Proteins > C-C chemokine receptor type 5
Page last updated: 2024-08-07 16:48:36
C-C chemokine receptor type 5
A C-C chemokine receptor type 5 that is encoded in the genome of human. [PRO:WCB, UniProtKB:P51681]
Synonyms
C-C CKR-5;
CC-CKR-5;
CCR-5;
CCR5;
CHEMR13;
HIV-1 fusion coreceptor
Research
Bioassay Publications (37)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 15 (40.54) | 29.6817 |
2010's | 19 (51.35) | 24.3611 |
2020's | 3 (8.11) | 2.80 |
Compounds (23)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
1,10-phenanthroline | Homo sapiens (human) | EC50 | 4.9559 | 1 | 2 |
2,2'-dipyridyl | Homo sapiens (human) | EC50 | 19.4763 | 1 | 2 |
4,4'-dimethyl-2,2'-bipyridine | Homo sapiens (human) | EC50 | 11.7946 | 1 | 2 |
5,5'-dimethyl-2,2'-bipyridyl | Homo sapiens (human) | EC50 | 2.4059 | 1 | 2 |
neocuproine | Homo sapiens (human) | EC50 | 65.0478 | 1 | 2 |
2,2',2''-terpyridine | Homo sapiens (human) | EC50 | 30.3114 | 1 | 2 |
5-methyl-1,10-phenanthroline | Homo sapiens (human) | EC50 | 1,000.0000 | 1 | 2 |
3,4,7,8-tetramethyl-1,10-phenanthroline | Homo sapiens (human) | EC50 | 1.0000 | 1 | 2 |
tak 779 | Homo sapiens (human) | EC50 | 0.0070 | 1 | 1 |
aplaviroc | Homo sapiens (human) | Kd | 0.0030 | 1 | 1 |
maraviroc | Homo sapiens (human) | EC50 | 0.0180 | 1 | 1 |
maraviroc | Homo sapiens (human) | Kd | 0.0250 | 1 | 1 |
Drugs with Other Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
maraviroc | Homo sapiens (human) | IC90 | 0.0100 | 1 | 1 |
Synthesis and Pharmacological Evaluation of Triazolopyrimidinone Derivatives as Noncompetitive, Intracellular Antagonists for CC Chemokine Receptors 2 and 5.Journal of medicinal chemistry, , 12-26, Volume: 62, Issue:24, 2019
Synthesis and biological evaluation of chemokine receptor ligands with 2-benzazepine scaffold.European journal of medicinal chemistry, , Jul-28, Volume: 135, 2017
Chemokine receptor antagonists.Journal of medicinal chemistry, , Nov-26, Volume: 55, Issue:22, 2012
The natural product CCR5 antagonist anibamine and its analogs as anti-prostate cancer agents.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 21, Issue:18, 2011
Design, synthesis, and structure-activity relationship of novel CCR2 antagonists.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 19, Issue:6, 2009
Highly potent and orally active CCR5 antagonists as anti-HIV-1 agents: synthesis and biological activities of 1-benzazocine derivatives containing a sulfoxide moiety.Journal of medicinal chemistry, , Mar-23, Volume: 49, Issue:6, 2006
Inhibition of protein-protein association by small molecules: approaches and progress.Journal of medicinal chemistry, , Apr-11, Volume: 45, Issue:8, 2002
Discovery of novel, potent, and selective small-molecule CCR5 antagonists as anti-HIV-1 agents: synthesis and biological evaluation of anilide derivatives with a quaternary ammonium moiety.Journal of medicinal chemistry, , May-18, Volume: 43, Issue:10, 2000
CCR2B receptor antagonists: conversion of a weak HTS hit to a potent lead compound.Bioorganic & medicinal chemistry letters, , Aug-21, Volume: 10, Issue:16, 2000
Structure-Based Design of Tropane Derivatives as a Novel Series of CCR5 Antagonists with Broad-Spectrum Anti-HIV-1 Activities and Improved Oral Bioavailability.Journal of medicinal chemistry, , 12-22, Volume: 65, Issue:24, 2022
Structure-Based Design and Development of Chemical Probes Targeting Putative MOR-CCR5 Heterodimers to Inhibit Opioid Exacerbated HIV-1 Infectivity.Journal of medicinal chemistry, , 06-10, Volume: 64, Issue:11, 2021
A "Two-Birds-One-Stone" Approach toward the Design of Bifunctional Human Immunodeficiency Virus Type 1 Entry Inhibitors Targeting the CCR5 Coreceptor and gp41 N-Terminal Heptad Repeat Region.Journal of medicinal chemistry, , 08-12, Volume: 64, Issue:15, 2021
Structure-Based Design of 1-Heteroaryl-1,3-propanediamine Derivatives as a Novel Series of CC-Chemokine Receptor 5 Antagonists.Journal of medicinal chemistry, , 11-08, Volume: 61, Issue:21, 2018
