Kevin Pfleger

2019

Complex Formation between VEGFR2 and the β₂-Adrenoceptor

Kilpatrick, L. E., Alcobia, D. C., White, C. W., Peach, C. J., Glenn, J. R., Zimmerman, K., Kondrashov, A., Pfleger, K. D. G., Ohana, R. F., Robers, M. B., Wood, K. V., Sloan, E. K., Woolard, J. & Hill, S. J., 20 Jun 2019, In : Cell Chemical Biology. 26, 6, p. 830-841.e9

Research output: Contribution to journal › Article

Open Access

Adrenergic Receptors

Intracellular Signaling Peptides and Proteins

Bioluminescence

Endosomes

Energy Transfer

Disease-associated missense variants in ZBTB18 disrupt DNA binding and impair the development of neurons within the embryonic cerebral cortex

Hemming, I. A., Clément, O., Gladwyn-Ng, I. E., Cullen, H. D., Ng, H. L., See, H. B., Ngo, L., Ulgiati, D., Pfleger, K. D. G., Agostino, M. & Heng, J. I. T., 21 May 2019, In : Human Mutation. 15 p.

Research output: Contribution to journal › Article

Cerebral Cortex

Neurons

DNA

Zinc Fingers

Brain Diseases

I8-arachnotocin–an arthropod-derived G protein-biased ligand of the human vasopressin V₂ receptor

Duerrauer, L., Muratspahić, E., Gattringer, J., Keov, P., Mendel, H. C., Pfleger, K. D. G., Muttenthaler, M. & Gruber, C. W., 1 Dec 2019, In : Scientific Reports. 9, 1, 19295.

Research output: Contribution to journal › Article

Open Access

Arthropods

GTP-Binding Proteins

Pharmacology

Ligands

Arrestin

4 Citations (Scopus)

77 Downloads (Pure)

NanoBRET ligand binding at a GPCR under endogenous promotion facilitated by CRISPR/Cas9 genome editing

White, C. W., Johnstone, E. K. M., See, H. B. & Pfleger, K. D. G., Feb 2019, In : Cellular Signalling. 54, p. 27-34 8 p.

Research output: Contribution to journal › Article

Open Access

File

2 Citations (Scopus)

Transactivation of RAGE mediates angiotensin-induced inflammation and atherogenesis

Pickering, R., Tikellis, C., Rosado, C., Tsorotes, D., Dimitrropoulos, A., Smith, M., Huet, O., Seeber, R., Abhayawardana, R., Johnstone, E., Golledge, J., Wang, Y., Jandeleit-Dahm, K., Cooper, M., Pfleger, K. & Thomas, M. C., 2 Jan 2019, In : The Journal of clinical investigation. 129, 1, p. 406-421 CI99987.

Research output: Contribution to journal › Article

Open Access

Angiotensins

Transcriptional Activation

Atherosclerosis

Inflammation

Angiotensin II

2018

2 Citations (Scopus)

112 Downloads (Pure)

BRET-based assay to monitor EGFR transactivation by the AT₁R reveals G_q/11 protein-independent activation and AT₁R-EGFR complexes

O'Brien, S. L., Johnstone, E. K. M., Devost, D., Conroy, J., Reichelt, M. E., Purdue, B. W., Ayoub, M. A., Kawai, T., Inoue, A., Eguchi, S., Hébert, T. E., Pfleger, K. D. G. & Thomas, W. G., 1 Dec 2018, In : Biochemical Pharmacology. 158, p. 232-242 11 p.

Research output: Contribution to journal › Article

Open Access

File

Gq-G11 GTP-Binding Protein alpha Subunits

Bioluminescence

Energy Transfer

Epidermal Growth Factor Receptor

Energy transfer

2 Citations (Scopus)

Investigation of interactions between TLR2, MyD88 and TIRAP by bioluminescence resonance energy transfer is hampered by artefacts of protein overexpression

Sampaio, N. G., Kocan, M., Schofield, L., Pfleger, K. D. G. & Eriksson, E. M., 1 Aug 2018, In : PLoS One. 13, 8, e0202408.

