Structure-Based Design and Synthesis of an Isozyme-Selective MTHFD2 Inhibitor with a Tricyclic Coumarin Scaffold-Reference-Cited by-同舟云学术

Structure-Based Design and Synthesis of an Isozyme-Selective MTHFD2 Inhibitor with a Tricyclic Coumarin Scaffold

Published:2019-05-24 Issue:6 Volume:10 Page:893-898
ISSN:1948-5875
Container-title:ACS Medicinal Chemistry Letters
language:en
Short-container-title:ACS Med. Chem. Lett.

Author:

Kawai Junya¹^ORCID,Ota Masahiro²,Ohki Hitoshi¹,Toki Tadashi¹,Suzuki Makoto²,Shimada Takashi²,Matsui Satoshi¹,Inoue Hidekazu¹,Sugihara Chika²,Matsuhashi Norikazu²,Matsui Yumi²,Takaishi Sachiko¹,Nakayama Kiyoshi³

Affiliation:

1. R&D Division, Daiichi Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan

2. Daiichi Sankyo RD Novare Co., Ltd., 1-16-13 Kitakasai, Edogawa-ku, Tokyo 134-8630, Japan

3. Daiichi Sankyo Co., Ltd., 3-5-1 Nihonbashi-honcho, Chuo-ku, Tokyo 103-8426, Japan

Publisher

American Chemical Society (ACS)

Subject

Organic Chemistry,Drug Discovery,Biochemistry

Link

https://pubs.acs.org/doi/pdf/10.1021/acsmedchemlett.9b00069

Reference25 articles.

1. Reversal of Cytosolic One-Carbon Flux Compensates for Loss of the Mitochondrial Folate Pathway

2. The 3-D structure of a folate-dependent dehydrogenase/cyclohydrolase bifunctional enzyme at 1.5 å resolution

3. Metabolic enzyme expression highlights a key role for MTHFD2 and the mitochondrial folate pathway in cancer

4. Increased MTHFD2 expression is associated with poor prognosis in breast cancer

5. Modulation of Redox Homeostasis by Inhibition of MTHFD2 in Colorectal Cancer: Mechanisms and Therapeutic Implications

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