Kruidenier et al. reply

Laurens Kruidenier, Chun-wa Chung (), Zhongjun Cheng, John Liddle, KaHing Che, Gerard Joberty, Marcus Bantscheff, Chas Bountra, Angela Bridges, Hawa Diallo, Dirk Eberhard, Sue Hutchinson, Emma Jones, Roy Katso, Melanie Leveridge, Palwinder K. Mander, Julie Mosley, Cesar Ramirez-Molina, Paul Rowland, Christopher J. Schofield, Robert J. Sheppard, Julia E. Smith, Catherine Swales, Robert Tanner, Pamela Thomas, Anthony Tumber, Gerard Drewes, Udo Oppermann, Dinshaw J. Patel, Kevin Lee and David M. Wilson
Additional contact information
Laurens Kruidenier: Epinova DPU, Immuno-Inflammation Therapy Area, GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, UK
Chun-wa Chung: Platform Technology and Science, GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, UK
Zhongjun Cheng: Memorial Sloan-Kettering Cancer Center, 1275 York Avenue
John Liddle: Epinova DPU, Immuno-Inflammation Therapy Area, GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, UK
KaHing Che: Structural Genomics Consortium, University of Oxford, Old Road Campus, Roosevelt Drive, Headington OX3 7DQ, UK
Gerard Joberty: Cellzome AG, Meyerhofstrasse 1, 69117 Heidelberg, Germany
Marcus Bantscheff: Cellzome AG, Meyerhofstrasse 1, 69117 Heidelberg, Germany
Chas Bountra: Structural Genomics Consortium, University of Oxford, Old Road Campus, Roosevelt Drive, Headington OX3 7DQ, UK
Angela Bridges: Platform Technology and Science, GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, UK
Hawa Diallo: Epinova DPU, Immuno-Inflammation Therapy Area, GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, UK
Dirk Eberhard: Cellzome AG, Meyerhofstrasse 1, 69117 Heidelberg, Germany
Sue Hutchinson: Platform Technology and Science, GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, UK
Emma Jones: Platform Technology and Science, GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, UK
Roy Katso: Platform Technology and Science, GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, UK
Melanie Leveridge: Platform Technology and Science, GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, UK
Palwinder K. Mander: Epinova DPU, Immuno-Inflammation Therapy Area, GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, UK
Julie Mosley: Platform Technology and Science, GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, UK
Cesar Ramirez-Molina: Epinova DPU, Immuno-Inflammation Therapy Area, GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, UK
Paul Rowland: Platform Technology and Science, GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, UK
Christopher J. Schofield: Structural Genomics Consortium, University of Oxford, Old Road Campus, Roosevelt Drive, Headington OX3 7DQ, UK
Robert J. Sheppard: Epinova DPU, Immuno-Inflammation Therapy Area, GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, UK
Julia E. Smith: Epinova DPU, Immuno-Inflammation Therapy Area, GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, UK
Catherine Swales: Botnar Research Centre, NIHR Biomedical Research Unit, University of Oxford OX3 7LD
Robert Tanner: Platform Technology and Science, GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, UK
Pamela Thomas: Platform Technology and Science, GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, UK
Anthony Tumber: Structural Genomics Consortium, University of Oxford, Old Road Campus, Roosevelt Drive, Headington OX3 7DQ, UK
Gerard Drewes: Cellzome AG, Meyerhofstrasse 1, 69117 Heidelberg, Germany
Udo Oppermann: Structural Genomics Consortium, University of Oxford, Old Road Campus, Roosevelt Drive, Headington OX3 7DQ, UK
Dinshaw J. Patel: Memorial Sloan-Kettering Cancer Center, 1275 York Avenue
Kevin Lee: Epinova DPU, Immuno-Inflammation Therapy Area, GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, UK
David M. Wilson: Epinova DPU, Immuno-Inflammation Therapy Area, GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, UK

Nature, 2014, vol. 514, issue 7520, E2-E2

Abstract: Abstract Replying to B. Heinemann et al. Nature 514, 10.1038/nature13688 (2014) We welcome the accompanying Comment1 by Heinemann et al. , in which the authors use an extensive panel of sensitive KDM assays to independently confirm our results2 that GSK-J1 is a potent KDM6 inhibitor. Additionally, Heinemann et al.1 demonstrate that GSK-J1 has some, albeit weaker, activity towards KDM5B and KDM5C, for which we only had preliminary data available at the time of our original publication. As our jumonji assay portfolio expands, we have continued to update the GSK-J1 activity profile on the SGC website ( http://www.thesgc.org/chemical-probes/GSKJ1 ); this includes KDM5 inhibition activity by GSK-J1 similar to that reported by Heinemann. In conclusion, GSK-J1 remains the most selective KDM inhibitor yet disclosed and thus a valuable chemical tool.

Date: 2014
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DOI: 10.1038/nature13689

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