Research output: Contribution to journal › Article

Open Access

Bioluminescence

bioluminescence

Energy Transfer

energy transfer

Artifacts

2017

14 Citations (Scopus)

Key determinants of selective binding and activation by the monocyte chemoattractant proteins at the chemokine receptor CCR2

Huma, Z. E., Sanchez, J., Lim, H. D., Bridgford, J. L., Huang, C., Parker, B. J., Pazhamalil, J. G., Porebski, B. T., Pfleger, K. D. G., Lane, J. R., Canals, M. & Stone, M. J., 23 May 2017, In : Science Signaling. 10, 480, eaai8529.

Research output: Contribution to journal › Article

Monocyte Chemoattractant Proteins

Chemokine Receptors

Chemokines

Chemical activation

Chemokine CCL2

16 Citations (Scopus)

Using nanoBRET and CRISPR/Cas9 to monitor proximity to a genome-edited protein in real-time

White, C. W., Vanyai, H. K., See, H. B., Johnstone, E. K. M. & Pfleger, K. D. G., 9 Jun 2017, In : Scientific Reports. 7, 1, 3187.

Research output: Contribution to journal › Article

Open Access

Clustered Regularly Interspaced Short Palindromic Repeats

Energy Transfer

Genome

G-Protein-Coupled Receptors

Proteins

2016

44 Citations (Scopus)

Fluorescence- and bioluminescence-based approaches to study GPCR ligand binding

Stoddart, L. A., White, C., Nguyen, K., Hill, S. & Pfleger, K., 1 Oct 2016, In : British Journal of Pharmacology. 173, 20, p. 3028-3037 10 p.

Research output: Contribution to journal › Article

Open Access

Fluorescence

Ligands

Fluorescence Resonance Energy Transfer

Pharmacology

Fluorescence Polarization

104 Citations (Scopus)

G Protein-Coupled Receptor Heteromers

Gomes, I., Ayoub, M. A., Fujita, W., Jaeger, W., Pfleger, K. & Devi, L. A., 2016, In : Annual Review of Pharmacology and Toxicology. 56, p. 403-425

Research output: Contribution to journal › Article

G-Protein-Coupled Receptors

Physiological Phenomena

Pathologic Processes

Membrane Proteins

Pharmacology

25 Citations (Scopus)

i-bodies, human single domain antibodies that antagonize chemokine receptor CXCR4

Griffiths, K., Dolezal, O., Cao, B., Nilsson, S. K., See, E. B., Pfleger, K. D. G., Roche, M., Gorry, P. R., Pow, A., Viduka, K., Lim, K., Lu, B. G. C., Chang, D. H. C., Murray-Rust, T., Kvansakul, M., Perugini, M. A., Dogovski, C., Doerflinger, M., Zhang, Y., Parisi, K. & 3 othersCasey, J. L., Nuttall, S. D. & Foley, M., 2016, In : Journal of Biological Chemistry. 291, 24, p. 12641-12657 17 p.

Research output: Contribution to journal › Article

Single-Domain Antibodies

Chemokine Receptors

Stem cells

Human Body

Hematopoietic Stem Cell Mobilization

11 Citations (Scopus)

Mutations of vasopressin receptor 2 including novel L312S have differential effects on trafficking

Tiulpakov, A., White, C., Abhayawardana, R., See, H. B., Chan, A., Seeber, R., Heng, J., Dedov, I., Pavlos, N. & Pfleger, K., 1 Aug 2016, In : Molecular Endocrinology. 30, 8, p. 889-904

Research output: Contribution to journal › Article

Open Access

Vasopressin Receptors

Mutation

Hyponatremia

Nephrogenic Diabetes Insipidus

Natriuresis

2015

86 Citations (Scopus)

Application of BRET to monitor ligand binding to GPCRs

Stoddart, L. A., Johnstone, E., Wheal, A. J., Goulding, J., Robers, M. B., Machleidt, T., Wood, K. V., Hill, S. & Pfleger, K., Jul 2015, In : Nature Methods. 12, 7, p. 661-663 3 p.

