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BB-Cl-amidine
- Development stage
- Preclinical
- Lead developer
- UMass Chan Medical School
- Modality
- Small Molecules
- Administration
- Intraperitoneal, Subcutaneous
01
Overview
BB-Cl-amidine is a potent, second-generation pan-peptidylarginine deiminase (PAD) inhibitor that targets PAD1, PAD2, PAD3, and PAD4. It is a biphenyl-containing derivative of Cl-amidine, optimized for enhanced metabolic stability and cellular potency. PAD enzymes, particularly PAD4, are responsible for the post-translational conversion of arginine residues to citrulline on histones, a process essential for chromatin decondensation and the subsequent release of neutrophil extracellular traps (NETs). By irreversibly inhibiting these enzymes, BB-Cl-amidine effectively blocks NETosis and reduces the associated pro-inflammatory response. It has been extensively studied in preclinical models of various inflammatory and autoimmune conditions, including allergic asthma, pneumonia, rheumatoid arthritis, and systemic lupus erythematosus, as well as in oncology for its ability to modulate the tumor microenvironment.
- Other names
- BB-Cl-amidine
02
Targets
PADI4 (Peptidyl arginine deiminase 4)STING (Stimulator of interferon genes protein)PADI1 (Peptidyl arginine deiminase 1)PADI3 (Peptidyl arginine deiminase 3)PADI2 (Peptidyl arginine deiminase 2)
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