• 12119 Citations
  • 56 Scopus h-Index
1977 …2019
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Research Output 1977 2019

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Article
2019

Characterization of farnesyl diphosphate farnesyl transferase 1 expression in cancer

Tüzmen, Ş., Hostetter, G., Watanabe, A., Ekmekçi, C., Carrigan, P. E., Shechter, I., Kallioniemi, O., Miller, L. J. & Mousses, S., Jan 1 2019, In : Personalized Medicine. 16, 1, p. 51-65 15 p.

Research output: Contribution to journalArticle

Transferases
Neoplasms
Cholesterol
Enzymes
Metabolic Networks and Pathways

Molecular Basis of Action of a Small-Molecule Positive Allosteric Modulator Agonist at the Type 1 Cholecystokinin Holoreceptor

Desai, A. J., Mechin, I., Nagarajan, K., Valant, C., Wootten, D., Lam, P. C. H., Orry, A., Abagyan, R., Nair, A., Sexton, P. M., Christopoulos, A. & Miller, L. J., Mar 1 2019, In : Molecular Pharmacology. 95, 3, p. 245-259 15 p.

Research output: Contribution to journalArticle

Cholecystokinin
Structure-Activity Relationship
Cholecystokinin Receptors
Peptides
Structural Models
2018
25 Citations (Scopus)

Cryo-EM structure of the active, Gs-protein complexed, human CGRP receptor

Liang, Y. L., Khoshouei, M., Deganutti, G., Glukhova, A., Koole, C., Peat, T. S., Radjainia, M., Plitzko, J. M., Baumeister, W., Miller, L. J., Hay, D. L., Christopoulos, A., Reynolds, C. A., Wootten, D. & Sexton, P. M., Sep 27 2018, In : Nature. 561, 7724, p. 492-497 6 p.

Research output: Contribution to journalArticle

Calcitonin Receptor-Like Protein
Calcitonin Gene-Related Peptide Receptors
Receptor Activity-Modifying Protein 1
Calcitonin Gene-Related Peptide
G-Protein-Coupled Receptors
71 Citations (Scopus)

Phase-plate cryo-EM structure of a biased agonistbound human GLP-1 receptor-Gs complex

Liang, Y. L., Khoshouei, M., Glukhova, A., Furness, S. G. B., Zhao, P., Clydesdale, L., Koole, C., Truong, T. T., Thal, D. M., Lei, S., Radjainia, M., Danev, R., Baumeister, W., Wang, M. W., Miller, L. J., Christopoulos, A., Sexton, P. M. & Wootten, D., Mar 1 2018, In : Nature. 555, 7694, p. 121-125 5 p.

Research output: Contribution to journalArticle

Glucagon-Like Peptide 1
GTP-Binding Proteins
Peptides
G-Protein-Coupled Receptors
Type 2 Diabetes Mellitus
2017
7 Citations (Scopus)

Cholecystokinin responsiveness varies across the population dependent on metabolic phenotype

Desai, A. J., Dong, M., Langlais, B. T., Dueck, A. & Miller, L. J., Aug 1 2017, In : American Journal of Clinical Nutrition. 106, 2, p. 447-456 10 p.

Research output: Contribution to journalArticle

Cholecystokinin
Phenotype
Population
Obesity
Cholesterol
3 Citations (Scopus)

Coexpressed class B G protein-coupled secretin and GLP-1 receptors self-and cross-associate: Impact on pancreatic islets

Harikumar, K. G., Lau, S., Sexton, P. M., Wootten, D. & Miller, L. J., Jun 1 2017, In : Endocrinology. 158, 6, p. 1685-1700 16 p.

Research output: Contribution to journalArticle

Secretin
Peptide Receptors
Islets of Langerhans
GTP-Binding Proteins
Calcium
11 Citations (Scopus)

Dimerization of the transmembrane domain of amyloid precursor protein is determined by residues around the γ-secretase cleavage sites

Yan, Y., Xu, T. H., Harikumar, K. G., Miller, L. J., Melcher, K. & Xu, H. E., Sep 22 2017, In : Journal of Biological Chemistry. 292, 38, p. 15826-15837 12 p.