Research output: Contribution to journal › Article

Open Access

Bioluminescence

Energy Transfer

G-Protein-Coupled Receptors

Energy transfer

Luminescent Proteins

20 Citations (Scopus)

408 Downloads (Pure)

Functional Interaction between Angiotensin II Receptor Type 1 and Chemokine (C-C motif) Receptor 2 with Implications for Chronic Kidney Disease

Ayoub, M., Zhang, Y., Kelly, R. S., See, E., Johnstone, E., Mccall, E. A., Williams, J. H., Kelly, D. J. & Pfleger, K., 25 Mar 2015, In : PLoS One. 10, 3, 22 p., e0119803.

Research output: Contribution to journal › Article

Open Access

File

CCR Receptors

Angiotensin Type 1 Receptor

angiotensin II

G-Protein-Coupled Receptors

kidney diseases

2014

7 Citations (Scopus)

Homogeneous time-resolved fluorescence-based assay to monitor extracellular signal-regulated kinase signaling in a high-throughput format

Ayoub, M., Trebaux, J., Vallaghe, J., Charrier-Savournin, F., Al-Hosaini, K., Gonzalez Moya, A., Pin, J-P., Pfleger, K. & Trinquet, E., 2014, In : Frontiers in Endocrinology. 5, p. 1-11

Research output: Contribution to journal › Article

Open Access

12 Citations (Scopus)

Molecular determinants of orexin receptor-arrestin-ubiquitin complex formation

Jaeger, W., Seeber, R., Eidne, K. & Pfleger, K., Jan 2014, In : British Journal of Pharmacology. 171, 2, p. 364-374

Research output: Contribution to journal › Article

Open Access

2013

15 Citations (Scopus)

AIGaN/GaN-based biosensor for label-free detection of biological activity

Podolska, A., Hool, L., Pfleger, K., Mishra, U. K., Parish, G. & Nener, B., 2013, In : SENSORS AND ACTUATORS B-CHEMICAL. 177, p. 577-582

Research output: Contribution to journal › Article

19 Citations (Scopus)

Characterization of Three Vasopressin Receptor 2 Variants: An Apparent Polymorphism (V266A) and Two Loss-of-Function Mutations (R181C and M311V)

Armstrong, S., Seeber, R., Ayoub, M., Feldman, B. J. & Pfleger, K., 2013, In : PLoS One. 8, 6, p. 9pp e65885.

Research output: Contribution to journal › Article

Open Access

33 Citations (Scopus)

Identification and profiling of CXCR3-CXCR4 chemokine receptor heteromer complexes

Watts, A. O., Van Lipzig, M. M. H., Jaeger, W., Seeber, R., Van Zwam, M., Vinet, J., Van Der Lee, M. M. C., Siderius, M. H., Zaman, G. J. R., Boddeke, H. W. G. M., Smit, M. J., Pfleger, K., Leurs, R. & Vischer, H. F., 2013, In : British Journal of Pharmacology. 168, 7, p. 1662-1674

Research output: Contribution to journal › Article

CXC Chemokines

Chemokine Receptors

CC Chemokines

Chemokines

CCR2 Receptors

9 Citations (Scopus)

Profiling Epidermal Growth Factor Receptor and Heregulin Receptor 3 Heteromerization Using Receptor Tyrosine Kinase Heteromer Investigation Technology

Ayoub, M., See, E., Seeber, R., Armstrong, S. & Pfleger, K., 2013, In : PLoS One. 8, 5, p. 10pp e64672.

