ErSO

Last updated

ErSO
ErSO structure.png
Identifiers
  • (3R)-3-(4-hydroxyphenyl)-3-[4-(trifluoromethoxy)phenyl]-7-(trifluoromethyl)-1H-indol-2-one
CAS Number
PubChem CID
Chemical and physical data
Formula C22H13F6NO3
Molar mass 453.340 g·mol−1
3D model (JSmol)
  • C1=CC2=C(C(=C1)C(F)(F)F)NC(=O)[C@]2(C3=CC=C(C=C3)O)C4=CC=C(C=C4)OC(F)(F)F
  • InChI=1S/C22H13F6NO3/c23-21(24,25)17-3-1-2-16-18(17)29-19(31)20(16,12-4-8-14(30)9-5-12)13-6-10-15(11-7-13)32-22(26,27)28/h1-11,30H,(H,29,31)/t20-/m1/s1
  • Key:ZFSRXAHDJSCEDS-HXUWFJFHSA-N

ErSO is an experimental anticancer drug which induces the unfolded protein response. In tests on mice it was effective at eliminating xenografts of human breast cancer cell lines. While it is at an early developmental stage and this particular molecule may not be developed for medical use, it represents an important proof of concept for inducers of unfolded protein response as a novel class of anti-cancer drugs. [1] [2] [3] [4] [5]

References

  1. ↑ Boudreau MW, Duraki D, Wang L, Mao C, Kim JE, Henn MA, et al. (July 2021). "A small-molecule activator of the unfolded protein response eradicates human breast tumors in mice". Science Translational Medicine. 13 (603). doi:10.1126/scitranslmed.abf1383. PMC   8456366 . PMID   34290053.
  2. ↑ Boudreau MW, Mulligan MP, Shapiro DJ, Fan TM, Hergenrother PJ (March 2022). "Activators of the Anticipatory Unfolded Protein Response with Enhanced Selectivity for Estrogen Receptor Positive Breast Cancer". Journal of Medicinal Chemistry. 65 (5): 3894–3912. doi:10.1021/acs.jmedchem.1c01730. PMC   9067622 . PMID   35080871.
  3. ↑ Boudreau MW, Hergenrother PJ (June 2022). "Evolution of 3-(4-hydroxyphenyl)indoline-2-one as a scaffold for potent and selective anticancer activity". RSC Medicinal Chemistry. 13 (6): 711–725. doi:10.1039/d2md00110a. PMC   9215341 . PMID   35814932.
  4. ↑ Ghosh S, Yang R, Duraki D, Zhu J, Kim JE, Jabeen M, et al. (September 2023). "Plasma Membrane Channel TRPM4 Mediates Immunogenic Therapy-Induced Necrosis". Cancer Research. 83 (18): 3115–3130. doi:10.1158/0008-5472.CAN-23-0157. PMC   10635591 . PMID   37522838.
  5. ↑ Wei E, Shapiro D, Zhu J, Nelson E, Gosh S, Duraki D (March 2024). "Abstract 2210 To Die or Not to Die: Controlling Death in Breast and Ovarian Cancer Cells with a Novel Pathway Regulating Anticancer Drug". Journal of Biological Chemistry. 300 (3): 106122. doi: 10.1016/j.jbc.2024.106122 .
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