ISAM-140 is a selective non-xanthinic adenosine A2B receptor antagonist. Discovered in 2016,[1] it has a Ki of 3.49 nM on the A2B receptor and >1000-fold selectivity with respect to the other three adenosine receptor subtypes. It has been shown to help the immune system to attack cancer cells in in vitro assays by rescuing T and NK cell proliferation, cytokine release, and TIL infiltration.[2]

References

  1. ^ El Maatougui, Abdelaziz; Azuaje, Jhonny; González-Gómez, Manuel; Miguez, Gabriel; Crespo, Abel; Carbajales, Carlos; Escalante, Luz; García-Mera, Xerardo; Gutiérrez-de-Terán, Hugo; Sotelo, Eddy (2016-03-10). "Discovery of Potent and Highly Selective A 2B Adenosine Receptor Antagonist Chemotypes". Journal of Medicinal Chemistry. 59 (5): 1967–1983. doi:10.1021/acs.jmedchem.5b01586. ISSN 0022-2623. PMID 26824742.
  2. ^ Tay, Apple Hui Min; Prieto-Díaz, Rubén; Neo, Shiyong; Tong, Le; Chen, Xinsong; Carannante, Valentina; Önfelt, Björn; Hartman, Johan; Haglund, Felix; Majellaro, Maria; Azuaje, Jhonny (2022-05-01). "A2B adenosine receptor antagonists rescue lymphocyte activity in adenosine-producing patient-derived cancer models". Journal for ImmunoTherapy of Cancer. 10 (5): e004592. doi:10.1136/jitc-2022-004592. ISSN 2051-1426. PMC 9115112. PMID 35580926.
Allikas: https://en.wikipedia.org/wiki/ISAM-140
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