The use of resonance energy transfer in high-throughput screening: BRET versus FRET.

Abstract:

:Bioluminescence resonance energy transfer has developed in recent years as a new technique to study protein-protein interactions. Protein partners of interest are tagged with either luciferase or green fluorescent protein (GFP). Non-radiative energy transfer between the excited luciferase and the GFP permits the study of spatial relationships between the two partners. This technique constitutes an important tool for the study of the functional activity of different types of receptors, and can be used in sensitive, homogenous high-throughput screening assays.

journal_name

Trends Pharmacol Sci

authors

Boute N,Jockers R,Issad T

doi

10.1016/s0165-6147(02)02062-x

subject

Has Abstract

pub_date

2002-08-01 00:00:00

pages

351-4

issue

8

eissn

0165-6147

issn

1873-3735

pii

S0165-6147(02)02062-X

journal_volume

23

pub_type

杂志文章,评审
  • Of mice and flies: commonalities among 5-HT receptors.

    abstract::Pharmacological studies as well as molecular cloning of 5-HT receptors have revealed a multiplicity of receptor subtypes, not only in mammals but, as discussed in this review by René Hen, also in molluscs and arthropods. Most of these receptors belong to the G protein-coupled receptor family, and their mechanism of ac...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/0165-6147(92)90054-a

    authors: Hen R

    更新日期:1992-04-01 00:00:00

  • Ca2+ channel beta-subunits: structural insights AID our understanding.

    abstract::It has taken 17 years from the first identification of a voltage-gated Ca2+ channel (CaV) beta-subunit as a band on a gel following purification of skeletal muscle dihydropyridine (DHP) receptors in 1987 to the publication of key information on the structures of Ca2+ channel beta-subunits. Three recent X-ray crystallo...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.tips.2004.10.008

    authors: Richards MW,Butcher AJ,Dolphin AC

    更新日期:2004-12-01 00:00:00

  • Are formyl peptide receptors novel targets for therapeutic intervention in ischaemia-reperfusion injury?

    abstract::Ischaemia-reperfusion (I/R) injury is a common feature of several diseases associated with high morbidity and mortality, such as stroke and myocardial infarction. The damaged tissue displays cardinal signs of inflammation and microvascular injury that, unless resolved, lead to long-term tissue damage with associated d...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.tips.2010.04.001

    authors: Gavins FN

    更新日期:2010-06-01 00:00:00

  • The ubiquitin-dependent proteolytic pathway in skeletal muscle: its role in pathological states.

    abstract::It is generally accepted that muscle wasting is caused by an increase in protein breakdown which seems to be associated with an ATP-dependent, non-lysosomal proteolytic system based on conjugation of proteins to the small polypeptide ubiquitin. Increases in ubiquitin conjugates and in ubiquitin mRNAs are found in the ...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/0165-6147(96)10021-3

    authors: Argilés JM,López-Soriano FJ

    更新日期:1996-06-01 00:00:00

  • New insights into activation of the steroid hormone receptor superfamily.

    abstract::For many years the prevailing view of how steroid hormone receptors exert their effects on gene transcription has been that these intracellular receptor proteins, upon association with their specific cognate ligands, undergo a transformation to a state where they are capable of interacting with chromatin and regulatin...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/0165-6147(92)90099-r

    authors: Power RF,Conneely OM,O'Malley BW

    更新日期:1992-08-01 00:00:00

  • Cancer and Microenvironment Plasticity: Double-Edged Swords in Metastasis.

    abstract::Cancer initiates at one site (primary tumor) and, in most cases, spreads to other distant organs (metastasis). During the multistep process of metastasis, primary tumor cells acquire cellular and phenotypic plasticity to survive and thrive in different environments. Moreover, cancer cells also utilize and educate micr...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.tips.2019.04.005

    authors: Zhuang X,Zhang H,Hu G

    更新日期:2019-06-01 00:00:00

  • 5-HT3 receptors in the CNS: 3B or not 3B?

