L
Laurens Kruidenier
Researcher at GlaxoSmithKline
Publications - 28
Citations - 2998
Laurens Kruidenier is an academic researcher from GlaxoSmithKline. The author has contributed to research in topics: T cell & Cytokine. The author has an hindex of 17, co-authored 28 publications receiving 2482 citations. Previous affiliations of Laurens Kruidenier include University of Hertfordshire & University of London.
Papers
More filters
Journal ArticleDOI
Catalytic in vivo protein knockdown by small-molecule PROTACs
Daniel P. Bondeson,Alina Mares,Ian Edward David Smith,Ko Eunhwa,Sebastien Andre Campos,Afjal Hussain Miah,Katie E Mulholland,Natasha Routly,Dennis L. Buckley,Jeffrey L. Gustafson,Nico Zinn,Paola Grandi,Satoko Shimamura,Giovanna Bergamini,Maria Faelth-Savitski,Marcus Bantscheff,Carly S. Cox,Deborah A. Gordon,Ryan R. Willard,John J. Flanagan,Linda N. Casillas,Bartholomew J. Votta,Willem den Besten,Kristoffer Famm,Laurens Kruidenier,Paul S. Carter,John D. Harling,Ian Churcher,Craig M. Crews +28 more
TL;DR: Major improvements to the proteolysis targeting chimeras (PROTACs) method are described, a chemical knockdown strategy in which a heterobifunctional molecule recruits a specific protein target to an E3 ubiquitin ligase, resulting in the target's ubiquitination and degradation.
Journal ArticleDOI
A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response
Laurens Kruidenier,Chun-wa Chung,Zhongjun Cheng,John Liddle,K.H. Che,K.H. Che,Gerard Joberty,Marcus Bantscheff,C. Bountra,Angela Bridges,Hawa Diallo,Dirk Eberhard,Sue Hutchinson,Emma J. Jones,Roy Katso,Melanie Leveridge,Palwinder K. Mander,J. Mosley,Cesar Ramirez-Molina,Paul Rowland,Christopher J. Schofield,Robert J. Sheppard,Julia Smith,Catherine Swales,Robert Tanner,Pamela Thomas,Anthony Tumber,Gerard Drewes,Udo Oppermann,Udo Oppermann,Dinshaw J. Patel,Kevin Lee,Kevin Lee,David Matthew Wilson +33 more
TL;DR: It is demonstrated that the first small-molecule catalytic site inhibitor that is selective for the H3K27me3-specific JMJ subfamily binds in a novel manner and reduces lipopolysaccharide-induced proinflammatory cytokine production by human primary macrophages, a process that depends on both JMJD3 and UTX.
Journal ArticleDOI
Contrasting roles of histone 3 lysine 27 demethylases in acute lymphoblastic leukaemia
Panagiotis Ntziachristos,Panagiotis Ntziachristos,Aristotelis Tsirigos,G. Grant Welstead,Thomas Trimarchi,Sofia Bakogianni,Luyao Xu,Evangelia Loizou,Linda Holmfeldt,Alexandros Strikoudis,Bryan W. King,Jasper Mullenders,Jared Becksfort,Jelena Nedjic,Elisabeth Paietta,Martin S. Tallman,Jacob M. Rowe,Giovanni Tonon,Takashi Satoh,Laurens Kruidenier,Rab K. Prinjha,Shizuo Akira,Pieter Van Vlierberghe,Adolfo A. Ferrando,Rudolf Jaenisch,Charles G. Mullighan,Iannis Aifantis +26 more
TL;DR: It is shown that two proteins with a similar enzymatic function can have opposing roles in the context of the same disease, paving the way for treating haematopoietic malignancies with a new category of epigenetic inhibitors.
Journal ArticleDOI
Selective class IIa histone deacetylase inhibition via a nonchelating zinc-binding group
Mercedes Lobera,Kevin P. Madauss,Denise T Pohlhaus,Quentin G. Wright,Mark Trocha,Darby Schmidt,Erkan Baloglu,Ryan P. Trump,Martha S. Head,Glenn A. Hofmann,Monique F. Murray-Thompson,Benjamin Schwartz,Subhas J. Chakravorty,Zining Wu,Palwinder K. Mander,Laurens Kruidenier,Robert A. Reid,William Burkhart,Brandon J. Turunen,James X Rong,James X Rong,Craig D. Wagner,Mary B. Moyer,Carrow I. Wells,Xuan Hong,John T. Moore,Jon D. Williams,Dulce Soler,Shomir Ghosh,Michael A. Nolan +29 more
TL;DR: The discovery of inhibitors that fill this void with an unprecedented metal-binding group, trifluoromethyloxadiazole (TFMO), which circumvents the selectivity and pharmacologic liabilities of hydroxamates is reported.
Journal ArticleDOI
Targeting Gut T Cell Ca2+ Release-Activated Ca2+ Channels Inhibits T Cell Cytokine Production and T-Box Transcription Factor T-Bet in Inflammatory Bowel Disease
Antonio Di Sabatino,Laura Rovedatti,Rejbinder Kaur,J.P. Spencer,Jon T. Brown,Valerie Morisset,Paolo Biancheri,N A B Leakey,Jonathan I. Wilde,Laurie Scott,Gino Roberto Corazza,Kevin Lee,Neel Sengupta,Charles H. Knowles,Martin J. Gunthorpe,Peter G. McLean,Thomas T. MacDonald,Laurens Kruidenier +17 more
TL;DR: Evidence is provided that the suppression of CRAC channel function may dampen the increased T cell response in the inflamed gut, thus suggesting a promising role for CRAC inhibitor drugs in the therapeutic management of patients with IBD.