8UYN

Fundamental Characterization of Chelated and Crystallized Actinium in a Macromolecular Host

8UYN の概要

• エントリーDOI: 10.2210/pdb8uyn/pdb
• 分子名称: Neutrophil gelatinase-associated lipocalin, LANTHANUM (III) ION, N,N'-butane-1,4-diylbis[1-hydroxy-N-(3-{[(1-hydroxy-6-oxo-1,6-dihydropyridin-2-yl)carbonyl]amino}propyl)-6-oxo-1,6-dihydropyridine-2-carboxamide], ... (6 entities in total)
• 機能のキーワード: inhibitor, metal binding protein
• 由来する生物種: Homo sapiens (human)
• タンパク質・核酸の鎖数: 3
• 化学式量合計: 64736.60

構造登録者

Rupert, P.B.,Strong, R.K. (登録日: 2023-11-13, 公開日: 2024-09-25, 最終更新日: 2024-11-20)

主引用文献

Wacker, J.N.,Woods, J.J.,Rupert, P.B.,Peterson, A.,Allaire, M.,Lukens, W.W.,Gaiser, A.N.,Minasian, S.G.,Strong, R.K.,Abergel, R.J.
Actinium chelation and crystallization in a macromolecular scaffold.
Nat Commun, 15:5741-5741, 2024

PubMed Abstract: Targeted alpha therapy (TAT) pairs the specificity of antigen targeting with the lethality of alpha particles to eradicate cancerous cells. Actinium-225 [Ac; t = 9.920(3) days] is an alpha-emitting radioisotope driving the next generation of TAT radiopharmaceuticals. Despite promising clinical results, a fundamental understanding of Ac coordination chemistry lags behind the rest of the Periodic Table due to its limited availability, lack of stable isotopes, and inadequate systems poised to probe the chemical behavior of this radionuclide. In this work, we demonstrate a platform that combines an 8-coordinate synthetic ligand and a mammalian protein to characterize the solution and solid-state behavior of the longest-lived Ac isotope, Ac [t = 21.772(3) years]. We expect these results to direct renewed efforts for Ac-TAT development, aid in understanding Ac coordination behavior relative to other +3 lanthanides and actinides, and more broadly inform this element's position on the Periodic Table.

PubMed: 39009580
DOI: 10.1038/s41467-024-50017-5

実験手法

X-RAY DIFFRACTION (2 Å)