    abstract::5-HT(3) receptors are widely distributed in the CNS and PNS where they participate in a variety of physiological processes. Native 5-HT(3) receptors in the CNS display functional and pharmacological heterogeneity, suggesting the existence of multiple receptor subunits. However, recent evidence suggests that of the two...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/S0165-6147(03)00051-8

    authors: van Hooft JA,Yakel JL

    更新日期:2003-04-01 00:00:00

  • Pharmacological inhibitors of MAPK pathways.

    abstract::Mitogen-activated protein kinases [MAPKs, also called extracellular signal-regulated kinases (ERKs)] are constituents of numerous signal transduction pathways, and are activated by protein kinase cascades. Intense efforts are under way to develop and evaluate compounds that target components of MAPK pathways. In this ...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/s0165-6147(00)01865-4

    authors: English JM,Cobb MH

    更新日期:2002-01-01 00:00:00

  • Allostatic Mechanisms of Opioid Tolerance Beyond Desensitization and Downregulation.

    abstract::Mechanisms of opioid tolerance have focused on adaptive modifications within cells containing opioid receptors, defined here as cellular allostasis, emphasizing regulation of the opioid receptor signalosome. We review additional regulatory and opponent processes involved in behavioral tolerance, and include mechanisti...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.tips.2016.08.002

    authors: Cahill CM,Walwyn W,Taylor AMW,Pradhan AAA,Evans CJ

    更新日期:2016-11-01 00:00:00

  • Assay strategies for identification of therapeutic leads that target protein trafficking.

    abstract::Receptors, enzymes, and ion channels are traditional targets of therapeutic development. A common strategy is to target these proteins with agents that either activate or suppress their activity with ligands or substrates that occupy orthosteric sites or have allosteric interactions. An alternative approach involves r...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.tips.2015.05.004

    authors: Conn PM,Spicer TP,Scampavia L,Janovick JA

    更新日期:2015-08-01 00:00:00

  • Novel Targeted Therapies for Inflammatory Bowel Disease.

    abstract::Our growing understanding of the immunopathogenesis of inflammatory bowel disease (IBD) has opened new avenues for developing targeted therapies. These advances in treatment options targeting different mechanisms of action offer new hope for personalized management. In this review we highlight emerging novel and easil...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.tips.2016.10.014

    authors: Coskun M,Vermeire S,Nielsen OH

    更新日期:2017-02-01 00:00:00

  • Nicotine addiction: the possible role of functional upregulation.

    abstract::Upregulation of binding to nicotinic acetylcholine receptors (nAChRs) is observed in the brains of both smokers and animals chronically exposed to nicotine, although whether this in vivo change is accompanied by an increase in receptor function is unknown. In vitro recordings indicate that alpha4beta2- and alpha7-subt...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/S0165-6147(00)01979-9

    authors: Buisson B,Bertrand D

    更新日期:2002-03-01 00:00:00

  • Functional versus chemical diversity: is biodiversity important for drug discovery?

    abstract::Prospecting the full biodiversity of nature to find leads for new drugs is not necessary. Because finding leads is aimed at identifying biological activity, structure is of secondary importance. Furthermore, although natural chemical diversity might be unrivalled, functional diversity is bound to be considerably less....

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章

    doi:10.1016/s0165-6147(02)02007-2

    authors: Tulp M,Bohlin L

    更新日期:2002-05-01 00:00:00

  • AGXT2: a promiscuous aminotransferase.

    abstract::Alanine-glyoxylate aminotransferase 2 (AGXT2) is a multifunctional mitochondrial aminotransferase that was first identified in 1978. The physiological importance of AGXT2 was largely overlooked for three decades because AGXT2 is less active in glyoxylate metabolism than AGXT1, the enzyme that is deficient in primary h...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.tips.2014.09.005

    authors: Rodionov RN,Jarzebska N,Weiss N,Lentz SR

    更新日期:2014-11-01 00:00:00

  • Novel interactions between K+ channels and scorpion toxins.

