2021
109. Tarantelli, C., Cannas, E., Ekeh, H., Moscatello, C., Gaudio, E., Cascione, L., Napoli, S., Rech, C., Testa, A., Maniaci, C., Rinaldi, A., Zucca, E., Stathis, A., Ciulli, A., Bertoni, F.
The bromodomain and extra-terminal domain degrader MZ1 exhibits preclinical anti-tumoral activity in diffuse large B-cell lymphoma of the activated B cell-like type
Explor. Target Antitumor Ther. 2021, 2, 586–601
- PMID: 36046113 PMCID: PMC9400774
108. Klein, V.G., Bond, A.G., Craigon, C., Lokey, R.S.*, Ciulli, A.*
Amide-to-ester substitution as a strategy for optimizing PROTAC permeability and cellular activity
J. Med. Chem. 2021, 64 (24), 18082–18101
- PMID: 34881891 PMCID: PMC8713283
- Pre-print posted at ChemRxiv on 5 July 2021; DOI: 10.33774/chemrxiv-2021-47tqn
- See Figures here and here
- Listed as 2nd Most Read Article in the journal (1-month timeframe, Jan 2022)
- Featured as Literature Spotlight in the monthly EFMC MedChemBioWatch newsletter (February 2022)
107. Müller, S., Ackloo, S., Al Chawaf, A., Al-Lazikani, B., Antolin, A., Baell, J.B., Beck, H., Beedie, S., Betz, U.A.K., Arruda Bezerra, G., Brennan, P.E., Brown, D., Brown, P.J., Bullock, A.N., Carter, A.J., Chaikuad, A., Chaineau, M., Ciulli, A., Collins, I., Dreher, J., Drewry, D., Edfeldt, K., Edwards, A.M., Egner, U., Frye, S.V., Fuchs, S.M., Hall, M.D., Hartung, I.V., Hillisch, A., Hitchcock, S.H., Homan, E., Kannan, N., Kiefer, J.R., Knapp, S., Kostic, M., Kubicek, S., Leach, A.R., Lindemann, S., Marsden, B.D., Matsui, H., Meier, J.L., Merk, D., Michel, M., Morgan, M.R., Mueller-Fahrnow, A., Owen, D.R., Perry, B.G., Rosenberg, S.H., Singh Saikatendu, K., Schapira, M., Scholten, C., Sharma, S., Simeonov, A., Sundström, M., Superti-Furga, G., Todd, M.H., Tredup, C., Vedadi, M., von Delft, F., Willson, T.M., Winter, G.E., Workman, P., Arrowsmith, C.H.
Target 2035 – update on the quest for a probe for every protein
RSC Med. Chem. 2022, 13, 13-21
- PMID: 35211674 PMCID: PMC8792830
- Selected as the inside front cover of the issue.
106. Laveglia, V., Giachetti, A., Cerofolini, L., Haubrich, K., Fragai, M., Ciulli, A., Rosato, A.
Automated Determination of Nuclear Magnetic Resonance Chemical Shift Perturbations in Ligand Screening Experiments: The PICASSO Web Server
J. Chem. Inf. Model. 2021, 61 (12), 5726–5733
- PMID: 34843238 PMCID: PMC8715503
105. Imaide, S., Riching, K.M., Makukhin, N., Vetma, V., Whitworth, C., Hughes, S.J., Trainor, N., Mahan, S.D., Murphy, N., Cowan, A.D., Chan, K.-H., Craigon, C., Testa, A., Maniaci, C., Urh, M., Daniels, D.L.*; Ciulli, A.*
Trivalent PROTACs enhance protein degradation via combined avidity and cooperativity
Nat. Chem. Biol. 2021, 17 (11), 1157–1167
- PMID: 34675414 PMCID: PMC7611906
- Pre-print posted at ChemRxiv on 12 November 2020; DOI: 10.26434/chemrxiv.13218695.v1
- See Figures here
- Covered in UoD and SLS News websites
- Covered as joint Dundee-Promega Press Release in BusinessWire
- Read the article Open Access as SharedIt version here
- Highlighted in Blog Promega Connections
- Featured in Chemical & Engineering News
- Featured in Biocentury
- Recommended in Faculty Opinions
