Interesting Publications

  1. McCoull, W., Abrams, RD., Anderson, E., Blades, K., Barton, P. et al. (2017) Discovery of Pyrazolo[1,5-a]pyrimidine B-Cell Lymphoma 6 (BCL6) Binders and Optimization to High Affinity Macrocyclic Inhibitors. Journal of Medicinal Chemistry 60 (10), 4386-4402

  2. Niu, X., Brahmbhatt, H., Mergenthaler, P., Zhang, Z., Sang, J., et al. (2017) A Small-Molecule Inhibitor of Bax and Bak Oligomerization Prevents Genotoxic Cell Death and Promotes Neuroprotection. Cell Chemical Biology 24, 493-506.e5

  3. Berlow, R. B., Dyson, H. J. & Wright, P. E. (2017) Hypersensitive termination of the hypoxic response by a disordered protein switch. Nature 543, 447-451

  4. Kumar, S. & Hamilton, A.D. (2017) Alpha-Helix Mimetics as Modulators of Alpha-Beta Self-Assembly. J. Am. Chem. Soc. 139 (16), 5744-5755

  5. Johannes, J. W., Bates, S., et al.  (2017) Structure Based Design of Non-Natural Peptidic Macrocyclic Mcl-1 Inhibitors. ACS Med. Chem. Lett. 8, 239-244.

  6. Sarnowski, M. P., Kang, C. W., Elbatrawi, Y. M., Wojtas, L. & Del Valle, J. R. (2017) Peptide N-Amination Supports beta-Sheet Conformations. Angew. Chem. Int. Ed. 56, 2083-2086. 

  7. Spencer-Smith et al. (2017). Inhibition of RAS function through targeting an allosteric regulatory site. Nature Chemical Biology 13, 62-68 .

  8. Kotchy et al. (2016). The Mcl-1 inhibitor S63845 is tolerable and effective in diverse cancer models. Nature 538, 477-482.

  9. Akcay, G., Belmonte, M.A., Aquila, B., Chuaqui, C. et al. (2016). "Inhibition of Mcl-1 through covalent modification of a noncatalytic lysine side chain." Nat Chem Biol 12, 931-936.

  10. Sable, R., Durek, T., et al. (2016) Constrained Cyclic Peptides as Immunomodulatory Inhibitors of the CD2:CD58 Protein–Protein InteractionACS Chem. Biol. 11, 2366-2374

  11. Kim, W., G. H. Bird, et al. (2013). Targeted disruption of the EZH2–EED complex inhibits EZH2-dependent cancer. Nat Chem Biol 9(10): 643-650.

  12. Patrone, J. D., J. P. Kennedy, et al. (2013).Discovery of Protein–Protein Interaction Inhibitors of Replication Protein A. ACS Medicinal Chemistry Letters 4(7): 601-605.

  13. Lessene, G., P. E. Czabotar, et al. (2013). Structure-guided design of a selective BCL-XL inhibitor. Nat Chem Biol 9(6): 390-397.

  14. Karatas, H., E. C. Townsend, et al. (2012). High-Affinity, Small-Molecule Peptidomimetic Inhibitors of MLL1/WDR5 Protein–Protein Interaction. Journal of the American Chemical Society 135(2): 669-682.

  15. Ko, E., A. Raghuraman, et al. (2012). Exploring Key Orientations at Protein–Protein Interfaces with Small Molecule Probes. Journal of the American Chemical Society 135(1): 167-173.

  16. Guo, Y., C. L. Partch, et al. (2012). Regulating the ARNT/TACC3 Axis: Multiple Approaches to Manipulating Protein/Protein Interactions with Small Molecules. ACS Chemical Biology 8(3): 626-635.

  17. Thiel P, Kaiser M, Ottmann C. (2012) Small-molecule stabilization of protein-protein interactions: an underestimated concept in drug discovery?  Angew Chem.;51(9):2012-8. doi: 10.1002/anie.201107616.

  18. Buckley LD, Van Molle I, Gareiss PC, Tae HS, Michel J, Noblin DJ, Jorgensen WL, Ciulli A, Crews CM (2012) Targeting the von Hippel–Lindau E3 Ubiquitin Ligase Using Small Molecules To Disrupt the VHL/HIF-1? Interaction J. Am. Chem. Soc., DOI: 10.1021/ja209924v

  19. Surade S, Blundell TL, (2012)  Structural Biology and Drug Discovery of Difficult Targets: The Limits of Ligandability. Chemistry & Biology. Volume 19, Issue 1, Pages 42–50

  20. Wanner J, Fry DC, Peng Z, Roberts J. (2011) Druggability assessment of protein-protein interfaces. Future Med Chem. Dec;3(16):2021-38.

  21. Bullock BN, Jochim AL and Arora PS (2011) Assessing Helical Protein Interfaces for Inhibitor Design. J. Am. Chem. Soc. DOI: 10.1021/ja206074j

  22. Morelli X, Bourgeas R and Roche P (2011) Chemical and structural lessons from recent successes in protein-protein interaction inhibition (2P2I). Curr. Opin. Chem. Biol. 15:475-481

  23. Phillips C, Roberts LR, et al. (2011) Design and Structure of Stapled Peptides Binding to Estrogen Receptors. Journal of the American Chemical Society 133:9696-9699

  24. Patgiri A, Yadav KK, Arora PS and Bar-Sagi D (2011) An orthosteric inhibitor of the Ras-Sos interaction. Nat. Chem. Biol. 7:585-587

  25. Wells JA and McClendon CL (2007) Reaching for high-hanging fruit in drug discovery at protein-protein interfaces. Nature. 450:1001-1009

  26. Vassilev LT, Vu BT, Graves B, et al. (2004) In vivo activation of the p53 pathway by small-molecule antagonists of MDM2. Science. 303:844-848