University of Delaware

University of Southern California

Melissa Blackman

Joseph M Fox

Peter Conti

Zibo Li

Peter S Conti

Ramajeyam Selvaraj

Maksim Royzen

Matthew Hassink

Ni Yan

A Diels-Alder adduct of a trans-cyclooctene with a tetrazine is provided, wherein the adduct bears a substituent labeled with a radionuclide. A method of producing a PET or other image of an organ in an animal or human includes forming the Diels-Alder adduct in the animal or human. Trans-cyclooctenes and tetrazines suitable for preparing the adducts are provided.

Tetrazine-trans-cyclooctene ligation for the rapid construction of radionuclide labeled probes

Coupling reactions, suitable for use in organic or aqueous media, are performed by contacting a 1,2,4,5-tetrazine with a dienophile. The dienophile may be covalently bonded to a protein, and the coupling reaction may be performed in biological media such as those containing cells or cell lysates. The reactions may be performed in the presence of primary amines, thiols, acetylenes, azides, phosphines, and products of Staudinger and/or Sharpless-Huisgen reactions Novel 3-substituted cyclopropene compounds and trans-cyclooctenes are exemplary dienophiles for these reactions.

Tetrazine-based bio-orthogonal coupling reagents and methods

Growing community of inventors

Waltham, MA, United States of America

Melissa Blackman