Fragment-Based Discovery of a Novel, Brain Penetrant, Orally Active HDAC2 Inhibitor-Reference-Cited by-同舟云学术

Fragment-Based Discovery of a Novel, Brain Penetrant, Orally Active HDAC2 Inhibitor

Published:2022-09-06 Issue:10 Volume:13 Page:1591-1597
ISSN:1948-5875
Container-title:ACS Medicinal Chemistry Letters
language:en
Short-container-title:ACS Med. Chem. Lett.

Author:

Tamanini Emiliano¹^ORCID,Miyamura Shin²,Buck Ildiko M.¹,Cons Benjamin D.¹^ORCID,Dawson Lee¹,East Charlotte¹,Futamura Takashi²,Goto Shintaro²,Griffiths-Jones Charlotte¹,Hashimoto Tetsuya²,Heightman Tom D.¹^ORCID,Ishikawa Shunpei²,Ito Hideki²,Kaneko Yosuke²,Kawato Tatsuya²,Kondo Kazumi²,Kurihara Naoki²,McCarthy James M.¹,Mori Yukiko²,Nagase Tsuyoshi²,Nakaishi Yuichiro²,Reeks Judith¹,Sato Akimasa²,Schöpf Patrick¹,Tai Kuninori²,Tamai Taichi²,Tisi Dominic¹,Woolford Alison J.-A.¹^ORCID

Affiliation:

1. Astex Pharmaceuticals, 436 Cambridge Science Park, Milton Road, Cambridge CB4 0QA, U.K.

2. Otsuka Pharmaceutical Co., Ltd., 463-10 Kagasuno, Kawauchi-cho, Tokushima 771-0192, Japan

Publisher

American Chemical Society (ACS)

Subject

Organic Chemistry,Drug Discovery,Biochemistry

Link

https://pubs.acs.org/doi/pdf/10.1021/acsmedchemlett.2c00272

Reference28 articles.

1. Nuclear histone acetylases and deacetylases and transcriptional regulation: HATs off to HDACs

2. Conformational Refinement of Hydroxamate-Based Histone Deacetylase Inhibitors and Exploration of 3-Piperidin-3-ylindole Analogues of Dacinostat (LAQ824)

3. Deacetylase Enzymes

4. Histone deacetylases and cancer: causes and therapies

5. Human HDAC1 and HDAC2 function in the DNA-damage response to promote DNA nonhomologous end-joining

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