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Heterologous Expres...
Heterologous Expression, Biosynthetic Studies, and Ecological Function of the Selective Gq-Signaling Inhibitor FR900359
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- Crüsemann, Max (author)
- Univ Bonn, Inst Pharmazeut Biol, Bonn, Germany
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Reher, Raphael (author)
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- Schamari, Isabella (author)
- Univ Bonn, Inst Pharmazeut Biol, Bonn, Germany
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- Brachmann, Alexander O (author)
- ] Eidgenoss Tech Hsch ETH Zurich, Inst Mikrobiol, Zurich, Switzerland
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- Ohbayashi, Tsubasa (author)
- Univ Paris Sud, CEA, Gif Sur Yvette, France
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Kuschak, Markus (author)
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Malfacini, Davide (author)
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Seidinger, Alexander (author)
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Pinto-Carbó, Marta (author)
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Richarz, René (author)
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Reuter, Tatjana (author)
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Kehraus, Stefan (author)
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Hallab, Asis (author)
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- Attwood, Misty M. (author)
- Uppsala universitet,Funktionell farmakologi
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- Schiöth, Helgi B. (author)
- Uppsala universitet,Funktionell farmakologi
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Mergaert, Peter (author)
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- Kikuchi, Yoshitomo (author)
- Bioprod Res Inst AIST Hokkaido, Sapporo, Japan
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Schäberle, Till F (author)
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Kostenis, Evi (author)
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Wenzel, Daniela (author)
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Müller, Christa E (author)
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Piel, Jörn (author)
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- Carlier, Aurélien (author)
- Univ Ghent, Dept Biochem & Microbiol, Ghent, Belgium
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Eberl, Leo (author)
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König, Gabriele M (author)
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(creator_code:org_t)
- John Wiley & Sons, 2018
- 2018
- English.
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In: Angewandte Chemie International Edition. - : John Wiley & Sons. - 1433-7851 .- 1521-3773. ; 57:3, s. 836-840
- Related links:
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https://urn.kb.se/re...
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https://doi.org/10.1...
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Abstract
Subject headings
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- The cyclic depsipeptide FR900359 (FR), isolated from the tropical plant Ardisia crenata, is a strong and selective inhibitor of Gq proteins, making it an indispensable pharmacological tool to study Gq-related processes, as well as a promising drug candidate. Gq inhibition is a novel mode of action for defense chemicals and crucial for the ecological function of FR, as shown by in vivo experiments in mice, its affinity to insect Gq proteins, and insect toxicity studies. The uncultured endosymbiont of A. crenata was sequenced, revealing the FR nonribosomal peptide synthetase (frs) gene cluster. We here provide a detailed model of FR biosynthesis, supported by in vitro enzymatic and bioinformatic studies, and the novel analogue AC-1, which demonstrates the flexibility of the FR starter condensation domains. Finally, expression of the frs genes in E. coli led to heterologous FR production in a cultivable, bacterial host for the first time.
Subject headings
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Neurovetenskaper (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Neurosciences (hsv//eng)
Keyword
- FR900359
- G proteins
- biosynthesis
- heterologous expression
- natural products
Publication and Content Type
- ref (subject category)
- art (subject category)
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- By the author/editor
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Crüsemann, Max
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Reher, Raphael
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Schamari, Isabel ...
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Brachmann, Alexa ...
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Ohbayashi, Tsuba ...
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Kuschak, Markus
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show more...
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Malfacini, David ...
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Seidinger, Alexa ...
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Pinto-Carbó, Mar ...
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Richarz, René
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Reuter, Tatjana
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Kehraus, Stefan
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Hallab, Asis
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Attwood, Misty M ...
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Schiöth, Helgi B ...
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Mergaert, Peter
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Kikuchi, Yoshito ...
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Schäberle, Till ...
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Kostenis, Evi
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Wenzel, Daniela
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Müller, Christa ...
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Piel, Jörn
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Carlier, Aurélie ...
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Eberl, Leo
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König, Gabriele ...
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- About the subject
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- MEDICAL AND HEALTH SCIENCES
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MEDICAL AND HEAL ...
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and Basic Medicine
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and Neurosciences
- Articles in the publication
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Angewandte Chemi ...
- By the university
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Uppsala University