AFM-30a

Last updated

AFM-30a
AFM-30a structure.png
Identifiers
  • N-[(1S)-4-[(1-amino-2-fluoroethylidene)amino]-1-(1-methylbenzimidazol-2-yl)butyl]-3-oxo-1,2-dihydroisoindole-4-carboxamide
CAS Number
PubChem CID
ChemSpider
ChEMBL
Chemical and physical data
Formula C23H25FN6O2
Molar mass 436.491 g·mol−1
3D model (JSmol)
  • CN1C2=CC=CC=C2N=C1[C@H](CCCN=C(CF)N)NC(=O)C3=CC=CC4=C3C(=O)NC4
  • InChI=1S/C23H25FN6O2/c1-30-18-10-3-2-8-16(18)28-21(30)17(9-5-11-26-19(25)12-24)29-22(31)15-7-4-6-14-13-27-23(32)20(14)15/h2-4,6-8,10,17H,5,9,11-13H2,1H3,(H2,25,26)(H,27,32)(H,29,31)/t17-/m0/s1
  • Key:CHPVRACBRZIQQU-KRWDZBQOSA-N

AFM-30a is an experimental drug which was the first selective inhibitor to be developed of the enzyme peptidylarginine deiminase 2 (PAD2). It has been used to investigate the role of PAD2 in various inflammatory conditions and development of cancers. It was found to be active against pulmonary fibrosis in a mouse model. [1] [2] [3] [4] [5]

See also

References

  1. ↑ Muth A, Subramanian V, Beaumont E, Nagar M, Kerry P, McEwan P, et al. (April 2017). "Development of a Selective Inhibitor of Protein Arginine Deiminase 2". Journal of Medicinal Chemistry. 60 (7): 3198–3211. doi:10.1021/acs.jmedchem.7b00274. PMC   5477668 . PMID   28328217.
  2. ↑ Martín Monreal MT, Rebak AS, Massarenti L, Mondal S, Šenolt L, Ødum N, et al. (2021). "Applicability of Small-Molecule Inhibitors in the Study of Peptidyl Arginine Deiminase 2 (PAD2) and PAD4". Frontiers in Immunology. 12: 716250. doi: 10.3389/fimmu.2021.716250 . PMC   8560728 . PMID   34737738.{{cite journal}}: CS1 maint: article number as page number (link)
  3. ↑ Mansouri P, Mansouri P, Behmard E, Najafipour S, Kouhpayeh SA, Farjadfar A (October 2024). "Peptidylarginine deiminase (PAD): A promising target for chronic diseases treatment". International Journal of Biological Macromolecules. 278 (Pt 3): 134576. doi:10.1016/j.ijbiomac.2024.134576. PMID   39127273.{{cite journal}}: CS1 maint: article number as page number (link)
  4. ↑ Baird R, Yusuf A, Forde L, Pohl K, Kavanagh K, Fitzpatrick F, et al. (2024). "The vacuolar anti-Pseudomonal activity of neutrophil primary granule peptidyl-arginine deiminase enzymes". Frontiers in Immunology. 15: 1452393. doi: 10.3389/fimmu.2024.1452393 . PMC   11527647 . PMID   39493757.{{cite journal}}: CS1 maint: article number as page number (link)
  5. ↑ Zhang YM, Jin FY, Gao XM, Xu H, Zhu Y, Mao N (January 2025). "[The effects and mechanisms of PAD2 inhibitor AFM-30a attenuates pulmonary fibrosis in silicotic mice]". Zhonghua Lao Dong Wei Sheng Zhi Ye Bing Za Zhi = Zhonghua Laodong Weisheng Zhiyebing Zazhi = Chinese Journal of Industrial Hygiene and Occupational Diseases. 43 (1): 1–13. doi:10.3760/cma.j.cn121094-20240102-00001. PMID   39909591.
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