About: Selective and Dual Targeting of CCR2 and CCR5 Receptors: A Current Overview

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An Entity of Type : schema:ScholarlyArticle, within Data Space : covidontheweb.inria.fr associated with source document(s)

Attributes	Values
type	Academic Article research paper schema:ScholarlyArticle
isDefinedBy	Covid-on-the-Web dataset
has title	Selective and Dual Targeting of CCR2 and CCR5 Receptors: A Current Overview
Creator	Junker, Anna Kokornaczyk, Artur Strunz, Ann Junker, A Kokornaczyk, A Strunz, A Wü, Bernhard Wünsch, B
Source	PMC
abstract	The chemokine receptor 2 (CCR2) and chemokine receptor 5 (CCR5) are important mediators of leukocyte trafficking in inflammatory processes. The emerging evidence for a role of CCR2 and CCR5 receptors in human inflammatory diseases led to a growing interest in CCR2- and CCR5-selective antagonists. In this review, we focus on the recent development of selective CCR2/CCR5 receptor ligands and dual antagonists. Several compounds targeting CCR2, e.g., INCB8761 and MK0812, were developed as promising candidates for clinical trials, but failed to show clinical efficacy as presumed from preclinical models. The role of CCR5 receptors as the second co-receptor for the HIV-host cell fusion led to the development of various CCR5-selective ligands. Maraviroc is the first CCR5-targeting drug for the treatment of HIV-1 infections on the market. The role of CCR5 receptors in the progression of inflammatory processes fueled the use of CCR5 antagonists for the treatment of rheumatoid arthritis. Unfortunately, the use of maraviroc for the treatment of rheumatoid arthritis failed due to its inefficacy. Some of the ligands, e.g., TAK-779 and TAK-652, were also found to be dual antagonists of CCR2 and CCR5 receptors. The fact that CCR2 and CCR5 receptor antagonists contribute to the treatment of inflammatory diseases renders the development of dual antagonists as promising novel therapeutic strategy.
has issue date	2014-03-05(xsd:dateTime)
bibo:doi	10.1007/7355_2014_40
has license	no-cc
sha1sum (hex)	c6c2b70378ceb955eef5dcbb10bd65f91e32c8dd
schema:url	https://doi.org/10.1007/7355_2014_40
resource representing a document's title	Selective and Dual Targeting of CCR2 and CCR5 Receptors: A Current Overview
has PubMed Central identifier	PMC7123309
schema:publication	Chemokines
resource representing a document's body	covid:c6c2b70378ceb955eef5dcbb10bd65f91e32c8dd#body_text
is schema:about of	named entity 'Unfortunately' named entity 'chemokine receptor' named entity 'CCR5' named entity 'MEDIATORS' named entity 'EVIDENCE FOR' named entity 'NOVEL' named entity 'MARAVIROC' named entity 'SELECTIVE' named entity 'receptors' named entity 'CCR5' named entity 'therapeutic' named entity 'antagonists' named entity 'CCR2' named entity 'ligands' named entity 'promising' named entity 'CCR2' named entity 'co-receptor' named entity 'ligands' named entity 'leukocyte' named entity 'chemokine receptor 2' named entity 'CCR2' named entity 'chemokine receptor' named entity 'Maraviroc' named entity 'receptor ligands' named entity 'inflammatory processes' named entity 'preclinical models' named entity 'inflammatory diseases' named entity 'CCR5' named entity 'extracellular region' named entity 'heterocycle' named entity 'ligand binding' named entity 'hydrophobic' named entity 'CCR2' named entity 'binding sites' named entity 'atom' named entity 'adverse effects' named entity 'CCR5' named entity 'primary metabolites' named entity 'trans' named entity 'conformations' named entity 'moiety' named entity 'methyl' named entity 'ligand' named entity 'CCL2' named entity 'co-receptor' named entity 'CCR2' named entity 'CCR2' named entity 'radioligand' named entity 'CCR2' named entity 'atherosclerotic plaque' named entity 'binding sites' named entity 'gene' named entity 'amino acid sequences' named entity 'antiviral activity' named entity 'binding pocket' named entity 'pyridine' named entity 'CCR5' named entity 'CCR2' named entity 'CCR2' named entity 'tropane' named entity 'amino moiety' named entity 'CCR5' named entity 'CCR2' named entity 'lead compound' named entity 'Pfizer' named entity 'CCR5' named entity 'chemokine receptors' named entity 'CYP' named entity 'oxidizable' named entity 'interact' named entity 'oral bioavailability' named entity 'antagonist' named entity 'CCR5' named entity 'CCR5' named entity 'phenylalanine' named entity '4.3'

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