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PFI-1
- Development stage
- Discontinued
- Lead developer
- Pfizer
- Modality
- Small Molecules
01
Overview
PFI-1 (PF-6405761) is a highly selective small molecule inhibitor of the Bromodomain and Extra-Terminal (BET) family of proteins, specifically targeting BRD4 and BRD2. Developed by Pfizer in collaboration with the Structural Genomics Consortium (SGC), it functions as an acetyl-lysine mimetic that occupies the bromodomain binding pocket, thereby preventing the interaction between BET proteins and acetylated histones. This disruption leads to the downregulation of key oncogenes such as MYC. While PFI-1 has shown significant antiproliferative and pro-apoptotic effects in preclinical models of leukemia and other cancers, it is primarily utilized as a high-quality chemical probe for epigenetic research and has not been advanced into clinical development.
- Other names
- PF-6405761PF6405761PF 6405761
02
Targets
BRD4 (Bromodomain-containing protein 4)BRD2 (Bromodomain-containing protein 2)CREBBP BD (Creb-binding protein bromodomain)
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