Recent advances in structural biology, protein epitope mapping and computational analysis have identified interaction hotspots and increased confidence in the druggability of the complex targets that rely on these key surface contacts.

Encycle Therapeutics interrogates the extended binding sites common to large protein-protein interfaces. Our platform generates macrocycles that populate a multitude of closely related, low-energy conformers representing different regions of surface-exposed loops and grooves that accurately recreate inter-surface binding elements.

To address the long-standing challenge of cyclic peptide synthesis, we recently developed a powerful strategy for constraining linear peptides into their macrocyclic forms. The strategy further enables cyclization of diverse linear precursors comprising small molecule (non-peptidic) components. Our proprietary methods deliver atom- and step-economical syntheses of proprietary 3D macrocycles called nacellins.
  A proprietary chemistry platform from the laboratory of Dr. Andrei Yudin at the University of Toronto allows efficient synthesis of uniquely substituted ring systems comprising six to twenty or more contiguous atoms.

Our core Discovery capability focuses on the design of molecules that address emerging principles in the chemical space required to mediate protein-protein interactions.

The company's collaborative programs reflect the evolving understanding in this space and in the identification of key drug targets.
  Encycle Corporate Overview
April 2013

Role of Reversible Dimerization in Reactions of Amphoteric Aziridine Aldehydes
J. Org. Chem. 2012, 77(13), 5613-5623

Conformational Modulation of in Vitro Activity of Cyclic RGD Peptides via Aziridine Aldehyde-Driven Macrocyclization Chemistry
Bioconj. Chem. 2012 23(7), 1387-1395

Thioester-isocyanides: versatile reagents for the synthesis of cycle-tail peptides
Chem. Comm. 2012, 48, 3775-3777

Contemporary Strategies for Peptide Macrocyclization
Nat. Chem. 2011, 3(7), 509-524

Synthesis of Cyclic Peptides Using Amphoteric Amino Aldehydes
Nat. Protoc. 2010, 5(11), 1813

Macrocyclization of Linear Peptides Enabled by Amphoteric Molecules
J. Am. Chem. Soc. 2010, 132(9), 2889-2891

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