| Structural highlights
Publication Abstract from PubMed
EP300 and its paralog CBP play an important role in post-translational modification as histone acetyltransferases (HATs). EP300/CBP inhibition has been gaining attention as an anticancer treatment target in recent years. Herein, we describe the identification of a novel, highly selective EP300/CBP inhibitor, compound 11 (DS17701585), by scaffold hopping and structure-based optimization of a high-throughput screening hit 1. Compound 11 (DS17701585) shows dose-dependent inhibition of SRY-box transcription factor 2 (SOX2) mRNA expression in a human lung squamous cell carcinoma cell line LK2-xenografted mouse model.
Discovery of EP300/CBP histone acetyltransferase inhibitors through scaffold hopping of 1,4-oxazepane ring.,Kanada R, Kagoshima Y, Asano M, Suzuki T, Murata T, Haruta M, Takahashi M, Ubukata O, Hashimoto K, Obata K, Kihara K, Kuroha M, Banjo T, Togashi N, Sato K, Yamamoto Y, Suzuki K, Isoyama T, Tominaga Y, Higuchi S, Naito H Bioorg Med Chem Lett. 2022 Apr 9;66:128726. doi: 10.1016/j.bmcl.2022.128726. PMID:35413416[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
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References
- ↑ Kanada R, Kagoshima Y, Asano M, Suzuki T, Murata T, Haruta M, Takahashi M, Ubukata O, Hashimoto K, Obata K, Kihara K, Kuroha M, Banjo T, Togashi N, Sato K, Yamamoto Y, Suzuki K, Isoyama T, Tominaga Y, Higuchi S, Naito H. Discovery of EP300/CBP histone acetyltransferase inhibitors through scaffold hopping of 1,4-oxazepane ring. Bioorg Med Chem Lett. 2022 Jun 15;66:128726. PMID:35413416 doi:10.1016/j.bmcl.2022.128726
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