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Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

EP300/CBP

Action

inhibitors

Mechanism

EP300/CBP inhibitors(CREBBP/EP300 inhibitors)

Therapeutic Areas

NeoplasmsRespiratory Diseases

Active Indication

squamous cell lung carcinoma

Inactive Indication-

Originator Organization

Daiichi Sankyo Co., Ltd.

Active Organization

Daiichi Sankyo Co., Ltd.

Inactive Organization-

License Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

Author: Naito, Hiroyuki ; Kanada, Ryutaro ; Kuroha, Mutsumi ; Suzuki, Kanae ; Higuchi, Saito ; Hashimoto, Kazuyuki ; Banjo, Toshihiro ; Ubukata, Osamu ; Tominaga, Yuichi ; Takahashi, Mizuki ; Kagoshima, Yoshiko ; Sato, Kazumi ; Kihara, Kawori ; Suzuki, Takashi ; Murata, Takeshi ; Isoyama, Takeshi ; Asano, Masayoshi ; Yamamoto, Yuka ; Haruta, Makoto ; Togashi, Noriko ; Obata, Kenichi

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.

100 Deals associated with DS17701585

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