Design, synthesis and biological evaluation of (E)-3,4-dihydroxystyryl 4-acylaminophenethyl sulfone, sulfoxide derivatives as dual inhibitors of HIV-1 CCR5 and integrase.Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017
Exploration of bivalent ligands targeting putative mu opioid receptor and chemokine receptor CCR5 dimerization.Bioorganic & medicinal chemistry, , 11-15, Volume: 24, Issue:22, 2016
Design, synthesis, and biological evaluation of novel 2-methylpiperazine derivatives as potent CCR5 antagonists.Bioorganic & medicinal chemistry, , Mar-01, Volume: 23, Issue:5, 2015
Design, synthesis, and biological evaluation of novel piperidine-4-carboxamide derivatives as potent CCR5 inhibitors.European journal of medicinal chemistry, , Volume: 71, 2014
Preparation and activities of macromolecule conjugates of the CCR5 antagonist Maraviroc.ACS medicinal chemistry letters, , Feb-13, Volume: 5, Issue:2, 2014
A Bivalent Ligand Targeting the Putative Mu Opioid Receptor and Chemokine Receptor CCR5 Heterodimers: Binding Affinity versus Functional Activities.MedChemComm, , May-01, Volume: 4, Issue:5, 2013
Chemokine receptor antagonists.Journal of medicinal chemistry, , Nov-26, Volume: 55, Issue:22, 2012
An imidazopiperidine series of CCR5 antagonists for the treatment of HIV: the discovery of N-{(1S)-1-(3-fluorophenyl)-3-[(3-endo)-3-(5-isobutyryl-2-methyl-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridin-1-yl)-8-azabicyclo[3.2.1]oct-8-yl]propyl}acetamide (PF-2Journal of medicinal chemistry, , Jan-13, Volume: 54, Issue:1, 2011
Screening for GPCR Ligands Using Surface Plasmon Resonance.ACS medicinal chemistry letters, , Jul-14, Volume: 2, Issue:7, 2011
Novel hexahydropyrrolo[3,4-c]pyrrole CCR5 antagonists.Bioorganic & medicinal chemistry letters, , May-15, Volume: 20, Issue:10, 2010
Evaluation of a 3-amino-8-azabicyclo[3.2.1]octane replacement in the CCR5 antagonist maraviroc.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 20, Issue:5, 2010
1-Amido-1-phenyl-3-piperidinylbutanes - CCR5 antagonists for the treatment of HIV. Part 1.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 19, Issue:4, 2009
1-Amido-1-phenyl-3-piperidinylbutanes--CCR5 antagonists for the treatment of HIV: part 2.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 19, Issue:5, 2009
New approaches toward anti-HIV chemotherapy.Journal of medicinal chemistry, , Mar-10, Volume: 48, Issue:5, 2005
Chemokine receptor antagonists.Journal of medicinal chemistry, , Nov-26, Volume: 55, Issue:22, 2012
Discovery of INCB9471, a Potent, Selective, and Orally Bioavailable CCR5 Antagonist with Potent Anti-HIV-1 Activity.ACS medicinal chemistry letters, , Dec-09, Volume: 1, Issue:9, 2010
Piperazine-based CCR5 antagonists as HIV-1 inhibitors. IV. Discovery of 1-[(4,6-dimethyl-5-pyrimidinyl)carbonyl]- 4-[4-[2-methoxy-1(R)-4-(trifluoromethyl)phenyl]ethyl-3(S)-methyl-1-piperazinyl]- 4-methylpiperidine (Sch-417690/Sch-D), a potent, highly seleJournal of medicinal chemistry, , May-06, Volume: 47, Issue:10, 2004
Oximino-piperidino-piperidine-based CCR5 antagonists. Part 2: synthesis, SAR and biological evaluation of symmetrical heteroaryl carboxamides.Bioorganic & medicinal chemistry letters, , Feb-24, Volume: 13, Issue:4, 2003
Enables
This protein enables 10 target(s):
Target | Category | Definition |
virus receptor activity | molecular function | Combining with a virus component and mediating entry of the virus into the cell. [GOC:bf, GOC:dph, PMID:7621403, UniProtKB-KW:KW-1183] |
actin binding | molecular function | Binding to monomeric or multimeric forms of actin, including actin filaments. [GOC:clt] |
phosphatidylinositol phospholipase C activity | molecular function | Catalysis of the reaction: 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate + H2O = 1,2-diacylglycerol + 1D-myo-inositol 1,4,5-trisphosphate + H+. [EC:3.1.4.11, RHEA:33179] |
