Publication

Histidine Targeting Heterobimetallic Ruthenium(II)-Gold(I) Complexes

Paul Joseph Dyson, Daniel Ortiz Trujillo, Lucinda Kate Batchelor
2019
Journal Articles

Abstract

Inspired by the preferential, allosteric binding of RAPTA-T and auranofin to the nucleosome core particle, we describe the design and synthesis of a series of heterobimetallic ruthenium(II)-gold(I) complexes with varying spacer lengths ranging from four to eight polyethylene glycol units. Evaluation of their cytotoxicity reveals IC50 values in the low micromolar range against cisplatin sensitive and resistant human ovarian carcinoma (A2780, A2780cisR) and nontumoral human embryonic kidney (HEK293) cell lines. Binding studies monitored via mass spectrometry revealed an affinity for histidine residues on a fragment of the amyloid beta-protein (residues 1-16, employed as a model system), which is in accordance with the binding sites of parent drugs, RAPTA-C and auranofin, to the nucleosome core particle.

Official source

https://infoscience.epfl.ch/entities/publication/7af66523-99ab-459a-99a1-26ae4f3834f0

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Paul Joseph Dyson, Daniel Ortiz Trujillo, Lucinda Kate Batchelor
2019
Journal Articles

Abstract

Official source

https://infoscience.epfl.ch/entities/publication/7af66523-99ab-459a-99a1-26ae4f3834f0

About this result

Related concepts (21)

Nucleosome

A nucleosome is the basic structural unit of DNA packaging in eukaryotes. The structure of a nucleosome consists of a segment of DNA wound around eight histone proteins and resembles thread wrapped around a spool. The nucleosome is the fundamental subunit of chromatin. Each nucleosome is composed of a little less than two turns of DNA wrapped around a set of eight proteins called histones, which are known as a histone octamer. Each histone octamer is composed of two copies each of the histone proteins H2A, H2B, H3, and H4.

Stem-cell line

A stem cell line is a group of stem cells that is cultured in vitro and can be propagated indefinitely. Stem cell lines are derived from either animal or human tissues and come from one of three sources: embryonic stem cells, adult stem cells, or induced stem cells. They are commonly used in research and regenerative medicine. Stem cell By definition, stem cells possess two properties: (1) they can self-renew, which means that they can divide indefinitely while remaining in an undifferentiated state; and (2) they are pluripotent or multipotent, which means that they can differentiate to form specialized cell types.

Ovarian cancer

Ovarian cancer is a cancerous tumor of an ovary. It may originate from the ovary itself or more commonly from communicating nearby structures such as fallopian tubes or the inner lining of the abdomen. The ovary is made up of three different cell types including epithelial cells, germ cells, and stromal cells. When these cells become abnormal, they have the ability to divide and form tumors. These cells can also invade or spread to other parts of the body. When this process begins, there may be no or only vague symptoms.

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