A flexible method for preparation of peptide homo- and heterodimers functionalized with affinity probes, chelating ligands, and latent conjugating groups.
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.
Pillai
Radhakrishna
R
The Ernst Felder Laboratories, Bracco Research USA, Inc., 305 College Road East, Princeton, NJ 08540-6608, USA. rpillai@bru.bracco.com
Marinelli
Edmund R
ER
Swenson
Rolf E
RE
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
D002614:Chelating Agents; D008024:Ligands; D015335:Molecular Probes; D010455:Peptides