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Literature DB >> 24258965

An organometallic inhibitor for the human repair enzyme 7,8-dihydro-8-oxoguanosine triphosphatase.

Manuel Streib¹, Katja Kräling, Kristin Richter, Xiulan Xie, Holger Steuber, Eric Meggers.

Abstract

The probe-based discovery of the first small-molecule inhibitor of the repair enzyme 8-oxo-dGTPase (MTH1) is presented, which is an unconventional cyclometalated ruthenium half-sandwich complex. The organometallic inhibitor with low-nanomolar activity displays astonishing specificity, as verified in tests with an extended panel of protein kinases and other ATP binding proteins. The binding of the organometallic inhibitor to MTH1 is investigated by protein crystallography.

Entities: CellLine Chemical Disease Gene Species

Keywords: 7,8-dihydro-8-oxoguanosine triphosphatase; enzyme inhibitors; organometallic compounds; protein crystal structures; ruthenium

Mesh：

Substances：

Year: 2013 PMID： 24258965 PMCID： PMC4108727 DOI： 10.1002/anie.201307849

Source DB: PubMed Journal: Angew Chem Int Ed Engl ISSN： 1433-7851 Impact factor: 15.336

44 in total

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8. Extremely tight binding of a ruthenium complex to glycogen synthase kinase 3.

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9. Crystal structure of human MTH1 and the 8-oxo-dGMP product complex.

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Journal: FEBS Lett Date: 2011-07-23 Impact factor: 4.124

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2. Farnesyl phenolic enantiomers as natural MTH1 inhibitors from Ganoderma sinense.

Authors: Ya Gao; Lihan Zhu; Jing Guo; Ting Yuan; Liqing Wang; Hua Li; Lixia Chen
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3. Structural and Kinetic Studies of the Human Nudix Hydrolase MTH1 Reveal the Mechanism for Its Broad Substrate Specificity.

Authors: Shaimaa Waz; Teruya Nakamura; Keisuke Hirata; Yukari Koga-Ogawa; Mami Chirifu; Takao Arimori; Taro Tamada; Shinji Ikemizu; Yusaku Nakabeppu; Yuriko Yamagata
Journal: J Biol Chem Date: 2016-12-29 Impact factor: 5.157

4. In-Cell Activation of Organo-Osmium(II) Anticancer Complexes.

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5. Anticancer osmium complex inhibitors of the HIF-1α and p300 protein-protein interaction.

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Review 6. Targeting human MutT homolog 1 (MTH1) for cancer eradication: current progress and perspectives.

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7. NUDT2 Disruption Elevates Diadenosine Tetraphosphate (Ap4A) and Down-Regulates Immune Response and Cancer Promotion Genes.

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Journal: PLoS One Date: 2016-05-04 Impact factor: 3.240