Research output: Contribution to journalArticle

Amyloid Precursor Protein Secretases
Dimerization
Amyloid beta-Protein Precursor
Assays
Membranes
170 Citations (Scopus)

Phase-plate cryo-EM structure of a class B GPCR-G-protein complex

Liang, Y. L., Khoshouei, M., Radjainia, M., Zhang, Y., Glukhova, A., Tarrasch, J., Thal, D. M., Furness, S. G. B., Christopoulos, G., Coudrat, T., Danev, R., Baumeister, W., Miller, L. J., Christopoulos, A., Kobilka, B. K., Wootten, D., Skiniotis, G. & Sexton, P. M., Jun 1 2017, In : Nature. 546, 7656, p. 118-123 6 p.

Research output: Contribution to journalArticle

G-Protein-Coupled Receptors
GTP-Binding Proteins
Calcitonin Receptors
Cryoelectron Microscopy
Peptides
10 Citations (Scopus)

Spatial intensity distribution analysis quantifies the extent and regulation of homodimerization of the secretin receptor

Ward, R. J., Pediani, J. D., Harikumar, K. G., Miller, L. J. & Milligan, G., Jun 1 2017, In : Biochemical Journal. 474, 11, p. 1879-1895 17 p.

Research output: Contribution to journalArticle

Secretin
Dimerization
Cell membranes
GTP-Binding Proteins
Receptor-Interacting Protein Serine-Threonine Kinases
21 Citations (Scopus)

Spirohexene-Tetrazine Ligation Enables Bioorthogonal Labeling of Class B G Protein-Coupled Receptors in Live Cells

Ramil, C. P., Dong, M., An, P., Lewandowski, T. M., Yu, Z., Miller, L. J. & Lin, Q., Sep 27 2017, In : Journal of the American Chemical Society. 139, 38, p. 13376-13386 11 p.

Research output: Contribution to journalArticle

G-Protein-Coupled Receptors
Labeling
Ligation
Emitter coupled logic circuits
Ligands
124 Citations (Scopus)

THE CONCISE GUIDE TO PHARMACOLOGY 2017/18: Overview

CGTP Collaborators, Dec 1 2017, In : British Journal of Pharmacology. 174, p. S1-S16

Research output: Contribution to journalArticle

Terminology
Pharmacology
Ion Channels
Pharmaceutical Preparations
Ligands
19 Citations (Scopus)

Wnt5a promotes Frizzled-4 signalosome assembly by stabilizing cysteine-rich domain dimerization

DeBruine, Z. J., Ke, J., Harikumar, K. G., Gu, X., Borowsky, P., Williams, B. O., Xu, W., Miller, L. J., Xu, H. E. & Melcher, K., 2017, In : Genes and Development. 31, 9, p. 916-926 11 p.

Research output: Contribution to journalArticle

Dimerization
Cysteine
Frizzled Receptors
Low Density Lipoprotein Receptor-Related Protein-6
Low Density Lipoprotein Receptor-Related Protein-5
2016
25 Citations (Scopus)

A hydrogen-bonded polar network in the core of the glucagon-like peptide-1 receptor is a fulcrum for biased agonism: Lessons from class B crystal structuress

Wootten, D., Reynolds, C. A., Koole, C., Smith, K. J., Mobarec, J. C., Simms, J., Quon, T., Coudrat, T., Furness, S. G. B., Miller, L. J., Christopoulos, A. & Sexton, P. M., Mar 1 2016, In : Molecular Pharmacology. 89, 3, p. 335-347 13 p.

Research output: Contribution to journalArticle

Hydrogen
Peptides
Oxyntomodulin
Calcium
Corticotropin-Releasing Hormone Receptors
59 Citations (Scopus)

Glucagon-like peptide-1 and its class B G protein-coupled receptors: A long march to therapeutic successes

de Graaf, C., Donnelly, D., Wootten, D., Lau, J., Sexton, P. M., Miller, L. J., Ahn, J. M., Liao, J., Fletcher, M. M., Yang, D., Brown, A. J. H., Zhou, C., Deng, J. & Wang, M. W., Oct 1 2016, In : Pharmacological Reviews. 68, 4, p. 954-1013 60 p.