- Featured in BiopharmaTrend
- Our trivalent PROTAC degrader SIM1 is available from Tocris (September 2021)
- The non-degrading epimer cis-SIM1 is also available from Tocris (November 2021)
104. Riching, K.M., Vasta, J.D., Hughes, S.J., Zoppi, V., Maniaci, C., Testa, A., Urh, M., Ciulli, A.*, Daniels, D.L.*
Translating PROTAC chemical series optimization into functional outcomes underlying BRD7 and BRD9 protein degradation
Curr. Res. Chem. Biol., 2021, 1, 100009
- 2nd Most Downloaded Article in the journal (April 2022)
103. Bond, A.G., Craigon, C., Chan, K.-H., Testa, A., Karapetsas, A., Fasimoye, R., Macartney, T., Blow, J.J., Alessi, D.R., Ciulli, A.*
Development of BromoTag: A “Bump-and-Hole”–PROTAC System to Induce Potent, Rapid, and Selective Degradation of Tagged Target Proteins
J. Med. Chem. 2021, 64 (20), 15477–15502
- PMID: 34652918 PMCID: PMC8558867
- See Figures here
- Featured in UoD and SLS News websites
- Listed amongst the Most Read Articles in the journal (1-month timeframe, November 2021)
- Highlighted in SynFacts
- Our BromoTag-specific bumped-PROTAC degrader AGB1 is available from Tocris (April 2022)
- The non-degrading epimer cis-AGB1 is also available from Tocris (April 2022)
- A second BromoTag-specific bumped-PROTAC degrader AGB3 is also available from Tocris (November 2022)
- Addition/Correction published (Web): January 22, 2025. DOI: 10.1021/acs.jmedchem.5c00108
102. Castro, G.V, Ciulli, A.*
Estimating the cooperativity of PROTAC-induced ternary complexes using 19F NMR displacement assay
RSC Med. Chem. 2021, 12, 1765-1770
- PMID: 34778777 PMCID: PMC8528210
- Pre-print posted at ChemRxiv on 21 June 2021; DOI: 10.33774/chemrxiv-2021-zj19k
- See Figures here
- Correction published (Web): December 20, 2021. DOI: 10.1039/D1MD90045E (Correction)
(100. & 101. Casement et al. and Bartoschik et al. book chapters)
99. Ciulli, A.*, Trainor, N.
A beginner’s guide to PROTACs and targeted protein degradation
Biochem (Lond) 2021, 43 (5), 74–79
98. Frost, J.; Rocha, S.*; Ciulli, A.*
Von Hippel-Lindau (VHL) small molecule inhibitor binding increases stability and intracellular levels of VHL protein
J. Biol. Chem. 2021, 297 (2), 100910
- PMID: 34174286 PMCID: PMC8313594
- Pre-print posted at BioRxiv on 12 April 2021; DOI: 10.1101/2021.04.12.439487
- See Figures here
- Julianty Frost is recipient of one of the 2022 JBC Herbert Tabor Early Career Investigator Awards, recognizing first authors of exceptional JBC papers that appeared in the preceding year
97. Ciulli, A.; Hamann, L.; Jahnke, W.; Kalgutkar, A.S.; Magauer, T.; Ritter, T.; Steadman, V.; Williams, S.D.; Winter, G.; Hoegenauer, K.; Krawinkler, K.H.; Stepan, A.F.
The 2nd Alpine Winter Conference on Medicinal and Synthetic Chemistry.
ChemMedChem 2021, 16 (15), 2417-2413
- PMID: 34114371
96. Ciulli, A.*; Wertz, I.E.*
Editorial overview: Hot targets and new modalities.
Curr. Opin. Chem. Biol. 2021, 62, A1-A3
- PMID: 34116929
95. Pietrobono, S.; Gaudio, E.; Gagliardi, S.; Zitani, M.; Carrassa, L.; Migliorini, F.; Petricci, E.; Manetti, F.; Makukhin, N.; Bond, A.G.; Paradise, B.D.; Ciulli, A.; Fernandez-Zapico, M.E.; Bertoni, F.; Stecca, B.
