Thieno[3,2-b]pyrrole-5-carboxamides as New Reversible Inhibitors of Histone Lysine Demethylase KDM1A/LSD1. Part 2: Structure-Based Drug Design and Structure–Activity Relationship-Reference-Cited by-同舟云学术

Thieno[3,2-b]pyrrole-5-carboxamides as New Reversible Inhibitors of Histone Lysine Demethylase KDM1A/LSD1. Part 2: Structure-Based Drug Design and Structure–Activity Relationship

Published:2017-02-27 Issue:5 Volume:60 Page:1693-1715
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Vianello Paola¹^ORCID,Sartori Luca¹,Amigoni Federica¹,Cappa Anna¹,Fagá Giovanni¹,Fattori Raimondo¹,Legnaghi Elena¹,Ciossani Giuseppe²,Mattevi Andrea²^ORCID,Meroni Giuseppe¹,Moretti Loris¹^ORCID,Cecatiello Valentina³⁴,Pasqualato Sebastiano³,Romussi Alessia¹,Thaler Florian¹,Trifiró Paolo¹,Villa Manuela¹,Botrugno Oronza A.¹,Dessanti Paola¹,Minucci Saverio¹⁵,Vultaggio Stefania¹,Zagarrí Elisa¹,Varasi Mario¹,Mercurio Ciro¹⁶

Affiliation:

1. Department of Experimental Oncology, Academic Drug Discovery, European Institute of Oncology, Via Adamello 16, 20139 Milano, Italy

2. Department of Biology and Biotechnology, University of Pavia, Via Ferrata 1, 27100 Pavia, Italy

3. Crystallography Unit, Department of Experimental Oncology, European Institute of Oncology, Via Adamello 16, 20139 Milano, Italy

4. IFOM- The FIRC Institute of Molecular Oncology Foundation, Via Adamello 16, 20139 Milano, Italy

5. Department of Biosciences, University of Milan, Via Celoria 26, 20133 Milano, Italy

6. Genextra Group, DAC s.r.l., Via Adamello 16, 20139 Milano, Italy

Funder

Ministero dell?Istruzione, dell?Universit? e della Ricerca

Associazione Italiana per la Ricerca sul Cancro

Seventh Framework Programme

Fondazione Cariplo

Fondo per la Promozione di Accordi Istituzionale, Regione Lombardia

Rasna Theraupeutics Inc.

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.6b01019

Reference45 articles.

1. The role of histone demethylases in cancer therapy

2. Histone Demethylation Mediated by the Nuclear Amine Oxidase Homolog LSD1

3. A Novel Mammalian Flavin-dependent Histone Demethylase

4. LSD1 inhibition: a therapeutic strategy in cancer?

5. LSD1 demethylates repressive histone marks to promote androgen-receptor-dependent transcription

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