Key papers and reviews in the PPI field

For additional excellent recent manuscripts on the topic, please see: PPI-net paper of the month

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

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.

Pelay-Gimeno, M., A. Glas, O. Koch & T. N. Grossmann (2015) Structure-Based Design of Inhibitors of Protein–Protein Interactions: Mimicking Peptide Binding Epitopes. Angew. Chem. Int. Ed. 54, 8896-8927.

Arkin, M. R., Tang, Y. & Wells, J.A. (2014) Small-Molecule Inhibitors of Protein-Protein Interactions: Progressing toward the Reality. Chem. Biol. 21, 1102-1114.

Milroy, L.-G., Tom, N., Grossmann, S. Hennig, Brunsveld, L. & Ottmann, C. (2014) Modulators of Protein–Protein Interactions. Chem. Rev. 114, 4695-4748.

Walensky, L. D. & Bird, G.H. (2014) Hydrocarbon-Stapled Peptides: Principles, Practice, and Progress. J. Med. Chem. 57, 6275-6288.

Souers, A. J., Leverson, J.D.,  Boghaert, E.R.,  Ackler, S.L., Catron, N.D., Chen, J. et al. (2013) ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets. Nat. Med. 19, 202-208.

Ray-Coquard, I., Blay, J-Y., Italiano, A., Le Cesne, N., Penel, J., Zhi, F. et al. (2012) Effect of the MDM2 antagonist RG7112 on the P53 pathway in patients with MDM2-amplified, well-differentiated or dedifferentiated liposarcoma: an exploratory proof-of-mechanism study. Lancet Oncol. 13, 1133-1140.

Thompson, A. D., Dugan, A., Gestwicki, J.E. & Mapp, A.K. (2012) Fine-Tuning Multiprotein Complexes Using Small Molecules. ACS Chem. Biol. 7, 1311-1320.

Wilson, W. H., O’Connor, O.A., Czuczman, M.S., LaCasce, A.S., Gerecitano, J.F., Leonard, A. et al. (2010) Navitoclax, a targeted high-affinity inhibitor of BCL-2, in lymphoid malignancies: a phase 1 dose-escalation study of safety, pharmacokinetics, pharmacodynamics, and antitumour activity. Lancet Oncol. 11, 1149-1159.

Wells, J. A. & McClendon, C.L. (2007) Reaching for high-hanging fruit in drug discovery at protein-protein interfaces. Nature 450, 1001-1009.

Oltersdorf, T., Elmore, S.W., Shoemaker, A.R., Armstrong, R.C., Augeri, D.J., Belli, B.A.,  et al. (2005) An inhibitor of Bcl-2 family proteins induces regression of solid tumours. Nature 435, 677-681.

Arkin, M. R. & Wells, J.A. (2004) Small-molecule inhibitors of protein-protein interactions: progressing towards the dream. Nat. Rev. Drug. Discov. 3, 301-317.

Vassilev, L. T., Vu, B.T., Graves,B.,  Carvajal, D., Podlaski, F.,  Filipovic, Z., et. at. (2004) In Vivo Activation of the p53 Pathway by Small-Molecule Antagonists of MDM2. Science 303, 844-848.