New concepts in drug discovery: collateral efficacy and permissive antagonism (Q36303814)

13 August 2017

1 reference

title

New concepts in drug discovery: collateral efficacy and permissive antagonism (English)

1 reference

13 August 2017

1 reference

Terry Kenakin

1

1 reference

13 August 2017

1 November 2005

1 reference

Nature Reviews Drug Discovery

13 August 2017

1 reference

13 August 2017

4

1 reference

13 August 2017

11

1 reference

13 August 2017

919-927

1 reference

https://scigraph.springernature.com/pub.10.1038/nrd1875

13 August 2017

0 references

cites work

Efficacy at G-protein-coupled receptors

1 reference

G protein-coupled receptor interacting proteins: emerging roles in localization and signal transduction

21 January 2018

1 reference

G-protein-coupled receptor oligomerization and its potential for drug discovery

21 January 2018

1 reference

Aminooxypentane-RANTES induces CCR5 internalization but inhibits recycling: a novel inhibitory mechanism of HIV infectivity

21 January 2018

1 reference

Regulation of G protein-coupled receptor kinases and arrestins during receptor desensitization

21 January 2018

1 reference

Activation-independent parathyroid hormone receptor internalization is regulated by NHERF1 (EBP50).

21 January 2018

1 reference

Agonist-induced phosphorylation of the angiotensin II (AT(1A)) receptor requires generation of a conformation that is distinct from the inositol phosphate-signaling state

21 January 2018

1 reference

Signal transduction by calcitonin Multiple ligands, receptors, and signaling pathways.

21 January 2018

1 reference

Agonist-receptor efficacy. II. Agonist trafficking of receptor signals

21 January 2018

1 reference

The use of stimulus-biased assay systems to detect agonist-specific receptor active states: implications for the trafficking of receptor stimulus by agonists.

21 January 2018

1 reference

Ligand-selective receptor conformations revisited: the promise and the problem

21 January 2018

1 reference

Drug efficacy at G protein-coupled receptors

21 January 2018

1 reference

The ligand paradox between affinity and efficacy: can you be there and not make a difference?

21 January 2018

1 reference

A FlAsH-based FRET approach to determine G protein-coupled receptor activation in living cells

21 January 2018

1 reference

Real-time monitoring of receptor and G-protein interactions in living cells.

21 January 2018

1 reference

HIV-1 Entry Cofactor: Functional cDNA Cloning of a Seven-Transmembrane, G Protein-Coupled Receptor

21 January 2018

1 reference

Identification of allosteric peptide agonists of CXCR4.

21 January 2018

1 reference

Defects of B-cell lymphopoiesis and bone-marrow myelopoiesis in mice lacking the CXC chemokine PBSF/SDF-1

21 January 2018

1 reference

The chemokine receptor CXCR4 is essential for vascularization of the gastrointestinal tract

21 January 2018

1 reference

Function of the chemokine receptor CXCR4 in haematopoiesis and in cerebellar development

21 January 2018

1 reference

Antiviral activity and safety of 873140, a novel CCR5 antagonist, during short-term monotherapy in HIV-infected adults

21 January 2018

1 reference

The CCR5 receptor-based mechanism of action of 873140, a potent allosteric noncompetitive HIV entry inhibitor

21 January 2018

1 reference

Spirodiketopiperazine-based CCR5 inhibitor which preserves CC-chemokine/CCR5 interactions and exerts potent activity against R5 human immunodeficiency virus type 1 in vitro

21 January 2018

1 reference

Analysis of the mechanism by which the small-molecule CCR5 antagonists SCH-351125 and SCH-350581 inhibit human immunodeficiency virus type 1 entry.

21 January 2018

1 reference

Interaction of chemokine receptor CCR5 with its ligands: multiple domains for HIV-1 gp120 binding and a single domain for chemokine binding

21 January 2018

1 reference

The core domain of chemokines binds CCR5 extracellular domains while their amino terminus interacts with the transmembrane helix bundle

21 January 2018

1 reference

The HIV-1 Envelope Glycoproteins: Fusogens, Antigens, and Immunogens

21 January 2018

1 reference

gp120: Biologic aspects of structural features

21 January 2018

1 reference

HIV-1 escape from a small molecule, CCR5-specific entry inhibitor does not involve CXCR4 use

21 January 2018

1 reference

Genetic and phenotypic analyses of human immunodeficiency virus type 1 escape from a small-molecule CCR5 inhibitor

21 January 2018

1 reference

HIV-1 coreceptor activity of CCR5 and its inhibition by chemokines: independence from G protein signaling and importance of coreceptor downmodulation.

21 January 2018

1 reference

Endocytosis and recycling of the HIV coreceptor CCR5

21 January 2018

1 reference

Agonist-induced endocytosis of CC chemokine receptor 5 is clathrin dependent.

21 January 2018

1 reference

Spontaneous and antigen-induced production of HIV-inhibitory beta-chemokines are associated with AIDS-free status

21 January 2018

1 reference

Production of beta-chemokines in human immunodeficiency virus (HIV) infection: evidence that high levels of macrophage inflammatory protein-1beta are associated with a decreased risk of HIV disease progression

21 January 2018

1 reference

A small molecule antagonist of chemokine receptors CCR1 and CCR3. Potent inhibition of eosinophil function and CCR3-mediated HIV-1 entry.

21 January 2018

1 reference

The cholinergic hypothesis of geriatric memory dysfunction

21 January 2018

1 reference

Interfacial inhibition of macromolecular interactions: nature's paradigm for drug discovery

21 January 2018

1 reference

Rapid structure-activity and selectivity analysis of kinase inhibitors by BioMAP analysis in complex human primary cell-based models

21 January 2018

1 reference

An integrative biology approach for analysis of drug action in models of human vascular inflammation

21 January 2018

1 reference

31 March 2020

Identifiers

DOI

10.1038/NRD1875

1 reference

13 August 2017

1 reference

PubMed ID

16264435