Staff Publications

Staff Publications

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    'Staff publications' is the digital repository of Wageningen University & Research

    'Staff publications' contains references to publications authored by Wageningen University staff from 1976 onward.

    Publications authored by the staff of the Research Institutes are available from 1995 onwards.

    Full text documents are added when available. The database is updated daily and currently holds about 240,000 items, of which 72,000 in open access.

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Record number 504235
Title Synthesis and evaluation of locostatin-based chemical probes towards PEBP-proteins
Author(s) Hoogenboom, Jorin; Fiers, Martijn; Immink, Richard; Zuilhof, Han; Wennekes, Tom
Source Tetrahedron Letters 57 (2016)22. - ISSN 0040-4039 - p. 2406 - 2409.
DOI http://dx.doi.org/10.1016/j.tetlet.2016.04.071
Department(s) Laboratory for Organic Chemistry
PRI BIOS Plant Development Systems
VLAG
Publication type Refereed Article in a scientific journal
Publication year 2016
Keyword(s) Chemical probes - Flowering Locus T - Inhibitor - Locostatin - PEBP - RKIP
Abstract

Phosphatidyl ethanolamine-binding proteins (PEBPs) are implicated in various critical physiological processes in all eukaryotes. Among them is Flowering Locus T (FT), the protein recently discovered as the vital flowering hormone in plants. Small molecule inhibitors and activators of FT could provide control over plant flowering and are therefore an interesting target for industrial agriculture. No small molecule inhibitors or activators are known for FT, but for a structurally similar PEBP, RKIP, an inhibitor called locostatin has been reported to covalently bind in the RKIP ligand binding pocket. Herein, we report the synthesis of novel locostatin-based chemical PEBP probes and evaluate their ability and selectivity towards the binding of FT and RKIP.

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