    abstract::K(+) channels are macromolecules embedded in biological membranes, where they play a key role in cellular excitability and signal transduction pathways. Knowledge of their structure should help improve our understanding of their function and lead to the design of therapeutic compounds. Most pharmacological and structu...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/S0165-6147(03)00080-4

    authors: Rodríguez de la Vega RC,Merino E,Becerril B,Possani LD

    更新日期:2003-05-01 00:00:00

  • Epoxyeicosatrienoic Acid as Therapy for Diabetic and Ischemic Cardiomyopathy.

    abstract::Cardiovascular disease remains the leading cause of death worldwide. Among many potential targets for pharmacological intervention, a promising strategy involves epoxyeicosatrienoic acid (EET) and soluble epoxide hydroxylase (sEH) inhibition. sEH is the enzyme that converts EET to its less potent metabolite; therefore...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.tips.2016.08.001

    authors: Romashko M,Schragenheim J,Abraham NG,McClung JA

    更新日期:2016-11-01 00:00:00

  • Molecular biology of 5-HT receptors.

    abstract::Within the past six months, isolation of cDNA or genomic clones has been reported for three 5-HT receptors, the 5-HT1C, 5-HT1A and 5-HT2 subtypes. As members of the G protein receptor superfamily, all three 5-HT receptor clones encode single-subunit proteins containing approximately 450 amino acids arrayed as seven in...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/0165-6147(89)90080-1

    authors: Hartig PR

    更新日期:1989-02-01 00:00:00

  • Toward understanding ubiquitin-modifying enzymes: from pharmacological targeting to proteomics.

    abstract::Ubiquitination is a highly conserved post-translational modification that regulates protein trafficking, function, and turnover. Ubiquitin ligases (E3s) conjugate ubiquitin polypeptides on substrates, whereas deubiquitnases (DUBs) reverse ubiquitination. Engineering of chemical antagonists and inhibitors of ubiquitin ...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.tips.2014.01.005

    authors: Lill JR,Wertz IE

    更新日期:2014-04-01 00:00:00

  • Resolution of airway disease: removal of inflammatory cells through apoptosis, egression or both?

    abstract::Pathogenic granulocytes (eosinophils and neutrophils) infiltrate airway tissues in asthma and chronic obstructive pulmonary disease. Granulocytes release tissue-toxic and inflammatory mediators, making their removal an important pharmacological goal. Removal is thought to be accomplished through apoptosis followed by ...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章

    doi:10.1016/j.tips.2006.07.006

    authors: Uller L,Persson CG,Erjefält JS

    更新日期:2006-09-01 00:00:00

  • Molecular characterization of alpha 1- and alpha 2-adrenoceptors.

    abstract::Three 'alpha 1-adrenoceptors' and three 'alpha 2-adrenoceptors' have now been cloned. How closely do these receptors match the native receptors that have been identified pharmacologically? What are the properties of these receptors, and how do they relate to other members of the cationic amine receptor family? Kevin L...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/0165-6147(91)90499-i

    authors: Harrison JK,Pearson WR,Lynch KR

    更新日期:1991-02-01 00:00:00

  • Regulation of mglu(7) receptors by proteins that interact with the intracellular C-terminus.

    abstract::The metabotropic glutamate type 7 (mglu(7)) receptor is a widely distributed, mainly presynaptic Group III mglu receptor that can regulate glutamate release. Recently, largely as a result of the identification of specific proteins that interact with the C-terminal domain of this receptor, considerable progress has bee...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/s0165-6147(00)01684-9

    authors: Dev KK,Nakanishi S,Henley JM

    更新日期:2001-07-01 00:00:00

  • Reactivation of p53: from peptides to small molecules.

    abstract::Approximately 27 million people are living with a tumour in which the tumour suppressing activity of p53 has been inactivated. In half of these tumours, p53 itself is not mutated but the pathway is partially abrogated. Mechanisms include the overexpression of negative regulators of p53, such as MDM2 and MDM4, and dele...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.tips.2010.11.004

    authors: Brown CJ,Cheok CF,Verma CS,Lane DP

    更新日期:2011-01-01 00:00:00

  • Off-target effects associated with long dsRNAs in Drosophila RNAi screens.

