M
Myriam Ajakane
Researcher at GlaxoSmithKline
Publications - 4
Citations - 344
Myriam Ajakane is an academic researcher from GlaxoSmithKline. The author has contributed to research in topics: Visceral leishmaniasis & Benzimidazole. The author has an hindex of 3, co-authored 4 publications receiving 287 citations.
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Journal ArticleDOI
Discovery of Epigenetic Regulator I-BET762: Lead Optimization to Afford a Clinical Candidate Inhibitor of the BET Bromodomains
Olivier Mirguet,Romain Luc Marie Gosmini,Jérôme Toum,Catherine A. Clément,Mélanie Barnathan,Jean-Marie Brusq,Jacqueline Elizabeth Mordaunt,Grimes Richard Martin,Miriam Crowe,Olivier Pineau,Myriam Ajakane,Alain Claude-Marie Daugan,Phillip Jeffrey,Leanne Cutler,Andrea C. Haynes,Nicholas Smithers,Chun-wa Chung,Paul Bamborough,Iain Uings,Antonia J. Lewis,Jason Witherington,Nigel J. Parr,Rab K. Prinjha,Edwige Nicodeme +23 more
TL;DR: This work has yielded a potent, selective compound I-BET762 that is now under evaluation in a phase I/II clinical trial for nuclear protein in testis (NUT) midline carcinoma and other cancers.
Journal ArticleDOI
Identification of GSK3186899/DDD853651 as a Preclinical Development Candidate for the Treatment of Visceral Leishmaniasis.
Michael G. Thomas,Manu De Rycker,Myriam Ajakane,Sebastian Albrecht,Ana Isabel Alvarez-Pedraglio,Markus Boesche,Stephen Brand,Lorna Campbell,Juan Cantizani-Perez,Laura A. T. Cleghorn,Royston C. B. Copley,Sabrinia D. Crouch,Alain Claude-Marie Daugan,Gerard Drewes,Santiago Ferrer,Sonja Ghidelli-Disse,Silvia Gonzalez,Stephanie Gresham,Alan P. Hill,Sean J. Hindley,Rhiannon Lowe,Claire J. MacKenzie,Lorna MacLean,Sujatha Manthri,Franck Martin,Juan Miguel-Siles,Van Loc Nguyen,Suzanne Norval,Maria Osuna-Cabello,Andrew Woodland,Stephen Patterson,Imanol Peña,Maria Teresa Quesada-Campos,Iain H. Reid,Charlotte Revill,Jennifer Riley,Jose Ramon Ruiz-Gomez,Yoko Shishikura,Frederick R. C. Simeons,Alasdair Smith,Victoria Smith,Daniel Spinks,Laste Stojanovski,John Thomas,Stephen Thompson,Tim Underwood,David W. Gray,Jose M. Fiandor,Ian H. Gilbert,Paul G. Wyatt,Kevin D. Read,Timothy J. Miles +51 more
TL;DR: The optimization of a phenotypic hit against Leishmania donovani, the major causative organism of VL, is described, to balance solubility and metabolic stability while maintaining potency.
Journal ArticleDOI
Discovery and Optimization of Potent, Selective, and in Vivo Efficacious 2-Aryl Benzimidazole BCATm Inhibitors
Hongfeng Deng,Jingye Zhou,Flora S. Sundersingh,Jeffrey A. Messer,Donald O. Somers,Myriam Ajakane,Christopher C. Arico-Muendel,Arthur Beljean,Svetlana L. Belyanskaya,Ryan P. Bingham,Emily Blazensky,Anne-Benedicte Boullay,Eric Boursier,Jing Chai,Paul S. Carter,Chun-wa Chung,Alain Claude-Marie Daugan,Yun Ding,Kenny Herry,Clare I. Hobbs,Eric Humphries,Christopher S. Kollmann,Van Loc Nguyen,Edwige Nicodeme,Sarah E. Smith,Nerina Dodic,Nicolas Ancellin +26 more
TL;DR: X-ray structure revealed that 8b binds to the active site of BACTm in a unique mode via multiple H-bond and van der Waals interactions, which led to the discovery of a highly potent and selective compound, 1-(3-(5-bromothiophene- 2-carboxamido)cyclohexyl)-N-methyl-2-(pyridin-2-yl)-1H-benzo[d]imidazole-
Journal ArticleDOI
Identification of 6-amino-1H-pyrazolo[3,4-d]pyrimidines with in vivo efficacy against visceral leishmaniasis
Michael G. Thomas,Manu De Rycker,Myriam Ajakane,Sabrinia D. Crouch,Lorna Campbell,Alain Claude-Marie Daugan,Gloria Fra,César Guerrero,Claire J. MacKenzie,Lorna MacLean,Sujatha Manthri,Franck Martin,Suzanne Norval,Maria Osuna-Cabello,Jennifer Riley,Yoko Shishikura,Juan Miguel-Siles,Frederick R. C. Simeons,Laste Stojanovski,John Thomas,Stephen Thompson,Raul F. Velasco,Jose M. Fiandor,Paul G. Wyatt,Kevin D. Read,Ian H. Gilbert,Timothy J. Miles +26 more
TL;DR: The development of a chemical series with oral efficacy against visceral leishmaniasis is described and a new drug candidate is developed.