Targeting non-canonical activation of GLI1 by the SOX2-BRD4 transcriptional complex improves the efficacy of HEDGEHOG pathway inhibition in melanoma
- PMID: 33958721 PMCID: PMC8175236
94. Farnaby, W.; Koegl, M.; McConnell, D.B.; Ciulli, A.
Transforming targeted cancer therapy with PROTACs: A forward-looking perspective
Curr. Opin. Pharmacol. 2021, 57, 175-183
- PMID: 33799000
- See more info here
- 2nd Most Downloaded Article in the journal in the last 3 months (August 2021)
93. Ramachandran, S.; Ciulli, A.*
Building ubiquitination machineries: E3 ligase multi-subunit assembly and substrate targeting by PROTACs and molecular glues
Curr. Opin. Struct. Biol. 2021, 67, 110-119
- PMID: 33271439
- See Figures here
- Top Most Downloaded Article in the journal (April 2021)
92. Ishida, T., Ciulli, A.*
E3 Ligase Ligands for PROTACs: How They Were Found and How to Discover New Ones
SLAS Discov. 2021, 26 (4), 484-502
- PMID: 33143537 PMCID: PMC8013866
- See Figures here
- Most Read article in the journal in the last 6 months (August 2021)
- Honored with the 2021 SLAS Discovery Readers Choice Award, reflecting popularity among readers throughout 2021. Read more about this here.
- Top amongst SLAS Discovery’s Editor’s Top 10 for 2021. Read the full Editorial here
- Mentioned in SLAS ELN article: “Art of the Review: SLAS Journals Authors Offer Expert Interpretation of Life Science Literature”. Read the full article here
91. Makukhin, N., Ciulli, A.*
Recent advances in synthetic and medicinal chemistry of phosphotyrosine and phosphonate- based phosphotyrosine analogues
- PMID: 34041480 PMCID: PMC8130623
- See Figures here
2020
90. Klein, V.G., Townsend, C.E., Testa, A., Zengerle, M., Maniaci, C., Hughes, S.J., Chan, K.-H., Ciulli, A., Lokey, R.S.
Understanding and improving the membrane permeability of VH032-based PROTACs
ACS Med. Chem. Lett. 2020, 11 (9), 1732-1738
- PMID: 32939229 PMCID: PMC7488288
- See Figures here
- Listed amongst the Most Read Articles in the journal (1-month timeframe: September 2020; 12-month timeframe: April 2021)
89. Bond, A.G., Testa, A., Ciulli, A.*
Stereoselective Synthesis of Allele-Specific BET Inhibitors
Org. Biomol. Chem. 2020, 18, 7533-7539
- PMID: 3275671
- Pre-print posted at ChemRxiv on 18 May 2020; https://doi.org/10.26434/chemrxiv.12317354.v1
- See Figures here
- Selected as the front cover of the issue. Read more about it here
- PDB code
88. Cipriano, A., Sbardella, G.,* Ciulli, A.*
Targeting epigenetic reader domains by chemical biology
Curr. Opin. Chem. Biol. 2020, 57, 82-94
- PMID: 32739717
- Read the article open access before September 18, 2020 via the Share Link here
- See Figures here
87. Whitworth, C., Ciulli, A.*
Protein degraders extend their reach
- PMID: 32728153
- See Figure here
- News & Views article on Banik et al. Nature 2020, DOI: 10.1038/s41586-020-2545-9
86. Simpson, L.M., Macartney, T.J., Nardin, A., Fulcher, L.J., Röth, S., Testa, A., Maniaci, C., Ciulli, A., Ganley, I.G., Sapkota, G.P.
Inducible Degradation of Target Proteins through a Tractable Affinity-Directed Protein Missile System
Cell Chem. Biol. 2020, 27 (9), 1164-1180.e5
- PMID: 32668203 PMCID: PMC7505680
- See Figures here
- Highlighted in Nature Chemical Biology
85. Testa, A., Hughes, S.J., Lucas, X., Wright, J.E., Ciulli, A.*
Structure-Based Design of a Macrocyclic PROTAC
Angew. Chem. Int. Ed. 2020, 59, 1727-1734
- PMID: 31746102 PMCID: PMC7004083
- Pre-print posted at ChemRxiv on 22 July 2019; DOI: 10.26434/chemrxiv.8967941.v1
- Selected as a “Hot paper” by the Editors of Angew. Chem. and Angew. Chem. Int. Ed.
- See Figures here
- The coordinates and structure factors of the associated co-crystal structure of the ternary complex between VHL, Brd4-BD2 and macroPROTAC-1 is available in the PDB with accession code 6SIS.
