scholarly journals Chemical genetics and strigolactone perception

F1000Research ◽  
2017 ◽  
Vol 6 ◽  
pp. 975 ◽  
Author(s):  
Shelley Lumba ◽  
Michael Bunsick ◽  
Peter McCourt

Strigolactones (SLs) are a collection of related small molecules that act as hormones in plant growth and development. Intriguingly, SLs also act as ecological communicators between plants and mycorrhizal fungi and between host plants and a collection of parasitic plant species. In the case of mycorrhizal fungi, SLs exude into the soil from host roots to attract fungal hyphae for a beneficial interaction. In the case of parasitic plants, however, root-exuded SLs cause dormant parasitic plant seeds to germinate, thereby allowing the resulting seedling to infect the host and withdraw nutrients. Because a laboratory-friendly model does not exist for parasitic plants, researchers are currently using information gleaned from model plants like Arabidopsis in combination with the chemical probes developed through chemical genetics to understand SL perception of parasitic plants. This work first shows that understanding SL signaling is useful in developing chemical probes that perturb SL perception. Second, it indicates that the chemical space available to probe SL signaling in both model and parasitic plants is sizeable. Because these parasitic pests represent a major concern for food insecurity in the developing world, there is great need for chemical approaches to uncover novel lead compounds that perturb parasitic plant infections.

Agronomy ◽  
2021 ◽  
Vol 11 (3) ◽  
pp. 501
Author(s):  
Carlos Rial ◽  
Rosa M. Varela ◽  
José M.G. Molinillo ◽  
Sara Peralta ◽  
Francisco A. Macías

Several strategies have been proposed to control parasitic plants and these include biological control, the use of herbicides, and suicidal germination or trap crops. In the case of sunflower, the most effective solution is genetic resistance. Nevertheless, the use of resistant cultivars is followed by the appearance of new and more virulent races of the parasite that overcome the existing sources of resistance. For this reason, it is necessary to increase our knowledge of the mechanisms involved in the resistant varieties. In this study, the presence of compounds involved in pre-attachment resistance mechanisms in sunflower varieties was analyzed. The production of stimulators of the germination of parasitic plant seeds and the concentration of the haustorial elongation inhibitor, scopoletin, were measured in exudates of resistant and susceptible sunflower varieties. It was found that dehydrocostuslactone and orobanchyl acetate are not involved in the resistance of the sunflower varieties studied. The results demonstrate that costunolide, heliolactone, and scopoletin are related to sunflower resistance. The sunflower varieties studied do not use all available options to fight parasitic plants. This could be one of the reasons that sunflower resistance is rapidly overcome by broomrape.


2019 ◽  
Vol 5 (7) ◽  
pp. eaaw4607 ◽  
Author(s):  
Constantinos G. Neochoritis ◽  
Shabnam Shaabani ◽  
Maryam Ahmadianmoghaddam ◽  
Tryfon Zarganes-Tzitzikas ◽  
Li Gao ◽  
...  

The compatibility of free boronic acid building blocks in multicomponent reactions to readily create large libraries of diverse and complex small molecules was investigated. Traditionally, boronic acid synthesis is sequential, synthetically demanding, and time-consuming, which leads to high target synthesis times and low coverage of the boronic acid chemical space. We have performed the synthesis of large libraries of boronic acid derivatives based on multiple chemistries and building blocks using acoustic dispensing technology. The synthesis was performed on a nanomole scale with high synthesis success rates. The discovery of a protease inhibitor underscores the usefulness of the approach. Our acoustic dispensing–enabled chemistry paves the way to highly accelerated synthesis and miniaturized reaction scouting, allowing access to unprecedented boronic acid libraries.


2010 ◽  
Vol 21 (1) ◽  
pp. 55-61 ◽  
Author(s):  
Mónica Fernández-Aparicio ◽  
Koichi Yoneyama ◽  
Diego Rubiales

