Europium-labeled melanin-concentrating hormone analogues: ligands for measuring binding to melanin-concentrating hormone receptors 1 and 2.
AuthorsGao X, Hsu CK, Heinz LJ, Morin J, Shi Y, Shukla NK, Smiley DL, Xu J, Zhong B, Slieker LJ
JournalAnal Biochem
PubMed ID15113696
'We investigated the use of Eu3+ chelate-labeled analogues of melanin-concentrating hormone (MCH) as ligands for both human MCH receptors (MCHR1 and MCHR2). The analogues employed were Ala17 MCH, S36057 (Y-ADO-RC*MLGRVFRPC*W, where ADO=8-amino-3,6-dioxyoctanoyl and *=disulfide bond), and R2P (RC*MLGRVFRPC*Y-NH2). The peptides were readily labeled on the alpha-amino residue with the Eu3+ ... More
A convenient synthesis of bifunctional chelating agents based on diethylenetriaminepentaacetic acid and their coordination chemistry with yttrium(III).
AuthorsCummins CH, Rutter EW, Fordyce WA
JournalBioconjug Chem
PubMed ID1932217
'The bifunctional chelating agents N,N,N'',N'''',N''''-pentakis(carboxymethyl)-1- [(4-aminophenyl)methyl]-diethylenetriamine and N,N,N'',N'''',N''''-pentakis(carboxymethyl)-1-[(4-aminophenyl)methyl]-4- methyldiethylenetriamine were prepared in six-step syntheses in overall yields of 38% and 31%, respectively. The use of bromoacetate esters in the synthesis allowed large-scale flash chromatographic purification of reaction products. The synthesis of N,N,N'',N'''',N''''-pentakis(carboxymethyl)-1- [(4-aminophenyl)-methyl]-4-methyldiethylenetriamine resulted in a mixture of two diastereomers. ... More
Bifunctional chelators for therapeutic lanthanide radiopharmaceuticals.
AuthorsLiu S, Edwards DS
JournalBioconjug Chem
PubMed ID11170362
Efficient multigram synthesis of the bifunctional chelating agent (S)-1-p-isothiocyanatobenzyl-diethylenetriaminepentaacetic acid [correction of diethylenetetraminepentaacetic acid]
AuthorsCorson DT, Meares CF
JournalBioconjug Chem
PubMed ID10725108
We have developed and optimized the synthesis of the title compound, eliminating all HPLC purifications prior to the final product. The yield (and scale) of the synthesis was increased from 19% (200 mg) to 75% (26 g). ... More
Synthesis of novel bifunctional chelators and their use in preparing monoclonal antibody conjugates for tumor targeting.
AuthorsWesterberg DA, Carney PL, Rogers PE, Kline SJ, Johnson DK
JournalJ Med Chem
PubMed ID2491892
Bifunctional derivatives of the chelating agents ethylenediaminetetraacetic acid and diethylenetriaminepentaacetic acid, in which a p-isothiocyanatobenzyl moiety is attached at the methylene carbon atom of one carboxymethyl arm, was synthesized by reductive alkylation of the relevant polyamine with (p-nitrophenyl)pyruvic acid followed by carboxymethylation, reduction of the nitro group, and reaction with ... More