Research output: Contribution to journal › Article

Open Access

19 Citations (Scopus)

Quantitative Förster resonance energy transfer efficiency measurements using simultaneous spectral unmixing of excitation and emission spectra

Mustafa, S., Hannagan, J., Rigby, P., Pfleger, K. & Corry, B., 2013, In : Journal of Biomedical Optics. 18, 2, p. 026024-1 - 026024-14

Research output: Contribution to journal › Article

Open Access

2012

18 Citations (Scopus)

Biocompatibility of semiconducting AIGaN/GaN material with living cells

Podolska, A., Tham, S., Hart, R. D., Seeber, R., Kocan, M., Kocan, M., Mishra, U. K., Pfleger, K., Parish, G. & Nener, B., 2012, In : SENSORS AND ACTUATORS B-CHEMICAL. 169, p. 401-406

Research output: Contribution to journal › Article

38 Citations (Scopus)

Deleterious GRM1 Mutations in Schizophrenia

Ayoub, M., Angelicheva, D., Vile, D., Chandler, D., Morar, B., Cavanaugh, J. A., Visscher, P. M., Jablensky, A., Pfleger, K. & Kalaydjieva, L., 2012, In : PLoS One. 7, p. 8pp e32849.

Research output: Contribution to journal › Article

Open Access

36 Citations (Scopus)

Effect of enhanced Renilla luciferase and fluorescent protein variants on the Förster distance of Bioluminescence resonance energy transfer (BRET)

Dacres, H., Michie, M., Wang, J., Pfleger, K. & Trowell, S. C., 2012, In : Biochemical and Biophysical Research Communications. 425, p. 625-629

Research output: Contribution to journal › Article

37 Citations (Scopus)

Identification and profiling of novel α 1A-adrenoceptor-CXC chemokine receptor 2 heteromer

Mustafa, S., See, E., Seeber, R., Armstrong, S. P., White, C. W., Ventura, S., Ayoub, M. & Pfleger, K., 2012, In : Journal of Biological Chemistry. 287, 16, p. 12952-12965

Research output: Contribution to journal › Article

Open Access

2011

39 Citations (Scopus)

Application of G Protein-Coupled Receptor-Heteromer Identification Technology to Monitor beta-arrestin Recruitment to G Protein-Coupled Receptor Heteromers

See, E., Seeber, R., Kocan, M., Eidne, K. & Pfleger, K., 2011, In : Assay and Drug Development Technologies. 9, 1, p. 21-30

Research output: Contribution to journal › Article

Enhanced BRET technology for the monitoring of agonist-induced and agonist-independent interactions between GPCRs and β-arrestins

Kocan, M., Dalrymple, M., Seeber, R., Feldman, B. J. & Pfleger, K., 2011, In : Frontiers in Endocrinology. 1, p. 1-9 12.

Research output: Contribution to journal › Article

14 Citations (Scopus)

G Protein-Coupled Receptor Heteromer Identification Technology: Identification and Profiling of GPCR Heteromers

Mustafa, S. & Pfleger, K., 2011, In : Journal of Laboratory Automation. 16, p. 285-291

Research output: Contribution to journal › Article

Open Access

36 Citations (Scopus)

Heteromerization of angiotensin receptors changes trafficking and arrestin recruitment profiles

Porrello, E. R., Pfleger, K., Seeber, R., Qian, H., Oro, C., Abogadie, F., Delbridge, L. M. D. & Thomas, W. G., 2011, In : Cellular Signalling. 23, p. 1767-1776

Research output: Contribution to journal › Article

22 Citations (Scopus)

Temporal Profiling of Orexin Receptor-Arrestin-Ubiquitin Complexes Reveals Differences between Receptor Subtypes

Dalrymple, M., Jaeger, W., Eidne, K. & Pfleger, K., 2011, In : Journal of Biological Chemistry. 286, p. 16726-16733