AbstractStrigolactones are apocarotenoids regulating shoot branching. They are also known to be exuded by plant roots at very low concentrations, stimulating hyphal branching of arbuscular mycorrhizal fungi and germination of root parasitic weed seeds. We show that strigolactones play a major role in host specificity ofOrobancheandPhelipanche(the broomrapes) seed germination. This observation confirms that host-derived germination stimulants are an important component determining the host specificity of these parasitic plants. Weedy broomrape species were less specialized in germination requirements than the non-weedy species except forO. cumanaandO. foetidavar.broteri. Similar results were obtained with the root exudates. Some species, such asP. aegyptiacaandO. minor, showed a broad spectrum of host specificity in terms of seed germination, which was stimulated by exudates from the majority of species tested, whereas others, such asO. cumana,O. hederaeandO. densiflora, were highly specific. Some species, such asO. minor,P. aegyptiacaandP. nana, were responsive to the three strigolactones studied, whereas others were induced by only one of them, or did not respond to them at all. The synthetic strigolactone analogue GR24, generally used as a standard for germination tests, was not effective on someOrobancheandPhelipanchespecies. Seeds of some species that did not respond to GR24 were induced to germinate in the presence of fabacyl acetate or strigol, confirming the role of strigolactones in host specificity.


2011 ◽  
Vol 98 (4) ◽  
pp. 597-601 ◽  
Author(s):  
Clara de Vega ◽  
Montserrat Arista ◽  
Pedro L. Ortiz ◽  
Salvador Talavera

Mycorrhiza ◽  
2009 ◽  
Vol 19 (7) ◽  
pp. 449-459 ◽  
Author(s):  
J. M. García-Garrido ◽  
V. Lendzemo ◽  
V. Castellanos-Morales ◽  
S. Steinkellner ◽  
Horst Vierheilig

2017 ◽  
Author(s):  
Carrow I. Wells ◽  
Nirav R. Kapadia ◽  
Rafael M. Couñago ◽  
David H. Drewry

AbstractPotent, selective, and cell active small molecule kinase inhibitors are useful tools to help unravel the complexities of kinase signaling. As the biological functions of individual kinases become better understood, they can become targets of drug discovery efforts. The small molecules used to shed light on function can also then serve as chemical starting points in these drug discovery efforts. The Nek family of kinases has received very little attention, as judged by number of citations in PubMed, yet they appear to play many key roles and have been implicated in disease. Here we present our work to identify high quality chemical starting points that have emerged due to the increased incidence of broad kinome screening. We anticipate that this analysis will allow the community to progress towards the generation of chemical probes and eventually drugs that target members of the Nek family.


Molecules ◽  
2020 ◽  
Vol 25 (23) ◽  
pp. 5702
Author(s):  
Quentin T. L. Pasquer ◽  
Ioannis A. Tsakoumagkos ◽  
Sascha Hoogendoorn

Biologically active small molecules have a central role in drug development, and as chemical probes and tool compounds to perturb and elucidate biological processes. Small molecules can be rationally designed for a given target, or a library of molecules can be screened against a target or phenotype of interest. Especially in the case of phenotypic screening approaches, a major challenge is to translate the compound-induced phenotype into a well-defined cellular target and mode of action of the hit compound. There is no “one size fits all” approach, and recent years have seen an increase in available target deconvolution strategies, rooted in organic chemistry, proteomics, and genetics. This review provides an overview of advances in target identification and mechanism of action studies, describes the strengths and weaknesses of the different approaches, and illustrates the need for chemical biologists to integrate and expand the existing tools to increase the probability of evolving screen hits to robust chemical probes.


2010 ◽  
Vol 6 (1) ◽  
pp. 75-85 ◽  
Author(s):  
Scott M. Carlson ◽  
Forest M. White

2009 ◽  
Vol 14 (2) ◽  
pp. 111-120 ◽  
Author(s):  
Jingsong Yang ◽  
Robert A. Copeland ◽  
Zhihong Lai

High-throughput screening (HTS) is a common mechanism for identifying lead compounds for drug discovery efforts. Small molecules can inhibit enzymes by a variety of mechanisms, such as competitive, noncompetitive, and uncompetitive with respect to the substrate(s) of the catalytic reaction. To optimize the chances of finding the broadest diversity of inhibitor modalities during screening, one must run assays under ``balanced'' conditions where the potency of inhibitors with various modes of action falls within a similar range. When an enzyme reaction involves more than one substrate, the definition and assessment of the apparent potency of inhibitors (IC50), in relation to their true potency (Ki), can be nontrivial. This article provides a theoretical analysis, on the basis of the Cheng-Prusoff derivation, of the IC50/K i relationship of bisubstrate enzyme reactions following various sequential kinetic mechanisms, as well as the application and limitations of this information for defining optimal screening conditions for such enzymes. (Journal of Biomolecular Screening 2009:111-120)


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