SMARCA4-deficient cells have shown dependency on SMARCA2 for survival, suggesting SMARCA2 as a promising synthetic lethal target in SMARCA4-deficient cancers. Chinese researchers recently published data on a series of SMARCA2 PROTACs, among which compound [I] exerted good SMARCA2 degradation.
Gluetacs Therapeutics (Shanghai) Co. Ltd. has discovered new proteolysis targeting chimera (PROTAC) compounds comprising a cereblon (CRBN)-binding moiety coupled to a SWI/SNF-related matrix-associated actin-dependent regulator of chromatin subfamily A member 2 (SMARCA2) and SMARCA4-targeting moiety. They are designed for use in the treatment of cancer, transplant rejection, infections, diabetes, autoimmune, neurological, inflammatory and cardiovascular disorders, among others.
Gan & Lee Pharmaceuticals Co. Ltd. has disclosed proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase-binding moiety covalently linked to a probable global transcription activator SNF2L2 (SMARCA2; BAF190B; SNF2-α)- and/or SMARCA4-targeting moiety.
Aurigene Oncology Ltd. has identified proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase protein binding moiety covalently linked to probable global transcription activator SNF2L2 (SMARCA2; BAF190B; SNF2-α) and/or transcription activator BRG1 (SMARCA4; BAF190A; SNF2-β) binding moieties through a linker reported to be useful for the treatment of cancer.
Prelude Therapeutics Inc. has prepared and tested new proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase-binding moiety coupled to probable global transcription activator SNF2L2 (SMARCA2; BAF190B; SNF2-α) and SMARCA4-targeting moiety through a linker.
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.
Prelude Therapeutics Inc. has described proteolysis targeting chimera (PROTAC) compounds comprising a cereblon (CRBN) E3 ubiquitin ligase binding moiety covalently linked to a probable global transcription activator SNF2L2 (SMARCA2; BAF190B; SNF2-α) or transcription activator BRG1 (SMARCA4; BAF190A; SNF2-β) targeting moiety through a linker. They are reported to be useful for the treatment of cancer.
Astrazeneca AB patents describe new proteolysis targeting chimera (PROTAC) compounds comprising a cereblon (CRBN) E3 ubiquitin ligase-binding moiety covalently linked to probable global transcription activator SNF2L2 (SMARCA2; BAF190B; SNF2-α)-targeting moiety reported to be useful for the treatment of cancer.
