| # | Title | Journal | Year | Citations |
|---|
| 1 | Selective inhibition of BET bromodomains | Nature | 2010 | 3,456 |
| 2 | The use of differential scanning fluorimetry to detect ligand interactions that promote protein stability | Nature Protocols | 2007 | 2,069 |
| 3 | Histone Recognition and Large-Scale Structural Analysis of the Human Bromodomain Family | Cell | 2012 | 1,368 |
| 4 | Epigenetic protein families: a new frontier for drug discovery | Nature Reviews Drug Discovery | 2012 | 1,161 |
| 5 | Targeting bromodomains: epigenetic readers of lysine acetylation | Nature Reviews Drug Discovery | 2014 | 1,044 |
| 6 | Toward a unified nomenclature for mammalian ADP-ribosyltransferases | Trends in Biochemical Sciences | 2010 | 724 |
| 7 | The promise and peril of chemical probes | Nature Chemical Biology | 2015 | 698 |
| 8 | Chemical screening methods to identify ligands that promote protein stability, protein crystallization, and structure determination | Proceedings of the National Academy of Sciences of the United States of America | 2006 | 526 |
| 9 | Self-renewal as a therapeutic target in human colorectal cancer | Nature Medicine | 2014 | 438 |
| 10 | Large-Scale Structural Analysis of the Classical Human Protein Tyrosine Phosphatome | Cell | 2009 | 421 |
| 11 | Family-wide chemical profiling and structural analysis of PARP and tankyrase inhibitors | Nature Biotechnology | 2012 | 410 |
| 12 | Gain-of-function p53 mutants co-opt chromatin pathways to drive cancer growth | Nature | 2015 | 386 |
| 13 | Bromodomains as therapeutic targets | Expert Reviews in Molecular Medicine | 2011 | 368 |
| 14 | Small-Molecule Inhibition of BRDT for Male Contraception | Cell | 2012 | 353 |
| 15 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases | Proceedings of the National Academy of Sciences of the United States of America | 2007 | 342 |
| 16 | Stereospecific targeting of MTH1 by (S)-crizotinib as an anticancer strategy | Nature | 2014 | 336 |
| 17 | The bromodomain interaction module | FEBS Letters | 2012 | 325 |
| 18 | Crystal structures of histone demethylase JMJD2A reveal basis for substrate specificity | Nature | 2007 | 297 |
| 19 | Dual kinase-bromodomain inhibitors for rationally designed polypharmacology | Nature Chemical Biology | 2014 | 296 |
| 20 | A roadmap to generate renewable protein binders to the human proteome | Nature Methods | 2011 | 277 |
| 21 | The (un)targeted cancer kinome | Nature Chemical Biology | 2010 | 267 |
| 22 | A Strategy for Modulation of Enzymes in the Ubiquitin System | Science | 2013 | 257 |
| 23 | Druggability Analysis and Structural Classification of Bromodomain Acetyl-lysine Binding Sites | Journal of Medicinal Chemistry | 2012 | 254 |
| 24 | BRD4 assists elongation of both coding and enhancer RNAs by interacting with acetylated histones | Nature Structural and Molecular Biology | 2014 | 247 |
| 25 | Structure and Biochemical Functions of SIRT6 | Journal of Biological Chemistry | 2011 | 239 |
| 26 | Protein tyrosine phosphatases as drug targets: strategies and challenges of inhibitor development | Future Medicinal Chemistry | 2010 | 236 |
| 27 | Crystal structure of the CorA Mg2+ transporter | Nature | 2006 | 233 |
| 28 | Tet3 CXXC Domain and Dioxygenase Activity Cooperatively Regulate Key Genes for Xenopus Eye and Neural Development | Cell | 2012 | 227 |
| 29 | The ins and outs of selective kinase inhibitor development | Nature Chemical Biology | 2015 | 220 |
