title: A flexible method for preparation of peptide homo- and heterodimers functionalized with affinity probes, chelating ligands, and latent conjugating groups.
abstract: Dimerization of peptides can provide high binding entities to serve as targeted diagnostics or therapeutics. We developed methods for the preparation of homo- and heterodimer peptides bearing functional molecules (affinity probes, chelating ligands, or latent conjugating moieties). Monomer peptides, optionally bearing spacer groups, are tethered using a bifunctional linker, (di-succinimidyl glutarate, DSG) to provide the dimers. Protected or unprotected peptides can be employed for dimer assembly. Multiple lysine N(epsilon)-amino groups are controlled using the (4,4-dimethyl-2,6-dioxocyclohex-1-ylidene)-3-methylbutyl (ivDde) protecting group. Functional molecules are optionally incorporated into the component peptides or into the assembled dimer. The methods are efficient and scaleable.
authors.affiliation: The Ernst Felder Laboratories, Bracco Research USA, Inc., 305 College Road East, Princeton, NJ 08540-6608, USA. rpillai@bru.bracco.com
authors.forename: Radhakrishna
authors.initials: R
authors.lastname: Pillai
authors.forename: Edmund R
authors.initials: ER
authors.lastname: Marinelli
authors.forename: Rolf E
authors.initials: RE
authors.lastname: Swenson
mesh_terms: D000595:Amino Acid Sequence; D002614:Chelating Agents / Q000737:chemistry; D002616:Chemical Engineering / Q000379:methods*; D019281:Dimerization; D008024:Ligands; D015335:Molecular Probes / Q000737:chemistry; D008969:Molecular Sequence Data; D010455:Peptides / Q000138:chemical synthesis* / Q000737:chemistry
chemical_list: D002614:Chelating Agents; D008024:Ligands; D015335:Molecular Probes; D010455:Peptides