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Updated: Jun 11, 2026

Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
AS1387392, a novel immunosuppressive cyclic tetrapeptide compound with inhibitory activity against mammalian histone
Satoshi Sasamura1, Kazutoshi Sakamoto, Shoji Takagaki
1Pharmacology Research Laboratories, Astellas Pharma Inc., Tsukuba-shi, Ibaraki, Japan. satoshi.sasamura@jp.astellas.com
Abstract:
The novel immunosuppressant AS1387392 has been isolated from Acremonium sp. No. 27082. This compound showed a strong inhibitory effect against mammalian histone deacetylase and T-cell proliferation. Further, AS1387392 showed a good oral absorption, and its plasma concentration was higher than that of FR235222, an analog of AS1387392 that inhibited histone deacetylase previously reported. Given these findings, AS1387392 may represent an important new lead in developing immunosuppressant.
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