- Listed amongst the Most Accessed in the journal for the period 02/2020 to 01/2021 (April 2021)
(84. Zollman & Ciulli book chapter)
83. Hassell-Hart, S., Runcie, A.C., Krojer, T., Doyle, J., Lineham, E., Ocasio, C.A., Neto, B.A.D., Fedorov, O., Marsh, G., Maple, H., Felix, R., Banks, R., Ciulli, A., Picaud, S., Filippakopoulos, P., von Delft, F., Brennan, P., Stewart, H.J.S., Chevassut, T.J., Walker, M., Austin, C., Morley, S., Spencer, J.
Synthesis and Biological Investigation of (+)-JD1, an Organometallic BET Bromodomain Inhibitor
2019
82. Tovell, H., Testa, A., Zhou, H., Shpiro, N., Crafter, C., Ciulli, A.*, Alessi, D.R.*
Design and characterization of SGK3-PROTAC1, an isoform specific SGK3 kinase PROTAC degrader
ACS Chem. Biol. 2019, 14 (9), 2024-2034
- See Figures here
- Ranked Top amongst the Most Read Articles in the journal (1-month timeframe, Sept-Oct 2019)
- Our SGK3 degrader SGK3-PROTAC1 is available from MedChemExpress and AbMole
- Find out more about SGK3-PROTAC1 in the Chemical Probes Portal
81. Maniaci, C., Ciulli, A.*
Bifunctional chemical probes inducing protein-protein interactions
Curr. Opin. Chem. Biol. 2019, 52, 145-156
- Read the article open access until 2nd October 2019 via the Share Link here
- See Figures here
- Ranked amongst Most Popular Articles in the journal
80. Ciulli, A.*, Farnaby, W.*
Protein degradation for drug discovery. [Editorial]
Drug Discov. Today Technol. 2019 Apr 31: 1-3
79. Farnaby W, Koegl M, Roy MJ, Whitworth C, Diers E, Trainor N, Zollman D, Steurer S, Karolyi-Oezguer J, Riedmueller C, Gmaschitz T, Wachter J, Dank C, Galant M, Sharps B, Rumpel K, Traxler E, Gerstberger T, Schnitzer R, Petermann O, Greb P, Weinstabl H, Bader G, Zoephel A, Weiss-Puxbaum A, Ehrenhöfer-Wölfer K, Wöhrle S, Boehmelt G, Rinnenthal J, Arnhof H, Wiechens N, Wu MY, Owen-Hughes T, Ettmayer P, Pearson M, McConnell DB*, Ciulli A.*
BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design
Nat. Chem. Biol. 2019, 15 (7), 672-680
- 
A Publisher Correction to this article was published on 02 July 2019
- Highlighted in EurekAlert, the Medical News, and mentioned by BioWorld
- Read the article Open Access as SharedIt version here
- See Figures here
- The coordinates and structure factors of our co-crystal structures are available in the PDB. Accession codes of ternary complexes VCB (pVHL:ElonginC:ElonginB complex):PROTAC1:SMARCA2 bromodomain (PDB 6HAY), VCB:PROTAC2:SMARCA2 bromodomain (PDB 6HAX), and VCB:PROTAC2:SMARCA4 bromodomain (PDB 6HR2), as well as a binary complex between SMARCA2 bromodomain and SMARCA-BD ligand (PDB 6HAZ)
- 
Featured in a News & Views article by Daffyd Owen in Nature Chemical Biology
- 
Featured in Cancer Discovery Research Watch
- Featured in Biocentury Innovation
- Highlighted in SynFacts
- Check out Darryl McConnell’s video on Structure-Based SMARCA2 PROTAC Design here.
