The exploration of macrocycles for drug discovery — an underexploited structural class

By E. Driggers, S. Hale, Jinbo Lee, N. Terrett. Nature reviews. Drug discovery, 2008

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Contemporary strategies for peptide macrocyclization. (2011, background): “Synthetic macrocycles are projected to experience exponential growt”
Getting Across the Cell Membrane: An Overview for Small Molecules, Peptides, and Proteins (2015, background): “1 Addressing Conformation and Polarity—Macrocyclic drugs—those with a ring architecture of 12 or more atoms, including cyclic peptides—tend to be larger and more polar than most small-molecule drugs, falling outside the Rule of 5 [120, 121].”
A Comprehensive Review on Current Advances in Peptide Drug Development and Design (2019, background): “In recent years, peptides with balanced conformational flexibility and binding affinity that are up to five times larger than small molecule drugs have attracted enormous attention [10,11].”
Torsional Diffusion for Molecular Conformer Generation (2022, background): “In particular, torsional diffusion does not address the longstanding difﬁculty that existing cheminformatics methods have with macrocycles—rings with 12 or more atoms that have found several applications in drug discovery [Driggers et al., 2008].”
Phage-encoded combinatorial chemical libraries based on bicyclic peptides. (2009, background): “In a first embodiment, these conjugates are reminiscent of the peptide macrocyclic drug”