a cereblon (CRBN) E3 ubiquitin ligase-binding moiety coupled to a serine/threonine-protein kinase PAK4-targeting moiety through a linker reported to be useful for the treatment of cancer.

Shenzhen Targetrx Inc. has divulged proteolysis targeting chimera (PROTAC) compounds comprising a cereblon (CRBN)-binding moiety covalently linked to Raf kinase B (V600E mutant)-targeting moiety through linker reported to be useful for the treatment of cancer.

Acute myeloid leukemia (AML) is a hematological cancer with limited treatment options and characterized by frequent relapse and poor prognosis. The only approved antibody-drug conjugate for AML is gemtuzumab ozogamicin, which targets CD33.