- Our SMARCA2/4 degrader ACBI1 (and cis-ACBI1) are available from Boehringer Ingelheim’s OpnMe Portal: order for free, no strings attached! (Update July 2021: in vivo DMPK data are now available online)
- Our VHL ligand “VH101, phenol” functionalized for PROTAC conjugation is available from Tocris (January 2020)
- Find out more about ACBI1 in the Chemical Probes Portal
78. Kung, W.-W., Ramachandran, S., Makukhin, N., Bruno, E., Ciulli, A.*
Structural insights into substrate recognition by the SOCS2 E3 ubiquitin ligase
- Pre-print posted at bioRxiv 470187; 14 November 2018 doi: https://doi.org/10.1101/470187
- See Figures here
- Featured in SLS News
- Read the SharedIt version here
- The coordinates and structure factors of our co-crystal structures are available in the PDB. Accession codes of SOCS2:ElonginC:ElonginB in complex with EpoR (PDB 6I4X) and GHR peptides (PDBs 6I5J and 6I5N)
77. Tovell, H., Testa, A., Maniaci, C., Zhou, H., Prescott, A.R., Macartney, T., Ciulli, A.*, Alessi, D.R.*
Rapid and reversible knockdown of endogenously tagged endosomal proteins via an optimized HaloPROTAC degrader
ACS Chem. Biol. 2019, 14 (5), 882-892
- Featured in the SLS and MRC-PPU News websites
- Ranked Top amongst the Most Read Articles in the journal (1-month timeframe, May 2019)
- See Figures here
76. Girardini, M., Maniaci, C., Hughes, S.J., Testa, A., Ciulli, A.*
Cereblon vs VHL: Hijacking E3 Ligases Against Each Other Using PROTACs
Bioorg. Med. Chem. 2019, 27 (12), 2466-2479
- Pre-print posted at ChemRxiv on 11 February 2019; doi: https://doi.org/10.26434/chemrxiv.7698185.v1
- Listed amongst the top Most Downloaded Bioorganic & Medicinal Chemistry Articles of the last 90 days (Apr 2019)
- See Figures here
- Our VHL ligand “VH101, phenol” functionalized for PROTAC conjugation is available from Tocris (January 2020)
- Our CRBN degrader PROTAC 14a is available from Tocris (October 2020)
75. Popow, J., Arnhof, H., Bader, G., Berger, H., Ciulli, A., Covini, D., Dank, C., Gmaschitz, T., Greb, P., Karolyi-Özguer, J., Koegl, M., McConnell, D.B., Pearson, M., Rieger, M., Rinnenthal, J., Roessler, V., Schrenk, A., Spina, M., Steurer, S., Trainor, N., Traxler, E., Wieshofer, C., Zoephel, A., Ettmayer, P.
Highly Selective PTK2 Proteolysis Targeting Chimeras to Probe Focal Adhesion Kinase Scaffolding Functions
J. Med. Chem. 2019, 62 (5), 2508-2520
- PTK2 PROTACs BI-0319 (VHL-based) and BI-3663 (CRBN-based) are available for free from the OpnMe Portal.
74. Roy, M.J., Winkler, S., Hughes, S.J., Whitworth, C., Galant, M., Farnaby, W., Rumpel, K., Ciulli, A.*
SPR-measured dissociation kinetics of PROTAC ternary complexes influence target degradation rate
ACS Chem. Biol. 2019, 14 (3), 361-368
- Pre-print posted at bioRxiv 451948; 25 October 2018 doi: https://doi.org/10.1101/451948
- Selected to be featured in ACS Editors’ Choice based on recommendation by ACS journals’ editors
- See Figures here
- Ranked Top amongst the Most Read Articles in the journal (1-month timeframe, Mar-Apr 2019)
- Highlighted in Derek Lowe’s blog In the Pipeline
- Featured in Cytiva’s web article/application note “Characterizing PROTAC ternary complex formation
73. Frost, J., Ciulli, A.*, Rocha, S.*
RNA-seq analysis of PHD and VHL inhibitors reveals differences and similarities to the hypoxia response. [version 1; referees: 2 approved]
Wellcome Open Res. 2019, 4:17 (https://doi.org/10.12688/wellcomeopenres.15044.1)
72. Castro, G.V, Ciulli, A.*
Spy vs. spy: selecting the best reporter for 19F NMR competition experiments
Chem. Commun. 2019, 55 (10), 1482-1485
- See Figures here
- Our fluorinated VHL “spy-molecule” ligands are now available from the Merck Sigma-Aldrich catalogue: Fluorinated VHL spy molecule 1, Fluorinated VHL Spy Molecule 2 and Fluorinated VHL Spy Molecule 4
71. Zoppi, V., Hughes, S.J., Maniaci, C., Testa, A., Gmaschitz, T., Wieshofer, C., Koegl, M., Riching, K., Daniels, D.L., Spallarossa, A., and Ciulli, A.*
Iterative design and optimization of initially inactive Proteolysis Targeting Chimeras (PROTACs) identify VZ185 as a potent, fast and selective von Hippel-Lindau (VHL)-based dual degrader probe of BRD9 and BRD7
J. Med. Chem. 2019, 62 (2), 699-726
- 
See Figures here
- 
The coordinates and structure factors of the associated co-crystal structure of human BRD9 bromodomain in complex with PROTAC 5 is available in the PDB with accession code 6HM0
- 
Listed as 1st Most Read Article in the journal (1-month timeframe, Jan 2019)
- 
Highlighted in the blog Promega Connection: “A Roadmap for PROTAC Development”
- 
Find out more about VZ185 in the Chemical Probes Portal
- 
Our dual Brd7/9 degrader VZ185 is available from Tocris (October 2019)
- The inactive epimer cis-VZ185 is also available from Tocris (April 2020)
- The PROTAC VZ185 (together with its negative control cis-VZ185) are also available from Boehringer Ingelheim’s OpnMe Portal: order for free, no strings attached!
