Identifying natural products with agonist activity against human nuclear receptors in extracts of cultured marine microalgae. Sæther, T., Moldes-Anaya, A., Larsen, L. N., Larsen, T., Paulsen, S., & Nebb, H. I. In Keystone Symposia - Nuclear Receptors and Friends: Roles in Energy Homeostasis and Metabolic Dysfunction, 2013.
abstract   bibtex   
Nuclear receptors (NRs) are highly conserved transcription factors that regulate transcription in response to small lipophilic molecules. These receptors regulate the expression of genes involved in many critical processes such as embryonic development, metabolism and inflammation. Dysfunctional signalling of NRs is thought to be involved in diseases such as cancer, type 2 diabetes, obesity and dyslipidemia. All these facts make NRs attractive targets for pharmacological intervention and development of therapeutics. Several NR ligands with well-recognised biological effects are in clinical use, like the hypolipidemic fibrates (e.g. Tricor), acting as peroxisome proliferator-activated receptors alpha (PPARα) activators, and the anti-diabetic thiazolidinediones (e.g. Avandia), targeting PPARγ. However, the negative side effects reported for thiazolidinediones points to the need of finding new medicines for treating diseases like type 2 diabetes. A bioassay guided strategy on identification, purification and characterisation of PPAR ligands from cultured microalgae is presented here. We are making use of biologically assay systems incorporating unique protein targets to identify secondary metabolites possessing desirable pharmacological profile from extract generated from microalgae cultures. We have identified PPAR agonist activity in organic extracts from xenic cultures of marine diatoms. Identifying natural products with agonist activity against human nuclear receptors in extracts of cultured marine microalgae
@inproceedings{sa_ether_identifying_2013,
	Abstract = {Nuclear receptors (NRs) are highly conserved transcription factors that regulate transcription in response to small lipophilic molecules. These receptors regulate the expression of genes involved in many critical processes such as embryonic development, metabolism and inflammation. Dysfunctional signalling of NRs is thought to be involved in diseases such as cancer, type 2 diabetes, obesity and dyslipidemia. All these facts make NRs attractive targets for pharmacological intervention and development of therapeutics. Several NR ligands with well-recognised biological effects are in clinical use, like the hypolipidemic fibrates (e.g. Tricor), acting as peroxisome proliferator-activated receptors alpha (PPARα) activators, and the anti-diabetic thiazolidinediones (e.g. Avandia), targeting PPARγ. However, the negative side effects reported for thiazolidinediones points to the need of finding new medicines for treating diseases like type 2 diabetes. A bioassay guided strategy on identification, purification and characterisation of PPAR ligands from cultured microalgae is presented here. We are making use of biologically assay systems incorporating unique protein targets to identify secondary metabolites possessing desirable pharmacological profile from extract generated from microalgae cultures. We have identified PPAR agonist activity in organic extracts from xenic cultures of marine diatoms. Identifying natural products with agonist activity against human nuclear receptors in extracts of cultured marine microalgae},
	Author = {S{æ}ther, Thomas and Moldes-Anaya, Angel and Larsen, Laila Norrheim and Larsen, Terje and Paulsen, Steinar and Nebb, Hilde Irene},
	Booktitle = {Keystone {Symposia} - {Nuclear} {Receptors} and {Friends}: {Roles} in {Energy} {Homeostasis} and {Metabolic} {Dysfunction}},
	Title = {Identifying natural products with agonist activity against human nuclear receptors in extracts of cultured marine microalgae},
	Year = {2013}}

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