DOTA-peptides

Li L, Olafsen T, Anderson A L, et al. (2002). Reduction of kidney uptake in radiometal labeled peptide linkers conjugated to recombinant antibody fragments. Site-specific conjugation of DOTA-peptides to a Cys-diabody. Bioconjug. Chem. 13 985-995. 

Solid phase synthesis of DOTA-peptides (Peterson et al. 1999)... 

There are several methods used to conjugate DOTA and other polyaminocarboxylate ligands to biomolecules.140,141 The simplest method, commonly used in solid-phase peptide synthesis, is the... 

Macke recently introduced a monoreactive DOTA prochelator (4,7,10-tricarboxymethyl-tert-butyl ester A, A, A", A "-tetraazacyclododecane-1 -acetate), which was coupled to Tyr3—Lys5 (BOQ-octreotide via solid-phase peptide synthesis. A one-step deprotection reaction generated the bioactive compound DOTATOC in about 65% yield.142 The 90Y and 177Lu DOTATOC complexes have shown promise for the treatment of neuroendocrine tumors in early clinical trials.143,444... 

Recently, researchers have built on the discovery of a class of novel 188Re cyclized peptides that exhibit high melanoma tumor uptake and good pharmacokinetics by designing analogs containing non-radioactive rhenium and an appended DOTA BFCA to act as a carrier for radiolanthanides.18... 

Li, M., and Meares, C.F. (1993) Synthesis, metal chelate stability studies, and enzyme digestion of a peptide-liked DOTA derivatives and its corresponding radiolabeled immunoconjugates. Bioconjugate Chem. 4, 275-283. 

PARACEST agents with a response to enzymatic activity have also been reported. Pagel et al. used a Tm1 DOTA monoamide complex containing a peptide chain which is hydrolyzed by the Caspase-3 enzyme (204,205). Following enzymatic cleavage, the PARACEST effect originating from the amide proton disappears due to the hydrolysis of the amide bond. 

Fig. 10. Structure of a tat-peptide labeled DOTA chelate [98] (M3+ = Dy3+, Gd3+ or inIn3+)...

De Jong M et al (1998) Internalization of radiolabelled [DTPA(0)]octreotide and [DOTA(O), Tyr(3)]octreotide Peptides for somatostatin receptor-targeted scintigraphy and radionuclide therapy. Nucl Med Com 19 283-288... 

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