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Thioredoxin reductase and cancer cell growth inhibition by organogold(III) compounds
Uppsala universitet, Teknisk-naturvetenskapliga vetenskapsområdet, Kemiska sektionen, Kemiska institutionen, Avdelningen för organisk kemi.
Uppsala universitet, Teknisk-naturvetenskapliga vetenskapsområdet, Kemiska sektionen, Kemiska institutionen, Avdelningen för organisk kemi.
Uppsala universitet, Teknisk-naturvetenskapliga vetenskapsområdet, Kemiska sektionen, Kemiska institutionen, Avdelningen för organisk kemi.
Uppsala universitet, Teknisk-naturvetenskapliga vetenskapsområdet, Kemiska sektionen, Kemiska institutionen, Avdelningen för organisk kemi.
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2006 (engelsk)Inngår i: Anti-Cancer Drugs, ISSN 0959-4973, E-ISSN 1473-5741, Vol. 17, nr 5, s. 539-544Artikkel i tidsskrift (Fagfellevurdert) Published
Abstract [en]

Thioredoxin (Trx) expression is increased in several human primary cancers associated with aggressive tumor growth and decreased patient survival, and the Trx/Trx reductase (TrxR) system therefore provides an attractive target for cancer drug development. Various gold(III) compounds with none, one, two or three carbon-gold bonds were evaluated for their capacity to inhibit TrxR and the growth of MCF-7 cancer cells in vitro. Compounds with up to two carbon-gold bonds were often potent inhibitors of TrxR with IC50 values as low as 2 nmol/l. In the presence of Trx and insulin the inhibiting capacity was much lower. However, the inhibitory concentrations of the compounds did not correlate with the ability to kill cells. Out of the organometallics tested, only compound 8 with two carbon-gold bonds was able to inhibit colony formation by MCF-7 breast cancer cells at low micromolar concentrations (IC50=1,6umol/l). Unfortunately, the compound did not show any anti-tumor activity against MCF-7 breast cancer and HT-29 colon cancer zenografts in scid mice.

sted, utgiver, år, opplag, sider
2006. Vol. 17, nr 5, s. 539-544
Emneord [en]
anti-tumor activity, organogold compounds, thioredoxin, thioredoxin reductase
HSV kategori
Identifikatorer
URN: urn:nbn:se:uu:diva-80771ISI: 000244316500007OAI: oai:DiVA.org:uu-80771DiVA, id: diva2:108685
Tilgjengelig fra: 2006-05-24 Laget: 2006-05-24 Sist oppdatert: 2017-12-14bibliografisk kontrollert

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