Research output: Contribution to journalArticle

Glucagon-Like Peptide 1
G-Protein-Coupled Receptors
Ligands
Enteroendocrine Cells
Pharmacology
15 Citations (Scopus)

Key interactions by conserved polar amino acids located at the transmembrane helical boundaries in Class B GPCRs modulate activation, effector specificity and biased signalling in the glucagon-like peptide-1 receptor

Wootten, D., Reynolds, C. A., Smith, K. J., Mobarec, J. C., Furness, S. G. B., Miller, L. J., Christopoulos, A. & Sexton, P. M., Oct 15 2016, In : Biochemical Pharmacology. 118, p. 68-87 20 p.

Research output: Contribution to journalArticle

Chemical activation
Amino Acids
Ligands
Molecular Models
Cytoplasmic and Nuclear Receptors
12 Citations (Scopus)

Metabolic Actions of the Type 1 Cholecystokinin Receptor: Its Potential as a Therapeutic Target

Miller, L. J. & Desai, A. J., 2016, (Accepted/In press) In : Trends in Endocrinology and Metabolism.

Research output: Contribution to journalArticle

Cholecystokinin Receptors
Obesity
Cholecystokinin
Appetite
Drug Combinations

Signaling modification by GPCR heteromer and its implication on X-linked nephrogenic diabetes insipidus

Ng, H. K. H., Harikumar, K. G., Miller, L. J. & Chow, B. K. C., Sep 1 2016, In : PLoS One. 11, 9, e0163086.

Research output: Contribution to journalArticle

diabetes insipidus
Nephrogenic Diabetes Insipidus
Medical problems
secretin
Secretin
4 Citations (Scopus)

Structure and function of Cross-class complexes of G Protein-Coupled secretin and angiotensin 1a receptors

Harikumar, K. G., Augustine, M. L., Lee, L. T. O., Chow, B. K. C. & Miller, L. J., Aug 12 2016, In : Journal of Biological Chemistry. 291, 33, p. 17332-17344 13 p.

Research output: Contribution to journalArticle

Angiotensin Receptors
Secretin
Angiotensins
GTP-Binding Proteins
Calcium
48 Citations (Scopus)

The Extracellular Surface of the GLP-1 Receptor Is a Molecular Trigger for Biased Agonism

Wootten, D., Reynolds, C. A., Smith, K. J., Mobarec, J. C., Koole, C., Savage, E. E., Pabreja, K., Simms, J., Sridhar, R., Furness, S. G. B., Liu, M., Thompson, P. E., Miller, L. J., Christopoulos, A. & Sexton, P. M., Jun 16 2016, In : Cell. 165, 7, p. 1632-1643 12 p.

Research output: Contribution to journalArticle

Ligands
Peptides
Chemical activation
G-Protein-Coupled Receptors
Glucagon-Like Peptide-1 Receptor
5 Citations (Scopus)

Use of cysteine trapping to map spatial approximations between residues contributing to the helix N-capping motif of secretin and distinct residues within each of the extracellular loops of its receptor

Dong, M., Lam, P. C. H., Orry, A., Sexton, P. M., Christopoulos, A., Abagyan, R. & Miller, L. J., Mar 4 2016, In : Journal of Biological Chemistry. 291, 10, p. 5172-5184 13 p.

Research output: Contribution to journalArticle

Secretin
Cysteine
Labeling
Peptides
Mutagenesis
2015
9 Citations (Scopus)

Beneficial effects of β-sitosterol on type 1 cholecystokinin receptor dysfunction induced by elevated membrane cholesterol

Desai, A. J., Dong, M. & Miller, L. J., Sep 10 2015, (Accepted/In press) In : Clinical Nutrition.

Research output: Contribution to journalArticle

Cholecystokinin Receptors
Hypercholesterolemia
Cholesterol
Membranes
Phytosterols
7 Citations (Scopus)

Development of a highly selective allosteric antagonist radioligand for the type 1 cholecystokinin receptor and elucidation of its molecular basis of binding

Dong, M., Vattelana, A. M., Lam, P. C. H., Orry, A. J., Abagyan, R., Christopoulos, A., Sexton, P. M., Haines, D. R. & Miller, L. J., Jan 1 2015, In : Molecular Pharmacology. 87, 1, p. 130-140 11 p.

