F
Francesco Rianjongdee
Researcher at GlaxoSmithKline
Publications - Â 4
Citations - Â 85
Francesco Rianjongdee is an academic researcher from GlaxoSmithKline. The author has contributed to research in topics: Bromodomain & Binding site. The author has an hindex of 2, co-authored 4 publications receiving 28 citations.
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Journal ArticleDOI
Design and Synthesis of a Highly Selective and In Vivo-Capable Inhibitor of the Second Bromodomain of the Bromodomain and Extra Terminal Domain Family of Proteins
Alex Preston,Stephen John Atkinson,Paul Bamborough,Chun-wa Chung,Peter D. Craggs,Laurie J. Gordon,Paola Grandi,James Gray,Emma J. Jones,Matthew J Lindon,Anne-Marie Michon,Darren Jason Mitchell,Rab K. Prinjha,Francesco Rianjongdee,Inmaculada Rioja,Jonathan Thomas Seal,Simon Taylor,Ian D. Wall,Robert J. Watson,James Michael Woolven,Emmanuel Hubert Demont +20 more
TL;DR: The profile of GSK046, also known as iBET-BD2, a highly selective inhibitor of the second bromodomains of the BET proteins that has undergone extensive pre-clinical in vitro and in vivo characterisation is disclosed.
Journal ArticleDOI
Discovery of a Highly Selective BET BD2 Inhibitor from a DNA-Encoded Library Technology Screening Hit.
Francesco Rianjongdee,Stephen John Atkinson,Chun-wa Chung,Paola Grandi,James Gray,Laura J. Kaushansky,Patricia F Medeiros,Cassie Messenger,Alex Phillipou,Alex Preston,Rab K. Prinjha,Inmaculada Rioja,Alexander L. Satz,Simon Taylor,Ian D. Wall,Robert J. Watson,Gang Yao,Emmanuel Hubert Demont +17 more
TL;DR: In this paper, the authors describe the discovery of a novel BET BD2-selective chemotype using a structure-based drug design from a hit identified by DNA-encoded library technologies.
Journal ArticleDOI
Fragment-based Scaffold Hopping: Identification of Potent, Selective, and Highly Soluble Bromo and Extra Terminal Domain (BET) Second Bromodomain (BD2) Inhibitors.
Jonathan Thomas Seal,Stephen John Atkinson,Paul Bamborough,Anna K. Bassil,Chun-wa Chung,James J. Foley,Laurie J. Gordon,Paola Grandi,James Gray,Lee Andrew Harrison,Ryan G. Kruger,Jeanne J. Matteo,Michael T. McCabe,Cassie Messenger,Darren Jason Mitchell,Alex Phillipou,Alex Preston,Rab K. Prinjha,Francesco Rianjongdee,Inmaculada Rioja,Simon Taylor,Ian D. Wall,Robert J. Watson,James Michael Woolven,Anastasia Wyce,Xi-Ping Zhang,Emmanuel Hubert Demont +26 more
TL;DR: In this paper, the authors reveal the identification of potent and selective drug-like pan-BD2 inhibitors, such as pyrazole 23 (GSK809) and furan 24(GSK743), derived from the pyrrole fragment 6.
Journal ArticleDOI
Template-Hopping Approach Leads to Potent, Selective, and Highly Soluble Bromo and Extraterminal Domain (BET) Second Bromodomain (BD2) Inhibitors.
Aylott Helen Elizabeth,Stephen John Atkinson,Paul Bamborough,Anna K. Bassil,Chun-wa Chung,Laurie J. Gordon,Paola Grandi,James Gray,Lee Andrew Harrison,Thomas George Christopher Hayhow,Cassie Messenger,Darren Jason Mitchell,Alexander N Phillipou,Alex Preston,Rab K. Prinjha,Francesco Rianjongdee,Inmaculada Rioja,Jonathan Thomas Seal,Ian D. Wall,Robert J. Watson,James Michael Woolven,Emmanuel Hubert Demont +21 more
TL;DR: In this paper, the second bromodomain (BD2) was replaced with a heterocyclic ring to mitigate the genotoxicity risk of GSK046.