Design strategies for bivalent ligands targeting GPCRs (Q34180510)

31 July 2017

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title

Design strategies for bivalent ligands targeting GPCRs (English)

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G protein-coupled receptor

31 July 2017

main subject

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Jeremy Shonberg

1

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Peter J. Scammells

object named as

Peter J Scammells

series ordinal

2

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author name string

Ben Capuano

series ordinal

3

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31 July 2017

publication date

21 April 2011

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31 July 2017

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31 July 2017

volume

6

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31 July 2017

issue

6

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31 July 2017

page(s)

963-974

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How many drug targets are there?

31 July 2017

cites work

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

The G-protein-coupled receptors in the human genome form five main families. Phylogenetic analysis, paralogon groups, and fingerprints

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Opiate (Enkephalin) Receptors of Neuroblastoma Cells: Occurrence in Clusters on the Cell Surface

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

How and why do GPCRs dimerize?

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Evolution, structure, and activation mechanism of family 3/C G-protein-coupled receptors

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Heterodimerization of g protein-coupled receptors: specificity and functional significance.

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Hetero-oligomerization between GABAA and GABAB receptors regulates GABAB receptor trafficking

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Heterodimerization of alpha 2A- and beta 1-adrenergic receptors

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Homo- and hetero-oligomeric interactions between G-protein-coupled receptors in living cells monitored by two variants of bioluminescence resonance energy transfer (BRET): hetero-oligomers between receptor subtypes form more efficiently than between

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

From models to molecules: opioid receptor dimers, bivalent ligands, and selective opioid receptor probes

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Homodimerization of adenosine A2A receptors: qualitative and quantitative assessment by fluorescence and bioluminescence energy transfer

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Adenosine A2A-dopamine D2 receptor-receptor heteromerization: qualitative and quantitative assessment by fluorescence and bioluminescence energy transfer

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Coaggregation, cointernalization, and codesensitization of adenosine A2A receptors and dopamine D2 receptors

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

An update on adenosine A2A-dopamine D2 receptor interactions: implications for the function of G protein-coupled receptors

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Molecular aspects of muscarinic receptor dimerization

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

D2/D3 dopamine receptor heterodimers exhibit unique functional properties

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Potent activation of dopamine D3/D2 heterodimers by the antiparkinsonian agents, S32504, pramipexole and ropinirole

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Dopamine D1 and D2 receptor Co-activation generates a novel phospholipase C-mediated calcium signal

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Hetero-dimerization of serotonin 5-HT(2A) and dopamine D(2) receptors

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Synthesis and biological evaluation of bivalent ligands for the cannabinoid 1 receptor.

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Metabotropic glutamate type 5, dopamine D2 and adenosine A2a receptors form higher-order oligomers in living cells

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Narcotic antagonistic potency of bivalent ligands which contain beta-naltrexamine. Evidence for bridging between proximal recognition sites

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Opioid agonist and antagonist bivalent ligands. The relationship between spacer length and selectivity at multiple opioid receptors

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Opioid agonist and antagonist bivalent ligands as receptor probes

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

From magic bullets to designed multiple ligands

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Synthesis of specific bivalent probes that functionally interact with 5-HT(4) receptor dimers

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

A bivalent ligand (KDN-21) reveals spinal delta and kappa opioid receptors are organized as heterodimers that give rise to delta(1) and kappa(2) phenotypes. Selective targeting of delta-kappa heterodimers

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Bivalent ligands and the message-address concept in the design of selective opioid receptor antagonists

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Orthosteric/allosteric bitopic ligands: going hybrid at GPCRs.

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Allosteric Modulation of G Protein–Coupled Receptors

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

G protein-coupled receptor allosterism and complexing

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Hybrid ortho/allosteric ligands for the adenosine A(1) receptor

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

A novel mechanism of G protein-coupled receptor functional selectivity. Muscarinic partial agonist McN-A-343 as a bitopic orthosteric/allosteric ligand.

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Allosteric modulation of G protein-coupled receptors: a pharmacological perspective.