chemokine receptor activity | molecular function | Combining with a chemokine, and transmitting the signal from one side of the membrane to the other to initiate a change in cell activity. Chemokines are a family of small chemotactic cytokines; their name is derived from their ability to induce directed chemotaxis in nearby responsive cells. All chemokines possess a number of conserved cysteine residues involved in intramolecular disulfide bond formation. Some chemokines are considered pro-inflammatory and can be induced during an immune response to recruit cells of the immune system to a site of infection, while others are considered homeostatic and are involved in controlling the migration of cells during normal processes of tissue maintenance or development. Chemokines are found in all vertebrates, some viruses and some bacteria. [GOC:BHF, GOC:rl, GOC:signaling, IUPHAR_GPCR:1280, PMID:12183377, PMID:8662823, Wikipedia:Chemokine] |
protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
coreceptor activity | molecular function | Combining with an extracellular or intracellular messenger, and in cooperation with a nearby primary receptor, initiating a change in cell activity. [GOC:go_curators] |
C-C chemokine receptor activity | molecular function | Combining with a C-C chemokine and transmitting the signal from one side of the membrane to the other to initiate a change in cell activity. C-C chemokines do not have an amino acid between the first two cysteines of the characteristic four-cysteine motif. [GOC:signaling, PMID:8662823] |
C-C chemokine binding | molecular function | Binding to a C-C chemokine; C-C chemokines do not have an amino acid between the first two cysteines of the characteristic four-cysteine motif. [GOC:ai] |
identical protein binding | molecular function | Binding to an identical protein or proteins. [GOC:jl] |
chemokine (C-C motif) ligand 5 binding | molecular function | Binding to chemokine (C-C motif) ligand 5. [GOC:add, GOC:amm] |
Located In
This protein is located in 4 target(s):
Target | Category | Definition |
endosome | cellular component | A vacuole to which materials ingested by endocytosis are delivered. [ISBN:0198506732, PMID:19696797] |
plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
external side of plasma membrane | cellular component | The leaflet of the plasma membrane that faces away from the cytoplasm and any proteins embedded or anchored in it or attached to its surface. [GOC:dos, GOC:tb] |
cell surface | cellular component | The external part of the cell wall and/or plasma membrane. [GOC:jl, GOC:mtg_sensu, GOC:sm] |
Active In
This protein is active in 3 target(s):
Target | Category | Definition |
cell surface | cellular component | The external part of the cell wall and/or plasma membrane. [GOC:jl, GOC:mtg_sensu, GOC:sm] |
external side of plasma membrane | cellular component | The leaflet of the plasma membrane that faces away from the cytoplasm and any proteins embedded or anchored in it or attached to its surface. [GOC:dos, GOC:tb] |
cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
Involved In
This protein is involved in 20 target(s):
Target | Category | Definition |
MAPK cascade | biological process | An intracellular protein kinase cascade containing at least a MAP kinase (MAPK). It starts with the activation of a MAP3K, and the consecutive activation of a MPK2K and a MAPK. The cascade can also contain an additional tier: the upstream MAP4K. The kinases in each tier phosphorylate and activate the kinase in the downstream tier to transmit a signal within a cell. [PMID:20811974, PMID:9561267] |
dendritic cell chemotaxis | biological process | The movement of a dendritic cell in response to an external stimulus. [CL:0000451, GOC:add, ISBN:0781735149, PMID:15814331, PMID:16056255] |
calcium ion transport | biological process | The directed movement of calcium (Ca) ions into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. [GOC:ai] |
chemotaxis | biological process | The directed movement of a motile cell or organism, or the directed growth of a cell guided by a specific chemical concentration gradient. Movement may be towards a higher concentration (positive chemotaxis) or towards a lower concentration (negative chemotaxis). [ISBN:0198506732] |
cellular defense response | biological process | A defense response that is mediated by cells. [GOC:ebc] |
