8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors-Reference-Cited by-同舟云学术

8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors

Published:2016-01-07 Issue:4 Volume:59 Page:1388-1409
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Bavetsias Vassilios¹,Lanigan Rachel M.¹,Ruda Gian Filippo²³,Atrash Butrus¹,McLaughlin Mark G.¹,Tumber Anthony²³,Mok N. Yi¹,Le Bihan Yann-Vaï¹,Dempster Sally¹,Boxall Katherine J.¹,Jeganathan Fiona¹,Hatch Stephanie B.²³,Savitsky Pavel²,Velupillai Srikannathasan²,Krojer Tobias²,England Katherine S.²³,Sejberg Jimmy¹,Thai Ching¹,Donovan Adam¹,Pal Akos¹,Scozzafava Giuseppe²³,Bennett James M.²³,Kawamura Akane⁴,Johansson Catrine²⁵,Szykowska Aleksandra²,Gileadi Carina²,Burgess-Brown Nicola A.²,von Delft Frank²⁶⁷,Oppermann Udo²⁵,Walters Zoe⁸,Shipley Janet⁸,Raynaud Florence I.¹,Westaway Susan M.⁹,Prinjha Rab K.⁹,Fedorov Oleg²³,Burke Rosemary¹,Schofield Christopher J.⁴,Westwood Isaac M.¹,Bountra Chas²,Müller Susanne²³,van Montfort Rob L. M.¹,Brennan Paul E.²³,Blagg Julian¹

Affiliation:

1. Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, 15 Cotswold Road, London SM2 5NG, U.K.

2. Structural Genomics Consortium (SGC), University of Oxford, ORCRB Roosevelt Drive, Oxford OX3 7DQ, U.K.

3. Target Discovery Institute (TDI), Nuffield Department of Medicine, University of Oxford, NDMRB Roosevelt Drive, Oxford OX3 7FZ, U.K.

4. Chemistry Research Laboratory, University of Oxford, Mansfield Road, Oxford OX1 3TA, U.K.

5. Botnar Research Centre, NIHR Oxford Biomedical Research Unit, Oxford OX3 7LD, U.K.

6. Diamond Light Source (DLS), Harwell Science and Innovation Campus, Didcot OX11 0DE, U.K.

7. Department of Biochemistry, University of Johannesburg, Auckland Park 2006, South Africa

8. Divisions of Molecular Pathology and Cancer Therapeutics, The Institute of Cancer Research, London SM2 5NG, U.K.

9. Epinova Discovery Performance Unit, Medicines Research Centre, GlaxoSmithKline R&D, Stevenage SG1 2NY, U.K.

Funder

Avon Foundation for Women

Wellcome Trust

Cancer Research UK

Royal Marsden NHS Foundation Trust

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.5b01635

Reference62 articles.

1. Histone demethylases in development and disease

2. Dynamic Regulation of Histone Lysine Methylation by Demethylases

3. Reconstitution of Nucleosome Demethylation and Catalytic Properties of a Jumonji Histone Demethylase

4. Molecular mechanisms and potential functions of histone demethylases

5. The oncogenic potential of Jumonji D2 (JMJD2/KDM4) histone demethylase overexpression

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