Temporal and spatial expression patterns of two G-protein coupled receptors inDrosophila melanogaster

G-protein coupled receptors (GPCRs) play important roles in cell biology and insects’ physiological processes, toxicological response and the development of insecticide resistance. New information on genome sequences, proteomic and transcriptome analysis and expression patterns of GPCRs in organs such as the central nervous system in different organisms has shown the importance of these signaling regulatory GPCRs and their impact on vital cell functions. Our growing understanding of the role played by GPCRs at the cellular, genome, transcriptome and tissue levels is now being utilized to develop new targets that will sidestep many of the problems currently hindering human disease control and insect pest management. This article reviews recent work on the expression and function of GPCRs in insects, focusing on the molecular complexes governing the insect physiology and development of insecticide resistance and examining the genome information for GPCRs in two medically important insects, mosquitoes and house flies, and their orthologs in the model insect species Drosophila melanogaster. The tissue specific distribution and expression of the insect GPCRs is discussed, along with fresh insights into practical aspects of insect physiology and toxicology that could be fundamental for efforts to develop new, more effective, strategies for pest control and resistance management.

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G Protein-Coupled Receptors: Functional and Mechanistic Insights Through Altered Gene Expression

Physiological Reviews ◽

10.1152/physrev.1998.78.1.35 ◽

1998 ◽

Vol 78 (1) ◽

pp. 35-52 ◽

Cited By ~ 81

Author(s):

DANIEL K. ROHRER ◽

BRIAN K. KOBILKA

Keyword(s):

Gene Expression ◽

G Protein ◽

Mechanism Of Action ◽

Expression Patterns ◽

G Protein Coupled Receptors ◽

Action Current ◽

Altered Expression ◽

Altered Gene Expression ◽

Altered Gene ◽

G Protein Coupled

Rohrer, Daniel K., and Brian K. Kobilka. G-Protein Coupled Receptors: Functional and Mechanistic Insights Through Altered Gene Expression. Physiol. Rev. 78: 35–52, 1998. — G protein-coupled receptors (GPCRs) comprise a large and diverse family of molecules that play essential roles in signal transduction. In addition to a constantly expanding pharmacological repertoire, recent advances in the ability to manipulate GPCR expression in vivo have provided another valuable approach in the study of GPCR function and mechanism of action. Current technologies now allow investigators to manipulate GPCR expression in a variety of ways. Graded reductions in GPCR expression can be achieved through antisense strategies or total gene ablation or replacement can be achieved through gene targeting strategies, and exogenous expression of wild-type or mutant GPCR isoforms can be accomplished with transgenic technologies. Both the techniques used to achieve these specific alterations and the consequences of altered expression patterns are reviewed here and discussed in the context of GPCR function and mechanism of action.

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G-protein-coupled receptors for free fatty acids: nutritional and therapeutic targets

British Journal Of Nutrition ◽

10.1017/s0007114513002249 ◽

2014 ◽

Vol 111 (S1) ◽

pp. S3-S7 ◽

Cited By ~ 29

Author(s):

Graeme Milligan ◽

Trond Ulven ◽

Hannah Murdoch ◽

Brian D. Hudson

Keyword(s):

Fatty Acids ◽

Fatty Acid ◽

Free Fatty Acid ◽

Free Fatty Acids ◽

G Protein ◽

Metabolic Diseases ◽

Expression Patterns ◽

Nutrient Sensing ◽

G Protein Coupled Receptors ◽

G Protein Coupled

It is becoming evident that nutrients and metabolic intermediates derived from such nutrients regulate cellular function by activating a number of cell-surface G-protein coupled receptors (GPCRs). Until now, members of the GPCR family have largely been considered as the molecular targets that communicate cellular signals initiated by hormones and neurotransmitters. Recently, based on tissue expression patterns of these receptors and the concept that they may elicit the production of a range of appetite- and hunger-regulating peptides, such nutrient sensing GPCRs are attracting considerable attention due to their potential to modulate satiety, improve glucose homeostasis and supress the production of various pro-inflammatory mediators. Despite the developing interests in these nutrients sensing GPCR both as sensors of nutritional status, and targets for limiting the development of metabolic diseases, major challenges remain to exploit their potential for therapeutic purposes. Mostly, this is due to limited characterisation and validation of these receptors because of paucity of selective and high-potency/affinity pharmacological agents to define the detailed function and regulation of these receptors. However, ongoing clinical trials of agonists of free fatty acid receptor 1 suggest that this receptor and other receptors for free fatty acids may provide a successful strategy for controlling hyperglycaemia and providing novel approaches to treat diabetes. Receptors responsive to free fatty acid have been of particular interest, and some aspects of these are considered herein.

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