Bicycle Therapeutics Announces Publication of Article in Bioconjugate Chemistry, Describing an Extension of its Proprietary Technology Platform Based on Bicyclic Peptides

Bicycle Therapeutics plc (NASDAQ: BCYC), a biotechnology company pioneering a new and differentiated class of therapeutics based on its proprietary bicyclic peptide (Bicycle®) technology, today announced that an article highlighting data using tris-Gold complexes to increase the chemical diversity of Bicycles, was published in Bioconjugate Chemistry. The article, titled “Gold-Mediated Multiple Cysteine Arylation for the Construction of Highly Constrained Bicycle Peptides” is available at the publications section of the Bicycle website at this link.

“The research published in Bioconjugate Chemistry demonstrates that Gold-mediated cysteine arylation can be used as an approach for construction of novel, highly constrained Bicycles under conditions previously shown to be compatible with reactions on biological systems such as bacteriophage, highlighting the potential to be utilized for new Bicycle targets moving forward. Assessment of the suitability of this methodology to Bicycle phage screening is underway,” said Kevin Lee, Ph.D., Chief Executive Officer of Bicycle Therapeutics. “The article adds to the wealth of scientific papers coming from our Company, and the acceleration in output is a testament to the robustness of our platform as well as the hard work and quality of the Bicycle team.”

Bicycles are formed through the reaction of three cysteine residues within a linear sequence with a trivalent, symmetrical small molecule scaffold. Bicycles with high binding affinities to therapeutically important targets are discovered using a proprietary phage display technology. Tris-Gold complexes have recently been described as a method for the efficient bioconjugation of cysteine residues under conditions we believe to be compatible with phage display. The article exemplifies an approach for the construction of novel, highly constrained Bicycles.

About Bicycle Therapeutics

Bicycle Therapeutics (NASDAQ: BCYC) is a clinical-stage biopharmaceutical company developing a novel class of medicines, referred to as Bicycles, for diseases that are underserved by existing therapeutics. Bicycles are fully synthetic short peptides constrained with small molecule scaffolds to form two loops that stabilize their structural geometry. This constraint facilitates target binding with high affinity and selectivity, making Bicycles attractive candidates for drug development. Bicycle is evaluating BT5528, a second-generation Bicycle Toxin Conjugate (BTC™) targeting EphA2; BT8009, a second-generation BTC targeting Nectin-4, a well-validated tumor antigen; and BT7480, a Bicycle TICA™ targeting Nectin-4 and agonizing CD137, in company-sponsored Phase I/II trials. In addition, BT1718, a BTC that targets MT1-MMP, is being investigated in an ongoing Phase I/IIa clinical trial sponsored by the Cancer Research UK Centre for Drug Development. Bicycle is headquartered in Cambridge, UK, with many key functions and members of its leadership team located in Lexington, Massachusetts. For more information, visit


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