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Esther Fernández
Researcher at GlaxoSmithKline
Publications - 23
Citations - 497
Esther Fernández is an academic researcher from GlaxoSmithKline. The author has contributed to research in topics: Plasmodium falciparum & Skarn. The author has an hindex of 11, co-authored 22 publications receiving 426 citations.
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Journal ArticleDOI
Synthesis and Structure–Activity Relationships of 4-Pyridones as Potential Antimalarials
Clive Yeates,John F. Batchelor,Edward C. Capon,Neil J. Cheesman,Mitch Fry,Hudson Alan Thomas,Mary Pudney,Helen Trimming,James Michael Woolven,Jose M. Bueno,Jesús Chicharro,Esther Fernández,Jose M. Fiandor,Domingo Gargallo-Viola,Federico Gómez de las Heras,Esperanza Herreros,María Luisa León +16 more
TL;DR: A series of diaryl ether substituted 4-pyridones have been identified as having potent antimalarial activity superior to that of chloroquine against Plasmodium falciparum in vitro and murine PlasModium yoelii in vivo through a systematic study of the effects of varying the side chain on activity.
Journal ArticleDOI
An Invitation to Open Innovation in Malaria Drug Discovery: 47 Quality Starting Points from the TCAMS.
Félix Calderón,David Barros,Jose M. Bueno,Jose M. Coteron,Esther Fernández,Francisco-Javier Gamo,Jose Luis Lavandera,María Luisa León,Simon J. F. Macdonald,Araceli Mallo,Pilar Manzano,Esther Porras,Jose M. Fiandor,Julia Castro +13 more
TL;DR: This work has identified 47 starting points for lead optimization by using an agglomerative structural clustering technique followed by computational filters such as antimalarial activity, physicochemical properties, and dissimilarity to known antimalaria structures.
Journal ArticleDOI
Structural Insights into PROTAC-Mediated Degradation of Bcl-xL
Chun-wa Chung,Han Dai,Esther Fernández,Christopher P. Tinworth,Ian Churcher,Jenni Cryan,Jane Denyer,John D. Harling,Agnieszka Konopacka,Markus A. Queisser,Christopher J. Tame,Gillian F. Watt,Fan Jiang,Dongming Qian,Andrew B. Benowitz +14 more
TL;DR: The design, characterization and X-ray structure of a VHL E3 ligase-recruiting Bcl-xL PROTAC degrader reveals an extensive network of neo-interactions, between the E3ligase and the target protein, and between non-cognate parts of the PROTAC and partner proteins.
Journal ArticleDOI
Hundreds of dual-stage antimalarial molecules discovered by a functional gametocyte screen.
Celia Miguel-Blanco,Celia Miguel-Blanco,Irene Molina,Ana I. Bardera,Beatriz Hernández Díaz,Laura Fernández de las Heras,Sonia Lozano,Carolina González,Janneth Rodrigues,Michael J. Delves,Andrea Ruecker,Gonzalo Colmenarejo,Sara Viera,Maria Santos Martinez-Martinez,Esther Fernández,Jake Baum,Robert E. Sinden,Esperanza Herreros +17 more
TL;DR: This TCAMS gametocyte screen provides 276 promising antimalarial molecules with dual asexual/sexual activity, representing starting points for target identification and candidate selection.
Journal ArticleDOI
A new in vivo screening paradigm to accelerate antimalarial drug discovery.
María Belén Jiménez-Díaz,Sara Viera,Javier Ibáñez,Teresa Mulet,Noemí Magán-Marchal,Helen Garuti,Vanessa Gómez,Lorena Cortés-Gil,Antonio Martinez,Santiago Ferrer,María T. Fraile,Félix Calderón,Esther Fernández,Leonard D. Shultz,Didier Leroy,David Matthew Wilson,Jose F. Garcia-Bustos,Francisco-Javier Gamo,Iñigo Angulo-Barturen +18 more
TL;DR: A global multilateral collaborative project aimed at screening the significant chemical diversity within the antimalarial in vitro hits described in the literature is a feasible task.