L
Lourdes Rueda
Researcher at GlaxoSmithKline
Publications - 12
Citations - 237
Lourdes Rueda is an academic researcher from GlaxoSmithKline. The author has contributed to research in topics: Chemistry & DNA methylation. The author has an hindex of 6, co-authored 9 publications receiving 119 citations.
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Journal ArticleDOI
Discovery of a first-in-class reversible DNMT1-selective inhibitor with improved tolerability and efficacy in acute myeloid leukemia.
Melissa B. Pappalardi,Kathryn Keenan,Mark Cockerill,Wendy A. Kellner,Alexandra Stowell,Christian S. Sherk,Kristen Wong,Sarath Pathuri,Jacques Briand,Michael Steidel,Phil Chapman,Arthur Groy,Ashley K. Wiseman,Charles F. McHugh,Nino Campobasso,Alan P. Graves,Emma E. Fairweather,Thilo Werner,Ali Raoof,Roger J. Butlin,Lourdes Rueda,John R. Horton,David T. Fosbenner,Cunyu Zhang,Jessica L. Handler,Morris Muliaditan,Makda Mebrahtu,Jon Paul Jaworski,Dean E. McNulty,Charlotte Burt,H. Christian Eberl,Amy N. Taylor,Thau F. Ho,Susan Merrihew,Shawn W. Foley,Anna Rutkowska,Mei Li,Stuart Paul Romeril,Kristin M. Goldberg,Xing Zhang,Christopher S. Kershaw,Marcus Bantscheff,Anthony J. Jurewicz,Elisabeth A. Minthorn,Paola Grandi,Mehul Patel,Andrew B. Benowitz,Helai P. Mohammad,Aidan G. Gilmartin,Rab K. Prinjha,Donald J. Ogilvie,Christopher L. Carpenter,Dirk A. Heerding,Stephen B. Baylin,Peter A. Jones,Xiaodong Cheng,Bryan W. King,Juan I. Luengo,Allan M. Jordan,Ian D. Waddell,Ryan G. Kruger,Michael T. McCabe +61 more
TL;DR: The discovery of GSK3685032 is reported, a potent first-in-class DNMT1-selective inhibitor that was shown via crystallographic studies to compete with the active-site loop ofDNMT1 for penetration into hemi-methylated DNA between two CpG base pairs.
Journal ArticleDOI
In vitro and in vivo induction of fetal hemoglobin with a reversible and selective DNMT1 inhibitor
Aidan G. Gilmartin,Arthur Groy,Elizabeth R. Gore,Charity Atkins,Edward Long,Monica N. Montoute,Zining Wu,Wendy S. Halsey,Dean E. McNulty,Daniela Ennulat,Lourdes Rueda,Melissa B. Pappalardi,Ryan G. Kruger,Michael T. McCabe,Ali Raoof,Roger J. Butlin,Alexandra Stowell,Mark Cockerill,Ian D. Waddell,Donald J. Ogilvie,Juan I. Luengo,Allan M. Jordan,Andrew B. Benowitz +22 more
TL;DR: It is concluded that in these preclinical models, selective, reversible inhibition of DNMT1 is sufficient for the induction of HbF, and is well-tolerated.
Journal ArticleDOI
Cyclopropyl Carboxamides: A New Oral Antimalarial Series Derived from the Tres Cantos Anti-Malarial Set (TCAMS)
Lourdes Rueda,Isabel Castellote,Julia Castro-Pichel,María J. Chaparro,Juan C. de la Rosa,Adolfo García-Pérez,Mariola Gordo,María Belén Jiménez-Díaz,Albane Kessler,Simon J. F. Macdonald,María Santos Martínez,Laura M. Sanz,Francisco-Javier Gamo,Esther Fernández +13 more
TL;DR: Rapid triaging of three series of related hits selected from the Tres Cantos Anti-Malarial Set (TCAMS) are described, and a triazolopyrimidine series was deprioritized due to delayed inhibition of parasite growth.
Journal ArticleDOI
Cyclopropyl Carboxamides, a Chemically Novel Class of Antimalarial Agents Identified in a Phenotypic Screen
Laura M. Sanz,M. Belen Jiménez-Díaz,Benigno Crespo,Cristina De-Cozar,M. Jesus Almela,Iñigo Angulo-Barturen,Pablo Castañeda,Javier Ibáñez,Esther Fernández,Santiago Ferrer,Esperanza Herreros,Sonia Lozano,María Santos Martínez,Lourdes Rueda,Jeremy N. Burrows,Jose F. Garcia-Bustos,Francisco-Javier Gamo +16 more
TL;DR: The biological characterization of this chemical family with the generic name cyclopropyl carboxamides is described, showing that inhibition of their still unknown target has very favorable pharmacological consequences but the compounds themselves seem to select for resistance at a high frequency.
Journal ArticleDOI
Development of Chemical Entities Endowed with Potent Fast-Killing Properties against Plasmodium falciparum Malaria Parasites.
Alexios N Matralis,Adnan Malik,Maria Penzo,Maria Penzo,Inmaculada Moreno,Maria Jesus Almela,Isabel Camino,Benigno Crespo,Anas Saadeddin,Sonja Ghidelli-Disse,Lourdes Rueda,Félix Calderón,Simon A. Osborne,Gerard Drewes,Markus Boesche,Elena Fernández-Álvaro,Jose Ignacio Martin Hernando,David A. Baker +17 more
TL;DR: The medicinal chemistry efforts focused on a cGMP-dependent protein kinase (PKG) inhibitor scaffold are described, leading to the identification of novel chemical entities with very potent, similar to artemisinins, fast-killing potency against asexual blood stages that cause disease, and activity against gametocyte activation that is required for transmission.