Understanding substrate binding and the role of gatekeeping residues in PigC access tunnels

Stefanie Brands; Jarno G. Sikkens; Mehdi D. Davari; Hannah U. C. Brass; Andreas S. Klein; Jörg Pietruszka; Anna Joëlle Ruff; Ulrich Schwaneberg

doi:10.1039/D0CC08226K

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Understanding substrate binding and the role of gatekeeping residues in PigC access tunnels†

Stefanie Brands,

^a Jarno G. Sikkens,^a Mehdi D. Davari,

^a Hannah U. C. Brass,

^b Andreas S. Klein,

^b Jörg Pietruszka,

^bc Anna Joëlle Ruff

^a and Ulrich Schwaneberg

*^ad

Author affiliations

* Corresponding authors

^a Lehrstuhl für Biotechnologie, RWTH Aachen University, Bioeconomy Science Center (BioSC), Worringerweg 3, Aachen 52074, Germany
E-mail: u.schwaneberg@biotec.rwth-aachen.de

^b Institute of Bioorganic Chemistry, Heinrich Heine University Düsseldorf located at Forschungszentrum Jülich, Stetternicher Forst, Bioeconomy Science Center (BioSC), Building 15.8, Jülich 52426, Germany

^c Institute of Bio- and Geosciences (IBG-1: Biotechnology), Forschungszentrum Jülich, Jülich 52426, Germany

^d DWI-Leibniz Institut für Interaktive Materialien, Forckenbeckstraße 50, Aachen 52074, Germany

Abstract

Semi-rational redesign of the substrate binding pocket and access tunnels of prodigiosin ligase PigC enhanced the catalytic efficiency in the synthesis of pyrrolic anti-cancer agents more than 45 times. A molecular understanding was gained on residues V333 and T334 relevant to substrate binding and translocation of small pyrroles through PigC access tunnels.

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Article information

DOI: https://doi.org/10.1039/D0CC08226K
Article type: Communication
Submitted: 18 Dec 2020
Accepted: 02 Feb 2021
First published: 02 Feb 2021

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Chem. Commun., 2021,57, 2681-2684

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Understanding substrate binding and the role of gatekeeping residues in PigC access tunnels

S. Brands, J. G. Sikkens, M. D. Davari, H. U. C. Brass, A. S. Klein, J. Pietruszka, A. J. Ruff and U. Schwaneberg, Chem. Commun., 2021, 57, 2681 DOI: 10.1039/D0CC08226K

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Chemical Communications

Understanding substrate binding and the role of gatekeeping residues in PigC access tunnels†

Abstract

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Understanding substrate binding and the role of gatekeeping residues in PigC access tunnels

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