Research output: Contribution to journalArticle

Cholecystokinin Receptors
Cholecystokinin B Receptor
Molecular Models
Drug Design
Propionates
10 Citations (Scopus)

Differential impact of amino acid substitutions on critical residues of the human glucagon-like peptide-1 receptor involved in peptide activity and small-molecule allosterys

Koole, C., Wootten, D., Simms, J., Miller, L. J., Christopoulos, A. & Sexton, P. M., Apr 1 2015, In : Journal of Pharmacology and Experimental Therapeutics. 353, 1, p. 52-63 12 p.

Research output: Contribution to journalArticle

Amino Acid Substitution
Peptides
Glucagon-Like Peptide 1
Oxyntomodulin
Amino Acids
7 Citations (Scopus)
Cholecystokinin Receptors
Cholecystokinin
Modulators
Structure-Activity Relationship
Benzodiazepines
7 Citations (Scopus)
Ursodeoxycholic Acid
Binding Sites
Cholesterol
Cholecystokinin Receptors
Bile Acids and Salts
9 Citations (Scopus)

Molecular Mechanism of Action of Triazolobenzodiazepinone Agonists of the Type 1 Cholecystokinin Receptor. Possible Cooperativity across the Receptor Homodimeric Complex

Desai, A. J., Lam, P. C. H., Orry, A., Abagyan, R., Christopoulos, A., Sexton, P. M. & Miller, L. J., Dec 24 2015, In : Journal of Medicinal Chemistry. 58, 24, p. 9562-9577 16 p.

Research output: Contribution to journalArticle

Cholecystokinin Receptors
Ligands
Benzodiazepines
Gallbladder
Pharmaceutical Preparations

Use of fluorescence indicators in receptor ligands

Harikumar, K. G. & Miller, L. J., 2015, In : Methods in Molecular Biology. 1335, p. 115-130 16 p.

Research output: Contribution to journalArticle

Fluorescence
Ligands
Peptides
Fluorescence Polarization
G-Protein-Coupled Receptors
2014
11 Citations (Scopus)

A type 1 cholecystokinin receptor mutant that mimics the dysfunction observed for wild type receptor in a high cholesterol environment

Desai, A. J., Harikumar, K. G. & Miller, L. J., Jun 27 2014, In : Journal of Biological Chemistry. 289, 26, p. 18314-18326 13 p.

Research output: Contribution to journalArticle

Cholecystokinin A Receptor
Cholecystokinin Receptors
Cholecystokinin
Cholesterol
Ligands
17 Citations (Scopus)

Structural and functional insights into the juxtamembranous amino-terminal tail and extracellular loop regions of class B GPCRs

Dong, M., Koole, C., Wootten, D., Sexton, P. M. & Miller, L. J., 2014, In : British Journal of Pharmacology. 171, 5, p. 1085-1101 17 p.

Research output: Contribution to journalArticle

Ligands
Heterotrimeric GTP-Binding Proteins
Spatial Analysis
Guanine Nucleotides
Mutagenesis
28 Citations (Scopus)

Transmembrane peptides as unique tools to demonstrate the in vivo action of a cross-class GPCR heterocomplex

Lee, L. T. O., Ng, S. Y. L., Chu, J. Y. S., Sekar, R., Harikumar, K. G., Miller, L. J. & Chow, B. K. C., 2014, In : FASEB Journal. 28, 6, p. 2632-2644 13 p.

Research output: Contribution to journalArticle

Secretin
Angiotensins
Peptide Receptors
Cyclic AMP
Peptides
2013
3 Citations (Scopus)
Cholecystokinin B Receptor
Cholecystokinin
Labeling
Demonstrations
Cholecystokinin Receptors
2 Citations (Scopus)

Insights into the impact of phenolic residue incorporation at each position along secretin for receptor binding and biological activity

Dong, M., Pinon, D. I. & Miller, L. J., Jan 2013, In : Regulatory Peptides. 180, 1, p. 5-11 7 p.

Research output: Contribution to journalArticle

Bioactivity
Alanine
Ligands
Peptides
Secretin
14 Citations (Scopus)

Krüppel-like factor 11 regulates the expression of metabolic genes via an evolutionarily conserved protein interaction domain functionally disrupted in maturity onset diabetes of the young

Lomberk, G., Grzenda, A., Mathison, A., Escande, C., Zhang, J. S., Calvo, E., Miller, L. J., Iovanna, J., Chini, E. N., Fernandez-Zapico, M. E. & Urrutia, R., Jun 14 2013, In : Journal of Biological Chemistry. 288, 24, p. 17745-17758 14 p.

