Thieno[3,2-b]pyrrole-5-carboxamides as New Reversible Inhibitors of Histone Lysine Demethylase KDM1A/LSD1. Part 1: High-Throughput Screening and Preliminary Exploration-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 1: High-Throughput Screening and Preliminary Exploration

Published:2017-02-27 Issue:5 Volume:60 Page:1673-1692
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Sartori Luca¹,Mercurio Ciro¹²,Amigoni Federica¹,Cappa Anna¹,Fagá Giovanni¹,Fattori Raimondo¹,Legnaghi Elena¹,Ciossani Giuseppe³,Mattevi Andrea³^ORCID,Meroni Giuseppe¹,Moretti Loris¹^ORCID,Cecatiello Valentina⁴⁵,Pasqualato Sebastiano⁴,Romussi Alessia¹,Thaler Florian¹,Trifiró Paolo¹,Villa Manuela¹,Vultaggio Stefania¹,Botrugno Oronza A.¹,Dessanti Paola¹,Minucci Saverio¹⁶,Zagarrí Elisa¹,Carettoni Daniele⁷,Iuzzolino Lucia⁷,Varasi Mario¹,Vianello Paola¹^ORCID

Affiliation:

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

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

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

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

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

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

7. Axxam, via A. Meucci 3, 20091 Bresso, 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.6b01018

Reference55 articles.

1. Histone Lysine Methylation Dynamics: Establishment, Regulation, and Biological Impact

2. Histone methylation: a dynamic mark in health, disease and inheritance

3. SnapShot: Histone Modifications

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

5. LSD1 inhibition: a therapeutic strategy in cancer?

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