5E5E

X-ray structure of the adduct formed in the reaction between RNase A and a neutral organometallic derivative [Pt(pbi)(Me)(DMSO)], pbi=2-(2'-pyridil)benzimidazole (compound 3)

5E5E の概要

• エントリーDOI: 10.2210/pdb5e5e/pdb
• 分子名称: Ribonuclease pancreatic, PLATINUM (II) ION, DIMETHYL SULFOXIDE, ... (4 entities in total)
• 機能のキーワード: hydrolase
• 由来する生物種: Bos taurus (Bovine)
• 細胞内の位置: Secreted: P61823
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 27884.94

構造登録者

Merlino, A. (登録日: 2015-10-08, 公開日: 2015-12-09, 最終更新日: 2024-11-20)

主引用文献

Serratrice, M.,Maiore, L.,Zucca, A.,Stoccoro, S.,Landini, I.,Mini, E.,Massai, L.,Ferraro, G.,Merlino, A.,Messori, L.,Cinellu, M.A.
Cytotoxic properties of a new organometallic platinum(ii) complex and its gold(i) heterobimetallic derivatives.
Dalton Trans, 45:579-590, 2015

PubMed Abstract: A novel platinum(ii) organometallic complex, [Pt(pbi)(Me)(DMSO)], bearing the 2-(2'-pyridyl)-benzimidazole (pbiH) ligand, was synthesized and fully characterized. Interestingly, the reaction of this organometallic platinum(ii) complex with two distinct gold(i) phosphane compounds afforded the corresponding heterobimetallic derivatives with the pbi ligand bridging the two metal centers. The antiproliferative properties in vitro of [Pt(pbi)(Me)(DMSO)] and its gold(i) derivatives as well as those of the known coordination platinum(ii) and palladium(ii) complexes with the same ligand, of the general formula [MCl2(pbiH)], were comparatively evaluated against A2780 cancer cells, either sensitive or resistant to cisplatin. A superior biological activity of the organometallic compound clearly emerged compared to the corresponding platinum(ii) complex; the antiproliferative effects are further enhanced upon attaching the gold(i) triphenylphosphine moiety to the organometallic Pt compound. Remarkably, these novel metal species are able to overcome nearly complete resistance to cisplatin. Significant mechanistic insight into the study compounds was gained after investigating their reactions with a few representative biomolecules by electrospray mass spectrometry and X-ray crystallography. The obtained results are comprehensively discussed.

PubMed: 26609781
DOI: 10.1039/c5dt02714d

実験手法

X-RAY DIFFRACTION (1.98 Å)