Chemistry:GSK484

From HandWiki

GSK484 is an experimental drug which acts as a selective inhibitor of the enzyme peptidylarginine deiminase 4 (PAD4). It has antiinflammatory effects and has been researched for potential use in the treatment of various inflammatory conditions, primarily rheumatoid arthritis, but it has also been used to investigate the role of PAD4 in acute kidney injury, lung inflammation, heart muscle damage following heart attack, osteoporosis, diabetes, and some forms of cancer.[1][2][3][4][5][6][7][8][9][10][11]

See also

References

  1. ↑ "PAD4: pathophysiology, current therapeutics and future perspective in rheumatoid arthritis". Expert Opinion on Therapeutic Targets 21 (4): 433–447. April 2017. doi:10.1080/14728222.2017.1294160. PMID 28281906. 
  2. ↑ "Pharmacological targeting of peptidylarginine deiminase 4 prevents cancer-associated kidney injury in mice". Oncoimmunology 6 (8). 2017. doi:10.1080/2162402X.2017.1320009. PMID 28919990. 
  3. ↑ "Protein Arginine Deiminases (PADs): Biochemistry and Chemical Biology of Protein Citrullination". Accounts of Chemical Research 52 (3): 818–832. March 2019. doi:10.1021/acs.accounts.9b00024. PMID 30844238. 
  4. ↑ "Inhibition of peptidyl arginine deiminase-4 protects against myocardial infarction induced cardiac dysfunction". International Immunopharmacology 78. January 2020. doi:10.1016/j.intimp.2019.106055. PMID 31816575. 
  5. ↑ "Inhibition of Peptidyl Arginine Deiminase-4 Prevents Renal Ischemia-Reperfusion-Induced Remote Lung Injury". Mediators of Inflammation 2020. 2020. doi:10.1155/2020/1724206. PMID 33456369. 
  6. ↑ "Inhibition of NETosis via PAD4 alleviated inflammation in giant cell myocarditis". iScience 26 (7). July 2023. doi:10.1016/j.isci.2023.107162. PMID 37534129. Bibcode: 2023iSci...26j7162H. 
  7. ↑ "GSK484, an inhibitor of peptidyl arginine deiminase 4, increases the radiosensitivity of colorectal cancer and inhibits neutrophil extracellular traps". The Journal of Gene Medicine 25 (9). September 2023. doi:10.1002/jgm.3530. PMID 37203323. 
  8. ↑ "Neutrophil extracellular traps induce persistent lung tissue damage via thromboinflammation without altering virus resolution in a mouse coronavirus model". Journal of Thrombosis and Haemostasis 22 (1): 188–198. January 2024. doi:10.1016/j.jtha.2023.09.014. PMID 37748582. 
  9. ↑ "Activated NETosis of bone marrow neutrophils up-regulates macrophage osteoclastogenesis via cGAS-STING/AKT2 pathway to promote osteoporosis". Experimental Cell Research 446 (2). March 2025. doi:10.1016/j.yexcr.2025.114477. PMID 39988126. 
  10. ↑ "Intestinal neutrophil extracellular traps promote gut barrier damage exacerbating endotoxaemia, systemic inflammation and progression of diabetic retinopathy in type 2 diabetes". Diabetologia 68 (4): 866–889. April 2025. doi:10.1007/s00125-024-06349-4. PMID 39875729. 
  11. ↑ "C5a/C5aR regulates Th1/Th2 imbalance in sepsis-associated lung injury by promoting neutrophil activation to increase PAD4 expression". Annals of Medicine 57 (1). December 2025. doi:10.1080/07853890.2024.2447406. PMID 39831526. 



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