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Rational design of dualsteric GPCR ligands: quests and promise

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Receptor dimerization--rationale for the design of bivalent ligands

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Design and synthesis of specific probes for human 5-HT4 receptor dimerization studies

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Adenosine A2A receptor-antagonist/dopamine D2 receptor-agonist bivalent ligands as pharmacological tools to detect A2A-D2 receptor heteromers

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Synthesis and opioid receptor binding affinities of 2-substituted and 3-aminomorphinans: ligands for mu, kappa, and delta opioid receptors

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Induced association of mu opioid (MOP) and type 2 cholecystokinin (CCK2) receptors by novel bivalent ligands

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Synthesis and biological evaluation of 14-alkoxymorphinans. 22.(1) Influence of the 14-alkoxy group and the substitution in position 5 in 14-alkoxymorphinan-6-ones on in vitro and in vivo activities

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Synthesis of bivalent beta2-adrenergic and adenosine A1 receptor ligands

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Comparative pharmacology of human adenosine receptor subtypes - characterization of stably transfected receptors in CHO cells.

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Bivalent ligand approach on 4-[2-(3-methoxyphenyl)ethyl]-1-(2-methoxyphenyl)piperazine: synthesis and binding affinities for 5-HT(7) and 5-HT(1A) receptors.

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Synthesis and biological characterization of 1-methyl-1,2,5,6-tetrahydropyridyl-1,2,5-thiadiazole derivatives as muscarinic agonists for the treatment of neurological disorders

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Adenosine receptors: pharmacology, structure-activity relationships, and therapeutic potential

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Bivalent ligands as specific pharmacological tools for G protein-coupled receptor dimers

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Opioid-induced tolerance and dependence in mice is modulated by the distance between pharmacophores in a bivalent ligand series

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

A bivalent ligand (KMN-21) antagonist for mu/kappa heterodimeric opioid receptors

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

A bivalent ligand (KDAN-18) containing delta-antagonist and kappa-agonist pharmacophores bridges delta2 and kappa1 opioid receptor phenotypes

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Multivalent-based drug design applied to serotonin 5-HT(4) receptor oligomers

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Discovery of selective luteinizing hormone receptor agonists using the bivalent ligand method.

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

The influence of rigid or flexible linkage between two ligands on the effective affinity and avidity for reversible interactions with bivalent receptors.

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Synthesis and evaluation of homo-bivalent GnRHR ligands.

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Synthesis and pharmacological evaluation of dimeric follicle-stimulating hormone receptor antagonists.

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Design, synthesis, and biological characterization of bivalent 1-methyl-1,2,5,6-tetrahydropyridyl-1,2,5-thiadiazole derivatives as selective muscarinic agonists

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

In vivo characterization of (-)(-)MCL-144 and (+)(-)MCL-193: isomeric, bivalent ligands with mu/kappa agonist properties

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Dimerization of sumatriptan as an efficient way to design a potent, centrally and orally active 5-HT1B agonist

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Targeting the brain--surmounting or bypassing the blood-brain barrier

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

The factors that influence permeation across the blood-brain barrier.

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Synthesis and structure-activity relationships of amide and hydrazide analogues of the cannabinoid CB(1) receptor antagonist N-(piperidinyl)- 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (SR141716).

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Synthesis of long-chain amide analogs of the cannabinoid CB1 receptor antagonist N-(piperidinyl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (SR141716) with unique binding selectivities and pharmacological activities

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Serotonin Dimers: Application of the Bivalent Ligand Approach to the Design of New Potent and Selective 5-HT1B/1DAgonists

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Structure of Poly-L-Proline

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

Metabotropic glutamate receptor 5 is a disulfide-linked dimer

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

7 January 2021

Detection of beta 2-adrenergic receptor dimerization in living cells using bioluminescence resonance energy transfer (BRET)

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

7 January 2021

Dimers of 5HT1 ligands preferentially bind to 5HT1B/1D receptor subtypes

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

7 January 2021

Development of 1,4-benzodiazepine cholecystokinin type B antagonists

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

7 January 2021

Fluorescent probes for dopamine receptors: synthesis and characterization of fluorescein and 7-nitrobenz-2-oxa-1,3-diazol-4-yl conjugates of D-1 and D-2 receptor ligands

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

7 January 2021

New esters of 4-amino-5-chloro-2-methoxybenzoic acid as potent agonists and antagonists for 5-HT4 receptors

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

7 January 2021

Bivalent ligands of CXCR4 with rigid linkers for elucidation of the dimerization state in cells

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

7 January 2021

Carrier-mediated or specialized transport of drugs across the blood-brain barrier

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201100101

7 January 2021

Identifiers

DOI

10.1002/CMDC.201100101

1 reference

31 July 2017

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