Research output: Contribution to journal › Article

Open Access

2010

47 Citations (Scopus)

Differential association modes of the thrombin receptor PAR1 with Gαi1, Gα12, and β-arrestin 1

Ayoub, M., Trinquet, E., Pfleger, K. & Pin, J-P., 2010, In : FASEB Journal. 24, p. 3522-3535

Research output: Contribution to journal › Article

74 Citations (Scopus)

Recent advances in bioluminescence resonance energy transfer technologies to study GPCR heteromerization

Ayoub, M. & Pfleger, K., 2010, In : Current Opinion in Pharmacology. 10, p. 44-52

Research output: Contribution to journal › Article

14 Citations (Scopus)

Uncovering GPCR heteromer-biased ligands

Mustafa, S., Ayoub, M. & Pfleger, K., 2010, In : Drug Discovery Today. 7, p. 77-85

Research output: Contribution to journal › Article

2009

34 Citations (Scopus)

Agonist-independent interactions between beta-arrestins and mutant vasopressin type II receptors associated with nephrogenic syndrome of inappropriate antidiuresis

Kocan, M., See, E., Sampaio, N., Eidne, K., Feldman, B. J. & Pfleger, K., 2009, In : Molecular Endocrinology. 23, 4, p. 559-571

Research output: Contribution to journal › Article

Vasopressin Receptors

Hyponatremia

Codon

Mutation

Arginine

262 Citations (Scopus)

Building a new conceptual framework for receptor heteromers

Ferré, S., Baler, R., Bouvier, M., Caron, M. G., Devi, L. A., Fuxw, K., Durroux, T., Javitch, J. A., George, S. R., Lohse, M. J., Mackie, K., Milligan, G., Pfleger, K., Pin, J. P., Volkow, N. D., Waldhoer, M., Woods, A. S. & Franco, R., 2009, In : Nature Chemical Biology. 5, 3, p. 131-134

Research output: Contribution to journal › Article

G-protein-coupled receptors in drug discovery - seventh annual Informa conference

Pfleger, K., 2009, In : IDRUGS. 12, 5, p. 288-290

Research output: Contribution to journal › Article

2008

20 Citations (Scopus)

Changes to Gonadotropin-Releasing Hormone (GnRH) Receptor Extracellular Loops Differtially Affect GnRH Analog Binding and Activation : Evidence for Distinct Ligand-Stabilized Receptor Conformations

Pfleger, K., Pawson, A. J. & Millar, R. P., 2008, In : Endocrinology. 149, 6, p. 3118-3129

Research output: Contribution to journal › Article

LHRH Receptors

Gonadotropin-Releasing Hormone

Ligands

Catfishes

Mutation

70 Citations (Scopus)

Demonstration of Improvements to the Bioluminescence Resonance Energy Transfer (BRET) Technology for the Monitoring of G Protein-Coupled Receptors in Live Cells

Kocan, M., See, E., Seeber, R., Eidne, K. & Pfleger, K., 2008, In : Journal of Biomolecular Screening. 13, 9, p. 888-898

Research output: Contribution to journal › Article

Bioluminescence

Arrestin

Energy Transfer

G-Protein-Coupled Receptors

Thyrotropin Releasing Hormone Receptors

81 Citations (Scopus)

G protein-coupled receptor dimers: Functional consequences, disease states and drug targets

Dalrymple, M., Pfleger, K. & Eidne, K., 2008, In : Pharmacology & Therapeutics. 118, 3, p. 359-371

Research output: Contribution to journal › Article

G-Protein-Coupled Receptors

Pharmacology

Pharmaceutical Preparations

Ligands

Therapeutics

G Protein Coupled Receptors as Drug Targets: The Role of scientific symbols beta-Arrestins

Dromey, J. & Pfleger, K., 2008, In : Endocrine, Metabolic & Immune Disorders - Drug Targets. 7, p. 51-61

