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Here, we present the synthesis and characterization of a new potentially nonadentate chelator H 4 pypa and its bifunctional analogue t Bu 4 pypa-C7-NHS conjugated to prostate-specific membrane antigen (PSMA)-targeting peptidomimetic (Glu-urea-Lys). H 4 pypa is very functionally versatile and biologically stable. Compared to the conventional chelators (e.g., DOTA, DTPA), H 4 pypa has outstanding affinities for both 111 In (EC, t 1/2 ≈ 2.8 days) and 177 Lu (β - ,γ, t 1/2 ≈ 6.64 days). Its radiolabeled complexes were achieved at &gt;98% radiochemical yield, RT within 10 min, at a ligand concentration as low as 10 -6 M, with excellent stability in human serum over at least 5-7 days (&lt;1% transchelation). The thermodynamic stabilities of the [M(pypa)] - complexes (M 3+ = In 3+ , Lu 3+ , La 3+ ) were dependent on the ionic radii, where the smaller In 3+ has the highest pM value (30.5), followed by Lu 3+ (22.6) and La 3+ (19.9). All pM values are remarkably higher than those with DOTA, DTPA, H 4 octapa, H 4 octox, and H 4 neunpa. Moreover, the facile and versatile bifunctionalization enabled by the p-OH group in the central pyridyl bridge of the pypa scaffold (compound 14) allows incorporation of a variety of linkers for bioconjugation through easy nucleophilic substitution. In this work, an alkyl linker was selected to couple H 4 pypa to a PSMA-targeting pharmacophore, proving that the bioconjugation sacrifices neither the tumor-targeting nor the chelation properties. The biodistribution profiles of 111 In- and 177 Lu-labeled tracers are different, but promising, with the 177 Lu analogue particularly outstanding.

bioconjugate chemistry

Functionally Versatile and Highly Stable Chelator for <sup>111</sup>In and <sup>177</sup>Lu: Proof-of-Principle Prostate-Specific Membrane Antigen Targeting

Functionally Versatile and Highly Stable Chelator for 111In and 177Lu: Proof-of-Principle Prostate-Specific Membrane Antigen Targeting

Functionally Versatile and Highly Stable Chelator for ¹¹¹In and ¹⁷⁷Lu: Proof-of-Principle Prostate-Specific Membrane Antigen Targeting