Can BRET-based biosensors be used to characterize G-protein mediated signaling pathways of an insect GPCR, the Schistocerca gregaria CRF-related diuretic hormone receptor?

Lismont, Els; Verbakel, Lina; Vogel, Elise; Corbisier, Jenny; Degroot, Gaetan-Nagim; Verdonck, Rik; Verlinden, Heleen; Marchal, Elisabeth; Springael, Jean–Yves; Broeck, Jozef Vanden

doi:10.1016/j.ibmb.2020.103392

Cited by 6 publications

(6 citation statements)

References 90 publications

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“…BRET has been utilized to develop sensors for the determination of conformational states of GPCRs under different conditions. In this regard, the cAMP-dependent BRET-based CAMYEL biosensor confirmed the activation of G α by direct interaction with the CRF-related diuretic hormone receptor . Recent developments have seen the creation of biosensor BRET platforms that either detect G-protein dissociation for a wide range of G-proteins (TRUEPATH) or directly detect the formation of Gα-GTP and free Gβγ (BERKY) .…”

Section: Optical Methods Of Analysismentioning

confidence: 88%

“…In this regard, the cAMP-depend-ent BRET-based CAMYEL biosensor confirmed the activation of G α by direct interaction with the CRF-related diuretic hormone receptor. 148 Recent developments have seen the creation of biosensor BRET platforms that either detect Gprotein dissociation for a wide range of G-proteins (TRUEPATH) 149 or directly detect the formation of Gα-GTP and free Gβγ (BERKY). 150 These recent BRET platforms provide new tools for interrogating G-protein activation quickly and with single-pathway resolution, opening new possibilities for interrogating G-protein signaling under physiological conditions.…”

Section: Conformational Changes Of Gpcrs Have Been Historicallymentioning

confidence: 99%

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Illuminating the Path to Target GPCR Structures and Functions

et al. 2020

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G-Protein-coupled receptors (GPCRs) are ubiquitous within eukaryotes, responsible for a wide array of physiological and pathological processes. Indeed, the fact that they are the most drugged target in the human genome is indicative of their importance. Despite the clear interest in GPCRs, most information regarding their activity has been so far obtained by analyzing the response from a “bulk medium”. As such, this Perspective summarizes some of the common methods for this indirect observation. Nonetheless, by inspecting approaches applying super-resolution imaging, we argue that imaging is perfectly situated to obtain more detailed structural and spatial information, assisting in the development of new GPCR-targeted drugs and clinical strategies. The benefits of direct optical visualization of GPCRs are analyzed in the context of potential future directions in the field.

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Section: Optical Methods Of Analysismentioning

confidence: 88%

Section: Conformational Changes Of Gpcrs Have Been Historicallymentioning

confidence: 99%

Illuminating the Path to Target GPCR Structures and Functions

et al. 2020

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“…Another developed strategy is using microbial secondary metabolites (SMs) that are produced during the late growth phase of microorganisms and can be an alternative to [83], allatotropin receptor in Bombyx mori [84], thyrotropin-releasing hormone receptor-like in Nilaparvata lugens [85], and corticotropin-releasing factor-related diuretic hormone receptor in Schistocerca gregaria [86] have been annotated. Recently, our group used RNA sequencing and de novo transcriptome assembly to identify 430 putative GPCRs in the stick insect Carausius morosus that can be targeted as putative pesticides targets.…”

Section: Accepted Articlementioning

confidence: 99%

“…In the past two decades, many GPCRs in insects such as Drosophila melanogaster , and corticotropin-releasing factor-related diuretic hormone receptor in Schistocerca gregaria [86] have been annotated. Recently, our group used RNA sequencing and de novo transcriptome assembly to identify 430 putative GPCRs in the stick insect Carausius morosus that can be targeted as putative pesticides targets.…”

Section: Next-generation Pesticidesmentioning

confidence: 99%

“…Moreover, the genes coding neurohormone and neuropeptide GPCRs and their ligands have been reported in insects; the Allatostatins‐A and Allatostatins‐C receptors in Apis mellifera [81], tachykinin receptor in Rhodnius prolixus [82], adipokinetic and corazonin hormone receptors in A. gambiae [83], allatotropin receptor in Bo. mori [84], thyrotropin‐releasing hormone receptor‐like in Nilaparvata lugens [85], and corticotropin‐releasing factor‐related diuretic hormone receptor in Schistocerca gregaria [86] have been annotated. Recently, our group used RNA sequencing and de novo transcriptome assembly to identify 430 putative GPCRs in the stick insect Carausius morosus that can be targeted as putative pesticides targets.…”

Section: Next‐generation Pesticidesmentioning

confidence: 99%

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Are insect GPCRs ideal next‐generation pesticides: opportunities and challenges

et al. 2021

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The increasing human population, combined with low inefficiency and adverse effects of available pesticides, has magnified the urgent need of developing next-generation pesticides. Among the available approaches, strategies targeting invertebrate G protein-coupled receptors (GPCRs) are very promising as these receptors are the targets of endogenous neuropeptides/neuromodulators that upon binding to their receptors induce profound changes in insect physiology. Therefore, exploring GPCR regulators has great potential in the development of targeted next-generation pesticides. Despite the great potential of such alternative pesticides, so far there has been only one approved compound, Amitraz, which conveys its antipest activity via the GPCR Octopamine receptor. Here, we review the current status of pesticide development, hazards associated with conventional pesticide compounds, alternative strategies that involve next-generation of pesticides, structural features of GPCRs, and opportunities and challenges of targeting the members of this superfamily in invertebrates to develop anti-pest agents. In conclusion, we emphasize that the potential of GPCRs cannot be utilized in full without more genomic and transcriptomic data to improve our understanding of the complex network of peptidergic signaling pathways. We argue how vital it is to obtain three-dimensional (3D) structural data on physiologically important target GPCRs and encourage the readers to use the state of the art in silico methods such as virtual screening for the discovery of new pesticide compounds.

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