De novo identification of highly active fluorescent kappa opioid ligands from a rhodamine labeled tetrapeptide positional scanning library

Houghten, Richard A.; Dooley, Colette T.; Appel, Jon R.

doi:10.1016/j.bmcl.2004.01.090

Cited by 25 publications

(23 citation statements)

References 21 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…To perform useful microscopy studies, a fluorescent ligand for a GPCR needs to show discrete plasma membrane binding which can be blocked by an unlabelled ligand, and low levels of non-specific binding (including intracellular fluorescence). There are many examples in the literature of fluorescent ligands with good imaging properties, including those for the vasopressin and oxytocin receptors (Corbani et al, 2011), kappa opioid receptor (Houghten et al, 2004), b 2 adrenergic receptor (Baker et al, 2011), adenosine-A 3 receptor and the leukotriene B 4 receptor (Sabirsh et al, 2005). Recent work in our laboratory has focused on the development of fluorescent ligands for the adenosine receptors with improved imaging properties.…”

Section: Required Properties Of a Fluorescent Ligandmentioning

confidence: 98%

Probing the pharmacology of G protein-coupled receptors with fluorescent ligands

et al. 2015

View full text Add to dashboard Cite

G protein-coupled receptors control a wide range of physiological processes and are the target for many clinically used drugs. Understanding the way in which receptors bind agonists and antagonists, their organisation in the membrane and their regulation after agonist binding are important properties which are key to developing new drugs. One way to achieve this knowledge is through the use of fluorescent ligands, which have been used to study the expression and function of receptors in endogenously expressing systems. Fluorescent ligands with appropriate imaging properties can be used in conjunction with confocal microscopy to investigate the regulation of receptors after activation. Alternatively, through the use of single molecule microscopy, they can probe the spatial organisation of receptors within the membrane. This review focuses on the techniques in which fluorescent ligands have been used and the novel aspects of G protein-coupled receptor pharmacology which have been uncovered. This article is part of the Special Issue entitled 'Fluorescent Tools in Neuropharmacology'.

show abstract

Section: Required Properties Of a Fluorescent Ligandmentioning

confidence: 98%

Probing the pharmacology of G protein-coupled receptors with fluorescent ligands

et al. 2015

View full text Add to dashboard Cite

show abstract

“…The advantage of this system is that it does not require purification of ZF proteins and allows a direct measurement of ZF-DNA interactions. Using this strategy, several ZF libraries were created by randomizing one amino acid residue at the time, similarly to the Houghten's positional fixing methodology in peptide screenings [43].…”

Section: In Vitro and In Vivo Strategies For The Se-lection Zf Domainmentioning

confidence: 99%

Rational Design, Selection and Specificity of Artificial Transcription Factors (ATFs): The Influence of Chromatin in Target Gene Regulation

Blancafort¹,

Beltran²

2008

CCHTS

View full text Add to dashboard Cite

Artificial Transcription Factors (ATFs) are engineered DNA-binding proteins designed to bind specific sequences of DNA. ATFs made of Zinc Finger (ZF) domains have been developed to regulate specific genes and phenotypes both in cells and whole organisms. Recently, an emerging application of engineered DNA-binding domains include the specific editing of the genome, the ability to specifically cut, recombine, modify DNA and image protein-nucleic acid interactions in living cells. In this review we will summarize the techniques used for the rational design, screening and functional selection of ZF proteins in mammalian cell systems and their applications in areas of biotechnology, functional genomics and molecular therapeutics. The in vivo specificity of the engineered ATFs will be discussed, with particular emphasis on epigenetic modifications influencing ATF-DNA interactions.

show abstract

“…Positional scanning libraries were later invented by Houghtens laboratory as an alternative synthetic and screening technique [215][216][217][218][219][220][221][222]. In this version of mixture screening, the libraries in which all positions are defined are synthesized and screened, and ligands deduced from the most active mixtures are synthesized and their activities tested.…”

Section: Synthesis Of Peptide Mixturesmentioning

confidence: 99%

Combinatorial/Library Peptide Synthesis

Lebl

2011

Amino Acids, Peptides and Proteins in Organic Chemistry

View full text Add to dashboard Cite

De novo identification of highly active fluorescent kappa opioid ligands from a rhodamine labeled tetrapeptide positional scanning library

Cited by 25 publications

References 21 publications

Probing the pharmacology of G protein-coupled receptors with fluorescent ligands

Probing the pharmacology of G protein-coupled receptors with fluorescent ligands

Rational Design, Selection and Specificity of Artificial Transcription Factors (ATFs): The Influence of Chromatin in Target Gene Regulation

Combinatorial/Library Peptide Synthesis

Contact Info

Product

Resources

About