Reduction of stress responses in honey bees by synthetic ligands targeting an allatostatin receptor
Sánchez-Morales, Adrià (Universitat Autònoma de Barcelona. Departament de Química)
Gigoux, Véronique (Toulouse Cancer Research Center (CRT))
Matsoukas, Minos Timotheos (Universitat Autònoma de Barcelona. Departament de Pediatria, Obstetrícia i Ginecologia i Medicina Preventiva i Salut Pública)
Pérez-Benito, Laura (Universitat Autònoma de Barcelona. Departament de Pediatria, Obstetrícia i Ginecologia i Medicina Preventiva i Salut Pública)
Fourmy, Daniel (Toulouse Cancer Research Center (CRT))
Alibes, Ramón (Universitat Autònoma de Barcelona. Departament de Química)
Busqué Sánchez, Félix (Universitat Autònoma de Barcelona. Departament de Química)
Cordomí Montoya, Arnau (Universitat Autònoma de Barcelona. Departament de Pediatria, Obstetrícia i Ginecologia i Medicina Preventiva i Salut Pública)
Devaud, Jean Marc (Université de Toulouse. Centre de Recherches Sur La Cognition Animale)

Fecha:	2022
Descripción:	14 pàg.
Resumen:	Honey bees are of great economic and ecological importance, but are facing multiple stressors that can jeopardize their pollination efficiency and survival. Therefore, understanding the physiological bases of their stress response may help defining treatments to improve their resilience. We took an original approach to design molecules with this objective. We took advantage of the previous identified neuropeptide allatostatin A (ASTA) and its receptor (ASTA-R) as likely mediators of the honey bee response to a biologically relevant stressor, exposure to an alarm pheromone compound. A first series of ASTA-R ligands were identified through in silico screening using a homology 3D model of the receptor and in vitro binding experiments. One of these (A8) proved also efficient in vivo, as it could counteract two behavioral effects of pheromone exposure, albeit only in the millimolar range. This putative antagonist was used as a template for the chemical synthesis of a second generation of potential ligands. Among these, two compounds showed improved efficiency in vivo (in the micromolar range) as compared to A8 despite no major improvement in their affinity for the receptor in vitro. These new ligands are thus promising candidates for alleviating stress in honey bees.
Ayudas:	Agencia Estatal de Investigación PID2019-106403RB-I00 Agencia Estatal de Investigación CTQ2016-75363-R
Nota:	Altres ajuts: French Research Agency, ANR-13-ADAP-0002-01
Derechos:	Aquest document està subjecte a una llicència d'ús Creative Commons. Es permet la reproducció total o parcial, la distribució, la comunicació pública de l'obra i la creació d'obres derivades, fins i tot amb finalitats comercials, sempre i quan es reconegui l'autoria de l'obra original.
Lengua:	Anglès
Documento:	Article ; recerca ; Versió publicada
Publicado en:	Scientific reports, Vol. 12 Núm. 1 (2022) , p. 16760, ISSN 2045-2322

DOI: 10.1038/s41598-022-20978-y
PMID: 36202961

14 p, 1.4 MB

El registro aparece en las colecciones:
Documentos de investigación > Documentos de los grupos de investigación de la UAB > Centros y grupos de investigación (producción científica) > Ciencias > Synthesis of Bioactive Organic Compounds and Functional Materials (SynOrgFUN)
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