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University of Groningen Novel Approaches for Developing Small Molecules to Target Histone Deacetylases Cao, Fangyuan

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University of Groningen

Novel Approaches for Developing Small Molecules to Target Histone Deacetylases

Cao, Fangyuan

DOI:

10.33612/diss.157448844

IMPORTANT NOTE: You are advised to consult the publisher's version (publisher's PDF) if you wish to cite from it. Please check the document version below.

Document Version

Publisher's PDF, also known as Version of record

Publication date: 2021

Link to publication in University of Groningen/UMCG research database

Citation for published version (APA):

Cao, F. (2021). Novel Approaches for Developing Small Molecules to Target Histone Deacetylases. University of Groningen. https://doi.org/10.33612/diss.157448844

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Downloaded from the University of Groningen/UMCG research database (Pure): http://www.rug.nl/research/portal. For technical reasons the number of authors shown on this cover page is limited to 10 maximum.

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Fangyuan Cao

2021

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The research described in this thesis was carried out in the Department of Chemical and Pharmaceutical Biology (Groningen Research Institute of Pharmacy, University of Groningen, The Netherlands) and was financially supported by the China Scholarship Council.

The research work was carried out according to the requirement of the Graduate School of Science Faculty of Science and Engineering, University of Groningen, The Netherlands. Printing of this thesis was financially supported by the University Library and the Graduate School of Science, Faculty of Science and Engineering, University of Groningen, The Netherlands.

Cover design: Fangyuan Cao Printing: Ridderprint

Copyright © 2021 by Fangyuan Cao. All rights are reserved. No part of the thesis may be reproduced or transmitted in any form or by any means without the prior permission in writing of the author.

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Noovveell AApppprrooaacchheess ffoorr DDeevveellooppiinngg SSm

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PhD thesis

to obtain the degree of PhD at the University of Groningen

on the authority of the Rector Magnificus Prof. C. Wijmenga

and in accordance with the decision by the College of Deans. This thesis will be defended in public on Tuesday 23 February 2021 at 11.00 hours

by

Fangyuan Cao

born on 24 April 1990 in Changchun, China

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Supervisors

Prof. F.J. Dekker Prof. G.J. Poelarends

Assessment Committee

Prof. A.S.S. Dömling Prof. P.H. h. Elsinga Prof. R.J. Pieters

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CCoonntteennttss

CChhaapptteerr 11

Introduction and scope of the thesis

... 99

CChhaapptteerr 22

The process and strategy for developing selective histone deacetylase 3 Inhibitors

... 3311

CChhaapptteerr 33

Inhibitory selectivity among class I HDACs has a major impact on inflammatory gene expression in macrophages

... 5577

CChhaapptteerr 44

Induced protein degradation of histone deacetylases 3 (HDAC3) by proteolysis targeting chimera (PROTAC)

... 9955

CChhaapptteerr 55

HDAC/MIF dual inhibitor inhibits NSCLC cell survival and proliferation by blocking the AKT pathway

... 113333

CChhaapptteerr 66

Summary and future perspectives

... 116611

AAppppeennddiicceess

Acknowledgement

... 117777

Publication

... 118800

About the author

... 118811

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