PDBsum entry 5e5e

Hydrolase

PDB id: 5e5e

Contents

Protein chains

124 a.a.

Ligands

DMS

Metals

_PT ×2

Waters ×164

PDB id:

5e5e

Name:

Hydrolase

Title:

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)

Structure:

Ribonuclease pancreatic. Chain: a, b. Synonym: rnase 1,rnase a. Ec: 3.1.27.5

Source:

Bos taurus. Bovine. Organism_taxid: 9913

Resolution:

1.98Å R-factor: 0.195 R-free: 0.254

Authors:

A.Merlino

Key ref:

M.Serratrice et al. (2016). Cytotoxic properties of a new organometallic platinum(II) complex and its gold(I) heterobimetallic derivatives. Dalton Trans, 45, 579-590. PubMed id: 26609781 DOI: 10.1039/c5dt02714d

Date:

08-Oct-15 Release date: 09-Dec-15

Protein chains

P61823  (RNAS1_BOVIN) -  Ribonuclease pancreatic from Bos taurus

Seq: 150 a.a.

Struc: 124 a.a.

Enzyme reactions

• Enzyme class: E.C.4.6.1.18 - pancreatic ribonuclease.
• Reaction:
  1. an [RNA] containing cytidine + H2O = an [RNA]-3'-cytidine- 3'-phosphate + a 5'-hydroxy-ribonucleotide-3'-[RNA]
  2. an [RNA] containing uridine + H2O = an [RNA]-3'-uridine-3'-phosphate + a 5'-hydroxy-ribonucleotide-3'-[RNA]

DOI no: 10.1039/c5dt02714d

Dalton Trans 45:579-590 (2016)

PubMed id: 26609781

Cytotoxic properties of a new organometallic platinum(II) complex and its gold(I) heterobimetallic derivatives.

M.Serratrice, L.Maiore, A.Zucca, S.Stoccoro, I.Landini, E.Mini, L.Massai, G.Ferraro, A.Merlino, L.Messori, M.A.Cinellu.

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.