cell surface receptor signaling pathway | biological process | The series of molecular signals initiated by an extracellular ligand binding to a receptor located on the cell surface. The pathway ends with regulation of a downstream cellular process, e.g. transcription. [GOC:signaling] |
G protein-coupled receptor signaling pathway | biological process | The series of molecular signals initiated by a ligand binding to its receptor, in which the activated receptor promotes the exchange of GDP for GTP on the alpha-subunit of an associated heterotrimeric G-protein complex. The GTP-bound activated alpha-G-protein then dissociates from the beta- and gamma-subunits to further transmit the signal within the cell. The pathway begins with receptor-ligand interaction, and ends with regulation of a downstream cellular process. The pathway can start from the plasma membrane, Golgi or nuclear membrane. [GOC:bf, GOC:mah, PMID:16902576, PMID:24568158, Wikipedia:G_protein-coupled_receptor] |
cell-cell signaling | biological process | Any process that mediates the transfer of information from one cell to another. This process includes signal transduction in the receiving cell and, where applicable, release of a ligand and any processes that actively facilitate its transport and presentation to the receiving cell. Examples include signaling via soluble ligands, via cell adhesion molecules and via gap junctions. [GOC:dos, GOC:mah] |
release of sequestered calcium ion into cytosol by sarcoplasmic reticulum | biological process | The process in which the release of sequestered calcium ion by sarcoplasmic reticulum into cytosol occurs via calcium release channels. [GOC:mtg_muscle] |
calcium-mediated signaling | biological process | Any intracellular signal transduction in which the signal is passed on within the cell via calcium ions. [GOC:signaling] |
signaling | biological process | The entirety of a process in which information is transmitted within a biological system. This process begins with an active signal and ends when a cellular response has been triggered. [GOC:mtg_signal, GOC:mtg_signaling_feb11, GOC:signaling] |
symbiont entry into host cell | biological process | The process by which a symbiont breaches the plasma membrane or cell envelope and enters the host cell. The process ends when the symbiont or its genome is released into the host cell. [GOC:jl] |
chemokine-mediated signaling pathway | biological process | The series of molecular signals initiated by a chemokine binding to its receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:mah, GOC:signaling] |
response to cholesterol | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a cholesterol stimulus. [GOC:BHF, GOC:vk] |
cellular response to lipopolysaccharide | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a lipopolysaccharide stimulus; lipopolysaccharide is a major component of the cell wall of gram-negative bacteria. [GOC:mah] |
negative regulation of macrophage apoptotic process | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of macrophage apoptotic process. [GOC:BHF, GOC:mtg_apoptosis] |
inflammatory response | biological process | The immediate defensive reaction (by vertebrate tissue) to infection or injury caused by chemical or physical agents. The process is characterized by local vasodilation, extravasation of plasma into intercellular spaces and accumulation of white blood cells and macrophages. [GO_REF:0000022, ISBN:0198506732] |
positive regulation of cytosolic calcium ion concentration | biological process | Any process that increases the concentration of calcium ions in the cytosol. [GOC:ai] |
immune response | biological process | Any immune system process that functions in the calibrated response of an organism to a potential internal or invasive threat. [GO_REF:0000022, GOC:add] |
cell chemotaxis | biological process | The directed movement of a motile cell guided by a specific chemical concentration gradient. Movement may be towards a higher concentration (positive chemotaxis) or towards a lower concentration (negative chemotaxis). [GOC:dph] |