Themed collection Macrocycles with bio-related applications

The broad use of non-peptide synthetic macrocycles in drug discovery is benefitting from recent advances in our understanding of what molecular properties define a useful macrocyclic screening hit.

Integration of Pin1-binding and cell-penetrating sequences results in a cell-permeable, biologically active cycloheptapeptide inhibitor against Pin1.

The synthesis and in vivo pharmacokinetic profile of an analogue of cyclosporine is disclosed.

Searching for regularities in the large set of structurally diverse macrocyclic probes allowed us to determine the structural requirements for the selective recognition of chloride over more basic anions such as H₂PO₄⁻ or RCO₂⁻ by a putative anion receptor.

Describes the identification of macrocyclic peptide inhibitors of the ebola VP24 protein–karyopherin alpha 5 protein–protein interaction with nanomolar affinity for VP24.

A tetra-disulfide peptide dimer, representing an antiparallel hinge, is synthesised without the need for orthogonal cysteine protecting groups.

Synthesis of biaryl-containing macrocycles has been carried out through a four-step approach comprising two Ugi four component reactions and a Suzuki–Miyaura macrocyclization.

Apelin is the endogenous ligand for the G protein-coupled receptor APJ and exerts a key role in regulating cardiovascular functions.

The combination of pseudopeptidic dithiol building blocks leads to the generation of highly diverse dynamic libraries of macrocycles in aqueous media.

Using macrocycles to meet the challenge of reducing proteins to smaller molecules that maintain affinity and inhibitory potency for Bcl-xL.

Members of a new class of cyclic “extended” peptoids (the “benzylopeptoids”) efficiently capture sodium ions with different stoichiometries depending on the ring morphology.

NMR and X-ray crystallography reveals covalent attachment of the macrocyclic aldehyde to serine195 of α-chymotrypsin and that its backbone binds as a β-strand.