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BB-Cl-Amidine

Topic: Chemistry

 From HandWiki - Reading time: 2 min

BB-Cl-Amidine is an experimental drug which acts as a non-subtype selective, irreversible inhibitor of the enzyme peptidylarginine deiminase (PAD). It has anti-cancer effects and is useful for various inflammatory conditions such as arthritis, and while it may be unlikely to be developed for human use due to toxicity concerns, it is widely used in scientific research.[1][2][3][4][5][6][7][8] As well as its activity as a PAD inhibitor, BB-Cl-Amidine also inhibits the action of the Stimulator of interferon genes (STING) protein by preventing STING oligomerization and thereby terminating the signalling pathway.[9]

See also

References

  1. ↑ "Peptidylarginine deiminase inhibition disrupts NET formation and protects against kidney, skin and vascular disease in lupus-prone MRL/lpr mice". Annals of the Rheumatic Diseases 74 (12): 2199–2206. December 2015. doi:10.1136/annrheumdis-2014-205365. PMID 25104775. 
  2. ↑ "Abrogation of collagen-induced arthritis by a peptidyl arginine deiminase inhibitor is associated with modulation of T cell-mediated immune responses". Scientific Reports 6. May 2016. doi:10.1038/srep26430. PMID 27210478. Bibcode: 2016NatSR...626430K. 
  3. ↑ "PAD Inhibitors as a Potential Treatment for SARS-CoV-2 Immunothrombosis". Biomedicines 9 (12): 1867. December 2021. doi:10.3390/biomedicines9121867. PMID 34944683. 
  4. ↑ "Viral mimetic poly(I:C) induces neutrophil extracellular traps via PAD4 to promote inflammation and thrombosis". Biochemical and Biophysical Research Communications 565: 64–71. August 2021. doi:10.1016/j.bbrc.2021.05.091. PMID 34098313. Bibcode: 2021BBRC..565...64A. 
  5. ↑ "Peptidylarginine deiminase (PAD): A promising target for chronic diseases treatment". International Journal of Biological Macromolecules 278 (Pt 3). October 2024. doi:10.1016/j.ijbiomac.2024.134576. PMID 39127273. 
  6. ↑ "Peptidylarginine Deiminases Inhibitors Decrease Endothelial Cells Angiogenic Potential by Affecting Akt Signaling and the Expression and Secretion of Angiogenic Factors". Cellular Physiology and Biochemistry 58 (1): 63–82. February 2024. doi:10.33594/000000683. PMID 38374715. 
  7. ↑ "Silencing PADI-2 induces antitumor effects by downregulating NF-κB, Nrf2/HO-1 and AKT1 in A549 lung cancer cells". International Immunopharmacology 146. January 2025. doi:10.1016/j.intimp.2024.113830. PMID 39700962. 
  8. ↑ "Blocking peptidyl arginine deiminase 4 confers neuroprotective effect in the post-ischemic brain through both NETosis-dependent and -independent mechanisms". Acta Neuropathologica Communications 13 (1). February 2025. doi:10.1186/s40478-025-01951-y. PMID 39966968. 
  9. ↑ "Targeting STING oligomerization with small-molecule inhibitors". Proceedings of the National Academy of Sciences of the United States of America 120 (33). August 2023. doi:10.1073/pnas.2305420120. PMID 37549268. Bibcode: 2023PNAS..12005420H. 



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