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

DOI: 10.1021/acs.jmedchem.6b01019

Source and publish data:

Journal of Medicinal Chemistry p. 1693 - 1715 (2017)

Update date:2022-08-15

Topics:

Authors:

Vianello, Paola

Sartori, Luca

Amigoni, Federica

Cappa, Anna

Fagá, Giovanni

Fattori, Raimondo

Legnaghi, Elena

Ciossani, Giuseppe

Mattevi, Andrea

Meroni, Giuseppe

Moretti, Loris

Cecatiello, Valentina

Pasqualato, Sebastiano

Romussi, Alessia

Thaler, Florian

Trifiró, Paolo

Villa, Manuela

Botrugno, Oronza A.

Dessanti, Paola

Minucci, Saverio

Vultaggio, Stefania

Zagarrí, Elisa

Varasi, Mario

Mercurio, Ciro

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Article abstract of DOI:10.1021/acs.jmedchem.6b01019

The balance of methylation levels at histone H3 lysine 4 (H3K4) is regulated by KDM1A (LSD1). KDM1A is overexpressed in several tumor types, thus representing an emerging target for the development of novel cancer therapeutics. We have previously describe

Full text of DOI:10.1021/acs.jmedchem.6b01019

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