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The peptide discovery team at IRBM has extensive expertise in chemo-selective conjugation of peptides to a range of different entities, providing the tools necessary to support your peptide drug discovery across a range of therapeutic areas.

Peptides can be conjugated with proteins, mAbs, lipids, small molecules, fluorescent labels (eg AlexaFluor®), Cy reagents and radiometal chelators such as DOTA/NOTA.

We design and synthesize peptide conjugates using a variety of linkages, including thioethers, oximes, triazoles, and hydrazides. One such method links a peptide to a carrier protein through the side chain thiol (-SH) of a cysteine residue. We also use click chemistry, a novel, Nobel Prize winning method, to achieve site-specific derivatization of azide/alkyne functionalities.

To promote complexation of peptide drugs to plasma proteins and improve the PK properties of drug candidates, we conjugate peptides to half-life extending moieties such as fatty acids, cholesterol or albumin binders.

We’ll also conjugate peptides or proteins with other peptides, small molecules or tags to optimize activity such as to promote an antigenic immune response, cellular uptake, receptor mediated drug delivery and theranostic applications.

PEG conjugation: two schemes showing a protein linked to a polyethylene glycol chain, one through the side chain thiol of a cysteine residue and one through a click chemistry triazole.
Fatty acid conjugation: scheme showing a peptide linked through two PEG2 spacers and a gamma-glutamate residue to a C18 fatty di-acid.
Cholesterol conjugation: scheme showing a peptide linked to cholesterol through a click chemistry triazole and a PEG spacer.

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