Research output: Contribution to journalArticle

Protein Interaction Domains and Motifs
Medical problems
Genes
Gene Expression
Metabolic Networks and Pathways
12 Citations (Scopus)

Membrane cholesterol affects stimulus-activity coupling in type 1, but not type 2, CCK receptors: Use of cell lines with elevated cholesterol

Harikumar, K. G., Potter, R. M., Patil, A., Echeveste, V. & Miller, L. J., Mar 2013, In : Lipids. 48, 3, p. 231-244 14 p.

Research output: Contribution to journalArticle

Cholecystokinin B Receptor
Hypercholesterolemia
Cholesterol
Cells
Membranes
23 Citations (Scopus)

Minireview: Signal bias, allosterism, and polymorphic variation at the GLP-1R: Implications for drug discovery

Koole, C., Savage, E. E., Christopoulos, A., Miller, L. J., Sexton, P. M. & Wootten, D., Aug 1 2013, In : Molecular Endocrinology. 27, 8, p. 1234-1244 11 p.

Research output: Contribution to journalArticle

Drug Discovery
Insulin
Single Nucleotide Polymorphism
Ligands
Incretins
11 Citations (Scopus)

Molecular basis for benzodiazepine agonist action at the type 1 cholecystokinin receptor

Harikumar, K. G., Cawston, E. E., Lam, P. C. H., Patil, A., Orry, A., Henke, B. R., Abagyan, R., Christopoulos, A., Sexton, P. M. & Miller, L. J., Jul 19 2013, In : Journal of Biological Chemistry. 288, 29, p. 21082-21095 14 p.

Research output: Contribution to journalArticle

Cholecystokinin Receptors
Molecular Models
Benzodiazepines
Ligands
Molecules

Molecular basis of peptide activation of the GLP-1 receptor

Miller, L. J., Apr 2013, In : Molecular Metabolism. 2, 2, p. 60-61 2 p.

Research output: Contribution to journalArticle

Peptides
Glucagon-Like Peptide-1 Receptor
90 Citations (Scopus)

Polar transmembrane interactions drive formation of ligand-specific and signal pathway-biased family B G protein-coupled receptor conformations

Wootten, D., Simms, J., Miller, L. J., Christopoulos, A. & Sexton, P. M., Mar 26 2013, In : Proceedings of the National Academy of Sciences of the United States of America. 110, 13, p. 5211-5216 6 p.

Research output: Contribution to journalArticle

G-Protein-Coupled Receptors
Signal Transduction
Ligands
Oxyntomodulin
Glucagon-Like Peptide 1
44 Citations (Scopus)

Recent advances in understanding GLP-1R (glucagon-like peptide-1 receptor) function

Koole, C., Pabreja, K., Savage, E. E., Wootten, D., Furness, S. G. B., Miller, L. J., Christopoulos, A. & Sexton, P. M., Feb 2013, In : Biochemical Society Transactions. 41, 1, p. 172-179 8 p.

Research output: Contribution to journalArticle

Medical problems
Insulin
Type 2 Diabetes Mellitus
Incretins
Glucagon-Like Peptide 1
23 Citations (Scopus)

Receptor activity-modifying protein-dependent impairment of calcitonin receptor splice variant Δ(1-47)hCT(a) function

Qi, T., Dong, M., Watkins, H. A., Wootten, D., Miller, L. J. & Hay, D. L., Feb 2013, In : British Journal of Pharmacology. 168, 3, p. 644-657 14 p.

Research output: Contribution to journalArticle

Receptor Activity-Modifying Proteins
Calcitonin Receptors
Islet Amyloid Polypeptide Receptor
Pharmacology
Peptides
41 Citations (Scopus)

Structure and function of Norrin in assembly and activation of a Frizzled 4-Lrp5/6 complex

Ke, J., Harikumar, K. G., Erice, C., Chen, C., Gu, X., Wang, L., Parker, N., Cheng, Z., Xu, W., Williams, B. O., Melcher, K., Miller, L. J. & Eric Xu, H., Nov 1 2013, In : Genes and Development. 27, 21, p. 2305-2319 15 p.