| 30 | Structurally Sophisticated Octahedral Metal Complexes as Highly Selective Protein Kinase Inhibitors | Journal of the American Chemical Society | 2011 | 218 |
| 31 | Sgf29 binds histone H3K4me2/3 and is required for SAGA complex recruitment and histone H3 acetylation | EMBO Journal | 2011 | 218 |
| 32 | Genome-scale protein expression and structural biology of Plasmodium falciparum and related Apicomplexan organisms | Molecular and Biochemical Parasitology | 2007 | 216 |
| 33 | Rapid Covalent-Probe Discovery by Electrophile-Fragment Screening | Journal of the American Chemical Society | 2019 | 213 |
| 34 | A Potent, Selective, and Cell-Active Inhibitor of Human Type I Protein Arginine Methyltransferases | ACS Chemical Biology | 2016 | 208 |
| 35 | 3,5-Dimethylisoxazoles Act As Acetyl-lysine-mimetic Bromodomain Ligands | Journal of Medicinal Chemistry | 2011 | 204 |
| 36 | An Allosteric Inhibitor of the Human Cdc34 Ubiquitin-Conjugating Enzyme | Cell | 2011 | 203 |
| 37 | Quantitative, Wide-Spectrum Kinase Profiling in Live Cells for Assessing the Effect of Cellular ATP on Target Engagement | Cell Chemical Biology | 2018 | 197 |
| 38 | Generation of a Selective Small Molecule Inhibitor of the CBP/p300 Bromodomain for Leukemia Therapy | Cancer Research | 2015 | 193 |
| 39 | A multi-crystal method for extracting obscured crystallographic states from conventionally uninterpretable electron density | Nature Communications | 2017 | 186 |
| 40 | SMN and symmetric arginine dimethylation of RNA polymerase II C-terminal domain control termination | Nature | 2016 | 185 |
| 41 | Carbonyl Reductases: The Complex Relationships of Mammalian Carbonyl- and Quinone-Reducing Enzymes and Their Role in Physiology | Annual Review of Pharmacology and Toxicology | 2007 | 184 |
| 42 | Identification of a Chemical Probe for Bromo and Extra C-Terminal Bromodomain Inhibition through Optimization of a Fragment-Derived Hit | Journal of Medicinal Chemistry | 2012 | 184 |
| 43 | Structural Analysis Identifies Imidazo[1,2-b]Pyridazines as PIM Kinase Inhibitors with In vitro Antileukemic Activity | Cancer Research | 2007 | 183 |
| 44 | MOF and H4 K16 Acetylation Play Important Roles in DNA Damage Repair by Modulating Recruitment of DNA Damage Repair Protein Mdc1 | Molecular and Cellular Biology | 2010 | 181 |
| 45 | Structural basis and specificity of human otubain 1-mediated deubiquitination | Biochemical Journal | 2009 | 180 |
| 46 | Structural basis for the allosteric inhibitory mechanism of human kidney-type glutaminase (KGA) and its regulation by Raf-Mek-Erk signaling in cancer cell metabolism | Proceedings of the National Academy of Sciences of the United States of America | 2012 | 178 |
| 47 | Protein Lysine Methyltransferase G9a Inhibitors: Design, Synthesis, and Structure Activity Relationships of 2,4-Diamino-7-aminoalkoxy-quinazolines. | Journal of Medicinal Chemistry | 2010 | 177 |
| 48 | Structural diversity in the RGS domain and its interaction with heterotrimeric G protein α-subunits | Proceedings of the National Academy of Sciences of the United States of America | 2008 | 174 |
| 49 | The Crystal Structure of the Human Toll-like Receptor 10 Cytoplasmic Domain Reveals a Putative Signaling Dimer | Journal of Biological Chemistry | 2008 | 171 |
| 50 | EMA401, an orally administered highly selective angiotensin II type 2 receptor antagonist, as a novel treatment for postherpetic neuralgia: a randomised, double-blind, placebo-controlled phase 2 clinical trial | Lancet, The | 2014 | 171 |
