Design Strategies for Bivalent Ligands Targeting GPCRs

Hetero-dimerization of serotonin 5-HT2A and dopamine D2 receptors

(2010) Sylwia Łukasiewicz et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH

Effect of linker substitution on the binding of butorphan univalent and bivalent ligands to opioid receptors

(2010) Brian S. Fulton et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Rational design of dualsteric GPCR ligands: quests and promise

(2010) Klaus Mohr et al.   BRITISH JOURNAL OF PHARMACOLOGY

Hybrid Ortho/Allosteric Ligands for the Adenosine A1Receptor

(2010) Rajeshwar Narlawar et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and Biological Evaluation of Bivalent Ligands for the Cannabinoid 1 Receptor

(2010) Yanan Zhang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Bivalent Ligands of CXCR4 with Rigid Linkers for Elucidation of the Dimerization State in Cells

(2010) Tomohiro Tanaka et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Allosteric modulation of G protein-coupled receptors: A pharmacological perspective

(2010) Peter Keov et al.   NEUROPHARMACOLOGY

Oligoproline helices as structurally defined scaffolds for oligomeric G protein-coupled receptor ligands

(2010) Kimberly M. Bonger et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Formation and dissociation of M1 muscarinic receptor dimers seen by total internal reflection fluorescence imaging of single molecules

(2010) J. A. Hern et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Steroidal bivalent ligands for the estrogen receptor: Design, synthesis, characterization and binding affinities

(2009) Andrew L. LaFrate et al.   BIOORGANIC & MEDICINAL CHEMISTRY

A bivalent ligand (KMN-21) antagonist for μ/κ heterodimeric opioid receptors

(2009) Shijun Zhang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis and Pharmacological Evaluation of Dimeric Follicle-Stimulating Hormone Receptor Antagonists

(2009) Kimberly M. Bonger et al.   ChemMedChem

Discovery of Selective Luteinizing Hormone Receptor Agonists Using the Bivalent Ligand Method

(2009) Kimberly M. Bonger et al.   ChemMedChem

Multivalent-Based Drug Design Applied to Serotonin 5-HT4 Receptor Oligomers

(2009) Frank Lezoualc'h et al.   CURRENT PHARMACEUTICAL DESIGN

Adenosine A2AReceptor-Antagonist/Dopamine D2Receptor-Agonist Bivalent Ligands as Pharmacological Tools to Detect A2A-D2Receptor Heteromers

(2009) Aroa Soriano et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and Opioid Receptor Binding Affinities of 2-Substituted and 3-Aminomorphinans: Ligands for μ, κ, and δ Opioid Receptors

(2009) Michael Decker et al.   JOURNAL OF MEDICINAL CHEMISTRY

Metabotropic glutamate type 5, dopamine D2and adenosine A2areceptors form higher-order oligomers in living cells

(2009) Nuria Cabello et al.   JOURNAL OF NEUROCHEMISTRY

Orthosteric/Allosteric Bitopic Ligands: Going Hybrid at GPCRs

(2009) C. Valant et al.   MOLECULAR INTERVENTIONS

Heterodimerization of dopamine receptors: new insights into functional and therapeutic significance

(2009) Roberto Maggio et al.   PARKINSONISM & RELATED DISORDERS

GPCR homomers and heteromers: A better choice as targets for drug development than GPCR monomers?

(2009) Vicent Casadó et al.   PHARMACOLOGY & THERAPEUTICS

The role of G-proteins in the dimerisation of human somatostatin receptor types 2 and 5

(2009) Michael Grant et al.   REGULATORY PEPTIDES

Synthesis and evaluation of homodimeric GnRHR antagonists having a rigid bis-propargylated benzene core

(2008) Kimberly M. Bonger et al.   BIOORGANIC & MEDICINAL CHEMISTRY

A study of the structure–activity relationship of GABAA–benzodiazepine receptor bivalent ligands by conformational analysis with low temperature NMR and X-ray analysis

(2008) Dongmei Han et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Blood–brain barrier permeability considerations for CNS-targeted compound library design

(2008) Stephen A Hitchcock   CURRENT OPINION IN CHEMICAL BIOLOGY

An Update on Adenosine A2A-Dopamine D2 Receptor Interactions: Implications for the Function of G Protein-Coupled Receptors

(2008) S. Ferre et al.   CURRENT PHARMACEUTICAL DESIGN

A Novel Mechanism of G Protein-coupled Receptor Functional Selectivity

(2008) Celine Valant et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Synthesis of Bivalent β2-Adrenergic and Adenosine A1Receptor Ligands

(2008) Peter Karellas et al.   JOURNAL OF MEDICINAL CHEMISTRY

Induced Association of μ Opioid (MOP) and Type 2 Cholecystokinin (CCK2) Receptors by Novel Bivalent Ligands

(2008) Yaguo Zheng et al.   JOURNAL OF MEDICINAL CHEMISTRY

Detection of heteromerization of more than two proteins by sequential BRET-FRET

(2008) Paulina Carriba et al.   NATURE METHODS

Structural diversity of G protein-coupled receptors and significance for drug discovery

(2008) Malin C. Lagerström et al.   NATURE REVIEWS DRUG DISCOVERY

In Vivo Characterization of (−)(−)MCL-144 and (+)(−)MCL-193: Isomeric, Bivalent Ligands with Mu/Kappa Agonist Properties

(2008) Jennifer L. Mathews et al.   NEUROCHEMICAL RESEARCH

How and why do GPCRs dimerize?

(2008) Vsevolod V. Gurevich et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

The synthesis of bivalent 2β-carbomethoxy-3β-(3,4-dichlorophenyl)-8-heterobicyclo[3.2.1]octanes as probes for proximal binding sites on the dopamine and serotonin transporters

(2007) Peter C. Meltzer et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Dimerization of G protein-coupled receptors: New avenues for somatostatin receptor signalling, control and functioning

(2007) Mario Durán-Prado et al.   MOLECULAR AND CELLULAR ENDOCRINOLOGY