Stefan Knapp

Research interests

Publications

• Trends in kinase drug discovery: targets, indications and inhibitor design

  Nature Reviews Drug Discovery · 2021 · https://doi.org/10.1038/s41573-021-00252-y

• Accurate calculation of the absolute free energy of binding for drug molecules

  Chemical Science · 2015 · 10.1039/c5sc02678d

• The promise and peril of chemical probes

  Nature Chemical Biology · 2015 · https://doi.org/10.1038/nchembio.1867

• Comprehensive characterization of the Published Kinase Inhibitor Set

  Nature Biotechnology · 2015 · 10.1038/nbt.3374

• Exploration of Type II Binding Mode: A Privileged Approach for Kinase Inhibitor Focused Drug Discovery?

  ACS Chemical Biology · 2014 · https://doi.org/10.1021/cb500129t

• Targeting bromodomains: epigenetic readers of lysine acetylation

  Nature Reviews Drug Discovery · 2014 · https://doi.org/10.1038/nrd4286

• Stereospecific targeting of MTH1 by (S)-crizotinib as an anticancer strategy

  Nature · 2014 · 10.1038/nature13194

• Copper is required for oncogenic BRAF signalling and tumorigenesis

  Nature · 2014 · 10.1038/nature13180

• Dual kinase-bromodomain inhibitors for rationally designed polypharmacology

  Nature Chemical Biology · 2014 · 10.1038/nchembio.1471

• Structural Basis for Cul3 Protein Assembly with the BTB-Kelch Family of E3 Ubiquitin Ligases

  Journal of Biological Chemistry · 2013 · https://doi.org/10.1074/jbc.m112.437996

• RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain

  Proceedings of the National Academy of Sciences · 2013 · https://doi.org/10.1073/pnas.1310658110

• The bromodomain interaction module

  FEBS Letters · 2012 · 10.1016/j.febslet.2012.04.045

• Small-Molecule Inhibition of BRDT for Male Contraception

  Cell · 2012 · 10.1016/j.cell.2012.06.045

• Histone Recognition and Large-Scale Structural Analysis of the Human Bromodomain Family

  Cell · 2012 · https://doi.org/10.1016/j.cell.2012.02.013

• Bromodomains as therapeutic targets

  Expert Reviews in Molecular Medicine · 2011 · 10.1017/s1462399411001992

• Structurally Sophisticated Octahedral Metal Complexes as Highly Selective Protein Kinase Inhibitors

  Journal of the American Chemical Society · 2011 · https://doi.org/10.1021/ja1112996

• The (un)targeted cancer kinome

  Nature Chemical Biology · 2010 · 10.1038/nchembio.297

• Selective inhibition of BET bromodomains

  Nature · 2010 · https://doi.org/10.1038/nature09504

• PIM serine/threonine kinases in the pathogenesis and therapy of hematologic malignancies and solid cancers

  Haematologica · 2010 · 10.3324/haematol.2009.017079

• Large-Scale Structural Analysis of the Classical Human Protein Tyrosine Phosphatome

  Cell · 2009 · 10.1016/j.cell.2008.11.038

• Linear Motif Atlas for Phosphorylation-Dependent Signaling

  Science Signaling · 2008 · 10.1126/scisignal.1159433

• The structure of P‐TEFb (CDK9/cyclin T1), its complex with flavopiridol and regulation by phosphorylation

  The EMBO Journal · 2008 · 10.1038/emboj.2008.121

• A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases

  Proceedings of the National Academy of Sciences · 2007 · 10.1073/pnas.0708800104

• The molecular mechanism of nitrogen-containing bisphosphonates as antiosteoporosis drugs

  Proceedings of the National Academy of Sciences · 2006 · 10.1073/pnas.0601643103

• Structural Characterization of the GSK-3β Active Site Using Selective and Non-selective ATP-mimetic Inhibitors

  Journal of Molecular Biology · 2003 · 10.1016/j.jmb.2003.08.031

• Crystal structure of the tetrameric Mad1–Mad2 core complex: implications of a ‘safety belt’ binding mechanism for the spindle checkpoint

  The EMBO Journal · 2002 · 10.1093/emboj/21.10.2496

• Critical Residues for Structure and Catalysis in Short-chain Dehydrogenases/Reductases

  Journal of Biological Chemistry · 2002 · 10.1074/jbc.m202160200

Current projects

No projects listed.