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Open AccessArticle

Allosteric Activation of GDP-Bound Ras Isoforms by Bisphenol Derivative Plasticisers

1
Faculty of Chemistry and Biochemistry, Ruhr University of Bochum, Universitätsstr. 150, D-44780 Bochum, Germany
2
Skin Cancer Unit of the Dermatology Department, West German Cancer Center, University Hospital Essen, University Duisburg-Essen and the German Cancer Consortium (DKTK), D-45147 Essen, Germany
3
Institute of Pharmacology and Toxicology, Witten/Herdecke University, Stockumer Str. 10, D-58453 Witten, Germany
4
Faculty of Mathematics and Natural Sciences, University of Wuppertal, Gaußstr. 20, D-42119 Wuppertal, Germany
*
Author to whom correspondence should be addressed.
Int. J. Mol. Sci. 2018, 19(4), 1133; https://doi.org/10.3390/ijms19041133
Received: 27 February 2018 / Revised: 4 April 2018 / Accepted: 5 April 2018 / Published: 10 April 2018
(This article belongs to the Special Issue Advances in the Research of Endocrine Disrupting Chemicals)
The protein family of small GTPases controls cellular processes by acting as a binary switch between an active and an inactive state. The most prominent family members are H-Ras, N-Ras, and K-Ras isoforms, which are highly related and frequently mutated in cancer. Bisphenols are widespread in modern life because of their industrial application as plasticisers. Bisphenol A (BPA) is the best-known member and has gained significant scientific as well as public attention as an endocrine disrupting chemical, a fact that eventually led to its replacement. However, compounds used to replace BPA still contain the molecular scaffold of bisphenols. BPA, BPAF, BPB, BPE, BPF, and an amine-substituted BPAF-derivate all interact with all GDP-bound Ras-Isoforms through binding to a common site on these proteins. NMR-, SOScat-, and GDI- assay-based data revealed a new bisphenol-induced, allosterically activated GDP-bound Ras conformation that define these plasticisers as Ras allosteric agonists. View Full-Text
Keywords: bisphenols; K-Ras4B; Rap-1A; NMR spectroscopy; active conformation/allosteric agonists bisphenols; K-Ras4B; Rap-1A; NMR spectroscopy; active conformation/allosteric agonists
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MDPI and ACS Style

Schöpel, M.; Shkura, O.; Seidel, J.; Kock, K.; Zhong, X.; Löffek, S.; Helfrich, I.; Bachmann, H.S.; Scherkenbeck, J.; Herrmann, C.; Stoll, R. Allosteric Activation of GDP-Bound Ras Isoforms by Bisphenol Derivative Plasticisers. Int. J. Mol. Sci. 2018, 19, 1133. https://doi.org/10.3390/ijms19041133

AMA Style

Schöpel M, Shkura O, Seidel J, Kock K, Zhong X, Löffek S, Helfrich I, Bachmann HS, Scherkenbeck J, Herrmann C, Stoll R. Allosteric Activation of GDP-Bound Ras Isoforms by Bisphenol Derivative Plasticisers. International Journal of Molecular Sciences. 2018; 19(4):1133. https://doi.org/10.3390/ijms19041133

Chicago/Turabian Style

Schöpel, Miriam; Shkura, Oleksandr; Seidel, Jana; Kock, Klaus; Zhong, Xueyin; Löffek, Stefanie; Helfrich, Iris; Bachmann, Hagen S.; Scherkenbeck, Jürgen; Herrmann, Christian; Stoll, Raphael. 2018. "Allosteric Activation of GDP-Bound Ras Isoforms by Bisphenol Derivative Plasticisers" Int. J. Mol. Sci. 19, no. 4: 1133. https://doi.org/10.3390/ijms19041133

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