    abstract::Evidence of off-target effects (OTEs) associated with small interfering (si)RNAs (19-29bp) in mammalian cells has existed for several years. Two recent articles demonstrate that short sequences within long double-stranded (ds)RNAs frequently cause undesirable OTEs in cultured Drosophila cells. These results reveal the...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章

    doi:10.1016/j.tips.2007.02.009

    authors: Moffat J,Reiling JH,Sabatini DM

    更新日期:2007-04-01 00:00:00

  • Discoidin Domains as Emerging Therapeutic Targets.

    abstract::Discoidin (DS) domains are found in eukaryotic and prokaryotic extracellular and transmembrane multidomain proteins. These small domains play different functional roles and can interact with phospholipids, glycans, and proteins, including collagens. DS domain-containing proteins are often involved in cellular adhesion...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.tips.2016.06.003

    authors: Villoutreix BO,Miteva MA

    更新日期:2016-08-01 00:00:00

  • Chemokines, chemokine receptors and small-molecule antagonists: recent developments.

    abstract::The physiological roles of chemokine receptors have expanded beyond host defense and now represent important targets for intervention in several disease indications. Chemokine receptors have joined the ranks of other members of the G-protein-coupled receptor (GPCR) family in therapeutic potential as small-molecule che...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/s0165-6147(02)02064-3

    authors: Onuffer JJ,Horuk R

    更新日期:2002-10-01 00:00:00

  • Rho-Rho-kinase pathway in smooth muscle contraction and cytoskeletal reorganization of non-muscle cells.

    abstract::Hypercontraction or abnormal contraction of vascular smooth muscle is a major cause of diseases such as hypertension and vasospasm of the coronary and cerebral arteries. A better understanding of the mechanism of regulation of smooth muscle contraction should lead to improved treatments for such diseases. Recent studi...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/s0165-6147(00)01596-0

    authors: Fukata Y,Amano M,Kaibuchi K

    更新日期:2001-01-01 00:00:00

  • The Action Radius of Oxytocin Release in the Mammalian CNS: From Single Vesicles to Behavior.

    abstract::The hypothalamic neuropeptide oxytocin (OT) has attracted the attention both of the scientific community and a general audience because of its prosocial effects in mammals, and OT is now seen as a facilitator of mammalian species propagation. Furthermore, OT is a candidate for the treatment of social deficits in sever...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.tips.2017.08.005

    authors: Chini B,Verhage M,Grinevich V

    更新日期:2017-11-01 00:00:00

  • Historical review: a brief history and personal retrospective of seven-transmembrane receptors.

    abstract::Pharmacologists have studied receptors for more than a century but a molecular understanding of their properties has emerged only during the past 30-35 years. In this article, I provide a personal retrospective of how developments and discoveries primarily during the 1970s and 1980s led to current concepts about the l...

    journal_title:Trends in pharmacological sciences

    pub_type: 历史文章,杂志文章

    doi:10.1016/j.tips.2004.06.006

    authors: Lefkowitz RJ

    更新日期:2004-08-01 00:00:00

  • Heat Shock Proteins and Cancer.

    abstract::Heat shock proteins (HSPs) constitute a large family of proteins involved in protein folding and maturation whose expression is induced by heat shock or other stressors. The major groups are classified based on their molecular weights and include HSP27, HSP40, HSP60, HSP70, HSP90, and large HSPs. HSPs play a significa...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.tips.2016.11.009

    authors: Wu J,Liu T,Rios Z,Mei Q,Lin X,Cao S

    更新日期:2017-03-01 00:00:00

  • Folding Underlies Bidirectional Role of GPR37/Pael-R in Parkinson Disease.

    abstract::Since conformational flexibility, which is required for the function of a protein, comes at the expense of structural stability, many proteins, including G-protein-coupled receptors (GPCRs), are under constant risk of misfolding and aggregation. In this regard GPR37 (also named PAEL-R and ETBR-LP-1) takes a prominent ...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.tips.2017.05.006

    authors: Leinartaité L,Svenningsson P

    更新日期:2017-08-01 00:00:00