- 
Our VHL ligand “VH101, phenol” functionalized for PROTAC conjugation is available from Tocris (January 2020)
70. Aresu, L., Ferraresso, S., Marconato, L., Cascione, L., Napoli, S., Gaudio, E., Kwee, I., Tarantelli, C., Testa, A., Maniaci, C., Ciulli, A., Hillmann, P., Bohnacker, T., Wymann, M.P., Comazzi, S., Milan, M., Riondato, F., Dalla Rovere, G., Giantin, M., Giannuzzi, D., Bertoni, F.
New Molecular And Therapeutic Insights Into Canine Diffuse Large B Cell Lymphoma Elucidates The Role Of The Dog As A Model For Human Disease
Haematologica 2019, 104 (6), e256-e259
2018
69. Lucas, X., Van Molle, I., Ciulli, A.*
Surface probing by fragment-based screening and computational methods identifies ligandable pockets on the von Hippel-Lindau (VHL) E3 ubiquitin ligase
J. Med. Chem. 2018, 61 (16), 7387-7393
- See Figures here
- The coordinates and structure factors of our co-crystal structures are available in the PDB. Accession codes of VCB (pVHL:ElonginC:ElonginB complex) in complex with MB235 (PDB 6GMN), MB756 (PDB 6GMQ), MB1200 (PDB 6GMX), and VCBH (pVHL:ElonginC:ElonginB:HIF-1alpha complex) in complex with MB756 (PDB 6GMR)
- Listed amongst the Most Read Articles in the journal (Aug 2018)
- Highlighted in the Faculty of 1000 Prime  
68. Testa, A., Lucas, X., Castro, G.V., Chan, K.-H., Wright, J.E., Runcie, A.C., Gadd, M.S., Harrison, W.T.A., Ko, E.-J., Fletcher, D., Ciulli, A.*
3-Fluoro-4-hydroxyprolines: Synthesis, conformational analysis and stereoselective recognition by the VHL E3 ubiquitin ligase for targeted protein degradation
J. Am. Chem. Soc. 2018, 140 (29), 9299-9313
- See Figures here
- The coordinates and structure factors of our co-crystal structures are available in the PDB, with accession codes: 6GFX, 6GFY and 6GFZ
- Addition/Correction published (Web): April 24, 2019. DOI: 10.1021/jacs.9b03833
67. Soares, P., Lucas, X., Ciulli, A.*
Thioamide substitution to probe the hydroxyproline recognition of VHL ligands
Bioorg. Med. Chem. 2018, 26 (11), 2992-2995
- See Figures here
- The article is a contribution to the journal’s Special Issue for the 2018 Tetrahedron Young Investigators Award for Matthew Fuchter
- The coordinates and structure factors of our co-crystal structures are available in the Protein DataBank, with accession codes: 6FMI, 6FMJ, and 6FMK
- 4th Most Downloaded Article in the journal (June 2018)
66. Amato, A., Lucas, X., Bortoluzzi, A., Wright, D., Ciulli, A.*
Targeting ligandable pockets on plant homeodomain (PHD) zinc finger domains by a fragment-based approach
ACS Chem. Biol. 2018, 13 (4), 915-921
- See Figures here
- The coordinates and structure factors of our co-crystal structures are available in the Protein DataBank, with accession codes: 6FHU, 6FKP, 6FI0, 6FAP, 6FHQ, and 6FI1
65. Runcie, A.C., Zengerle, M., Chan, K.-H., Testa, A., van Beurden, L., Baud, M.G.J., Epemolu, O., Ellis, L.C.J., Read, K.D., Coulthard, V., Brien, A. and Ciulli, A.*
Optimization of a “bump-and-hole” approach to allele-selective BET bromodomain inhibition