Research output: Contribution to journalArticle

LDL-Receptor Related Proteins
Frizzled Receptors
Ligands
Cystine
Dimerization
3 Citations (Scopus)

The orthosteric agonist-binding pocket in the prototypic class B G-protein-coupled secretin receptor

Miller, L. J. & Dong, M., Feb 2013, In : Biochemical Society Transactions. 41, 1, p. 154-158 5 p.

Research output: Contribution to journalArticle

Mutagenesis
Molecular modeling
G-Protein-Coupled Receptors
GTP-Binding Proteins
Protein Binding
2012
16 Citations (Scopus)
GTP-Binding Proteins
Calcium
Mutation
Secretin
Leucine
27 Citations (Scopus)

Differential sensitivity of types 1 and 2 cholecystokinin receptors to membrane cholesterol

Potter, R. M., Harikumar, K. G., Wu, S. V. & Miller, L. J., Jan 2012, In : Journal of Lipid Research. 53, 1, p. 137-148 12 p.

Research output: Contribution to journalArticle

Cholecystokinin B Receptor
Cholesterol
Membranes
G-Protein-Coupled Receptors
Bearings (structural)
38 Citations (Scopus)

Glucagon-like peptide-1 receptor dimerization differentially regulates agonist signaling but does not affect small molecule allostery

Harikumar, K. G., Wootten, D., Pinon, D. I., Koole, C., Ball, A. M., Furness, S. G. B., Graham, B., Dong, M., Christopoulos, A., Miller, L. J. & Sexton, P. M., Nov 6 2012, In : Proceedings of the National Academy of Sciences of the United States of America. 109, 45, p. 18607-18612 6 p.

Research output: Contribution to journalArticle

Dimerization
Peptides
Phosphorylation
Ligands
Glucagon-Like Peptide 1
11 Citations (Scopus)

Ligand binding and activation of the secretin receptor, a prototypic family B G protein-coupled receptor

Miller, L. J., Dong, M. & Harikumar, K. G., May 2012, In : British Journal of Pharmacology. 166, 1, p. 18-26 9 p.

Research output: Contribution to journalArticle

G-Protein-Coupled Receptors
Ligands
Peptides
Secretin
Peptide Receptors
2 Citations (Scopus)
Cholecystokinin Receptors
Cholecystokinin
Ligands
Peptides
Arrestin
23 Citations (Scopus)

Mapping spatial approximations between the amino terminus of secretin and each of the extracellular loops of its receptor using cysteine trapping

Dong, M., Xu, X., Ball, A. M., Makhoul, J. A., Lam, P. C. H., Pinon, D. I., Orry, A., Sexton, P. M., Abagyan, R. & Miller, L. J., Dec 2012, In : FASEB Journal. 26, 12, p. 5092-5105 14 p.

Research output: Contribution to journalArticle

Secretin
Cysteine
Ligands
Disulfides
Mutagenesis
13 Citations (Scopus)

Modulation of β-catenin signaling by glucagon receptor activation

Ke, J., Zhang, C., Harikumar, K. G., Zylstra-Diegel, C. R., Wang, L., Mowry, L. E., Miller, L. J., Williams, B. O. & Xu, H. E., Mar 16 2012, In : PLoS One. 7, 3, e33676.

Research output: Contribution to journalArticle

Glucagon Receptors
Low Density Lipoprotein Receptor-Related Protein-5
Catenins
Glucagon
Chemical activation
14 Citations (Scopus)

Molecular basis for binding and subtype selectivity of 1,4-benzodiazepine antagonist ligands of the cholecystokinin receptor

Cawston, E. E., Lam, P. C. H., Harikumar, K. G., Dong, M., Ball, A. M., Augustine, M. L., Akgün, E., Portoghese, P. S., Orry, A., Abagyan, R., Sexton, P. M. & Miller, L. J., May 25 2012, In : Journal of Biological Chemistry. 287, 22, p. 18618-18635 18 p.

Research output: Contribution to journalArticle

Cholecystokinin Receptors
Ligands
Benzodiazepines
Stereochemistry
Cholecystokinin B Receptor