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Journal Article

The effect of the chemical nature of the side chains of amatoxins in the inhibition of eukaryotic RNA polymerase B

MPS-Authors
/persons/resource/persons197838

Wieland,  Theodor
Max Planck Institute for Medical Research, Max Planck Society;

/persons/resource/persons211607

Götzendörfer,  Christa
Max Planck Institute for Medical Research, Max Planck Society;

/persons/resource/persons232832

Vaisius,  Alain C.
Max Planck Institute for Medical Research, Max Planck Society;

/persons/resource/persons230237

Zanotti,  Giancarlo
Max Planck Institute for Medical Research, Max Planck Society;

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https://febs.onlinelibrary.wiley.com/doi/epdf/10.1111/j.1432-1033.1981.tb06315.x
(Any fulltext)

https://doi.org/10.1111/j.1432-1033.1981.tb06315.x
(Any fulltext)

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Citation

Wieland, T., Götzendörfer, C., Vaisius, A. C., & Zanotti, G. (1981). The effect of the chemical nature of the side chains of amatoxins in the inhibition of eukaryotic RNA polymerase B. European Journal of Biochemistry, 117(1), 161-164. doi:10.1111/j.1432-1033.1981.tb06315.x.


Cite as: https://hdl.handle.net/21.11116/0000-0004-C783-7
Abstract
The inhibition constants (Ki) of DNA-dependent RNA polymerase B (or II) from calf thymus were measured for eight synthetically obtained bicyclic amanitin-like thioethers, two R-sulfoxides, and two S-sulfoxides. These Ki values were compared with those of alpha-amanitin, its 6'-O-methylether Ia (an R-sulfoxide), the S-sulfoxide, the sulfone, the S-deoxo derivative (Id) of Ia, and several previously described amatoxins. The necessity of a beta-methyl side chain in position 3 and a hydroxy group in proline-2 was confirmed. Additionally, the presence of an isoleucine side chain in position 6 and the absence of a side chain in position 5 was recognized as important for binding to the enzyme. In the three sulfoxide samples examined, the R-diastereomer was found to be a stronger inhibitor than the S-form. The contribution of every structural element to biological activity has been discussed.