A molecular model of an extended DNA cross-linking agent binding in the minor groove of DNA
Description
SG2274 is a small molecule polypyrrole-PBD conjugate that recognises the NF-Y transcription factor-binding site in the promoter region of specific genes. The compound shows early promise as an anti-cancer agent with a novel mechanism of action.
SG2274, a compound with strong DNA binding and good sequence discrimination is being developed based on Spirogen's proprietary technologies involving pyrrolobenzodiazepines and heterocycle combinations which provide a covalent binding motif. SG2274 binds preferentially to the NF-Y transcription factor binding site and has been shown to inhibit both mRNA and protein expression in vitro. The molecule exhibits in vivo anti-tumor activity and further mechanism of action work is ongoing.
Developmental Status
Lead molecules are rapidly being progressed to pre-clinical development and good activity is being demonstrated.