Research output: Contribution to journal › Article

2007

30 Citations (Scopus)

Monitoring interactions between G-protein-coupled receptors and ß-arrestins

Pfleger, K., Dalrymple, M., Dromey, J. & Eidne, K., 2007, In : Biochemical Society Transactions. 35, 4, p. 764-766

Research output: Contribution to journal › Article

Arrestins

G-Protein-Coupled Receptors

Monitoring

Bioluminescence

Arrestin

2006

131 Citations (Scopus)

Bioluminescence resonance energy transfer (BRET) for the real-time detection of protein-protein interactions

Pfleger, K., Seeber, R. & Eidne, K., 2006, In : Nature Protocols. 1, 1, p. 336-345

Research output: Contribution to journal › Article

Bioluminescence

Energy Transfer

Energy transfer

Proteins

Cell culture

77 Citations (Scopus)

Extended bioluminescence resonance energy transfer (eBRET) for monitoring prolonged protein-protein interactions in live cells

Pfleger, K., Dromey, J., Dalrymple, M., Lim, E., Thomas, W. G. & Eidne, K., 2006, In : Cellular Signalling. 18, 10, p. 1664-1670

Research output: Contribution to journal › Article

Energy Transfer

Proteins

Drug Industry

G-Protein-Coupled Receptors

Technology

364 Citations (Scopus)

Illuminating insights into protein-protein interactions using bioluminescence resonance energy transfer (BRET)

Pfleger, K. & Eidne, K., 2006, In : Nature Methods. 3, 3, p. 165-174

Research output: Contribution to journal › Article

Bioluminescence

Energy Transfer

Energy transfer

Proteins

Molecules

2005

9 Citations (Scopus)

Helix I of beta-arrestin is involved in postendocytic trafficking but is not required for membrane translocation, receptor binding, and internalization

Dinh, D. T., Qian, H., Seeber, R., Lim, E., Pfleger, K., Eidne, K. & Thomas, W. G., 2005, In : Molecular Pharmacology. 67, 2, p. 375-382

Research output: Contribution to journal › Article

Membranes

Transport Vesicles

Angiotensin Type 1 Receptor

beta-Arrestins

Energy Transfer

2004

25 Citations (Scopus)

Gonadotropin-Releasing Hormone Receptor-Mediated Growth Suppression of Immortalized LβT2 Gonadotrope and Stable HEK293 Cell Lines

Miles, L. E. C., Hanyaloglu, A. C., Dromey, J., Pfleger, K. & Eidne, K., 2004, In : Endocrinology. 145, 1, p. 194-204

Research output: Contribution to journal › Article

LHRH Receptors

HEK293 Cells

Gonadotropin-Releasing Hormone

Cell Line

Growth

2003

75 Citations (Scopus)

G-protein coupled receptor oligomerization in neuroendocrine pathways

Kroeger, K. M., Pfleger, K. & Eidne, K., 2003, In : Frontiers in Neuroendocrinology. 24, 4, p. 254-278

Research output: Contribution to journal › Article

G-Protein-Coupled Receptors

Biological Phenomena

Drug Design

Dimerization

Pharmacology

36 Citations (Scopus)

New Technologies: Bioluminescence Resonance Energy Transfer (BRET) for the Detection of Real Time Interactions Involving G-Protein Coupled Receptors

Pfleger, K. & Eidne, K. A., 2003, In : Pituitary. 6, 3, p. 141-151

Research output: Contribution to journal › Article

2002

31 Citations (Scopus)

Conformational Constraint of Mammalian, Chicken, and Salmon GnRHs, But Not GnRH II, Enhances Binding at Mammalian and Nonmammalian Receptors: Evidence for Preconfiguration of GnRH II

Pfleger, K., Bogerd, J. & Millar, R. P., 2002, In : Molecular Endocrinology. 16, p. 2155-2162

Research output: Contribution to journal › Article