Proteins > C-X-C chemokine receptor type 2
Page last updated: 2024-08-07 16:16:51
C-X-C chemokine receptor type 2
A C-X-C chemokine receptor type 2 that is encoded in the genome of human. [PRO:WCB, UniProtKB:P25025]
Synonyms
CXC-R2;
CXCR-2;
CDw128b;
GRO/MGSA receptor;
High affinity interleukin-8 receptor B;
IL-8R B;
IL-8 receptor type 2
Research
Bioassay Publications (17)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 9 (52.94) | 29.6817 |
| 2010's | 5 (29.41) | 24.3611 |
| 2020's | 3 (17.65) | 2.80 |
Compounds (14)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| azd8309 | Homo sapiens (human) | Kd | 0.0013 | 1 | 1 |
Design, synthesis and anti-tumor evaluation of 1,2,4-triazol-3-one derivatives and pyridazinone derivatives as novel CXCR2 antagonists.European journal of medicinal chemistry, , Dec-15, Volume: 226, 2021
Discovery of 2-[5-(4-Fluorophenylcarbamoyl)pyridin-2-ylsulfanylmethyl]phenylboronic Acid (SX-517): Noncompetitive Boronic Acid Antagonist of CXCR1 and CXCR2.Journal of medicinal chemistry, , Oct-23, Volume: 57, Issue:20, 2014
Chemokine receptor antagonists.Journal of medicinal chemistry, , Nov-26, Volume: 55, Issue:22, 2012
Comparison of N,N'-diarylsquaramides and N,N'-diarylureas as antagonists of the CXCR2 chemokine receptor.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 17, Issue:6, 2007
Chemokine receptor antagonists.Journal of medicinal chemistry, , Nov-26, Volume: 55, Issue:22, 2012
2-Arylpropionic CXC chemokine receptor 1 (CXCR1) ligands as novel noncompetitive CXCL8 inhibitors.Journal of medicinal chemistry, , Jun-30, Volume: 48, Issue:13, 2005
Discovery, structure-activity relationship study and biological evaluation of 2-thioureidothiophene-3-carboxylates as a novel class of C-X-C chemokine receptor 2 (CXCR2) antagonists.European journal of medicinal chemistry, , Oct-15, Volume: 204, 2020
Nicotinanilides as inhibitors of neutrophil chemotaxis.Bioorganic & medicinal chemistry letters, , Jun-03, Volume: 12, Issue:11, 2002
Discovery of 1,5-Dihydro-4ACS medicinal chemistry letters, , May-13, Volume: 12, Issue:5, 2021
Discovery of Novel 1-Cyclopentenyl-3-phenylureas as Selective, Brain Penetrant, and Orally Bioavailable CXCR2 Antagonists.Journal of medicinal chemistry, , 03-22, Volume: 61, Issue:6, 2018
Chemokine receptor antagonists.Journal of medicinal chemistry, , Nov-26, Volume: 55, Issue:22, 2012
Diaminocyclobutenediones as potent and orally bioavailable CXCR2 receptor antagonists: SAR in the phenolic amide region.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 19, Issue:15, 2009
Fluoroalkyl alpha side chain containing 3,4-diamino-cyclobutenediones as potent and orally bioavailable CXCR2-CXCR1 dual antagonists.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 19, Issue:5, 2009
C(4)-alkyl substituted furanyl cyclobutenediones as potent, orally bioavailable CXCR2 and CXCR1 receptor antagonists.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 17, Issue:13, 2007
Discovery of 2-hydroxy-N,N-dimethyl-3-{2-[[(R)-1-(5- methylfuran-2-yl)propyl]amino]-3,4-dioxocyclobut-1-enylamino}benzamide (SCH 527123): a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist.Journal of medicinal chemistry, , Dec-28, Volume: 49, Issue:26, 2006
Discovery and evaluation of a novel monocyclic series of CXCR2 antagonists.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 25, Issue:7, 2015
Evaluation of a series of bicyclic CXCR2 antagonists.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 18, Issue:2, 2008
Enables
This protein enables 7 target(s):
| Target | Category | Definition |
|---|
| interleukin-8 receptor activity | molecular function | Combining with interleukin-8 and transmitting the signal from one side of the membrane to the other to initiate a change in cell activity. [GOC:jl, GOC:signaling] |
| G protein-coupled receptor activity | molecular function | Combining with an extracellular signal and transmitting the signal across the membrane by activating an associated G-protein; promotes the exchange of GDP for GTP on the alpha subunit of a heterotrimeric G-protein complex. [GOC:bf, http://www.iuphar-db.org, Wikipedia:GPCR] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| C-X-C chemokine receptor activity | molecular function | Combining with a C-X-C chemokine and transmitting the signal from one side of the membrane to the other to initiate a change in cell activity. A C-X-C chemokine has a single amino acid between the first two cysteines of the characteristic four cysteine motif. [GOC:signaling, PMID:8662823] |
| interleukin-8 binding | molecular function | Binding to interleukin-8. [GOC:jl] |
| 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] |
Located In
This protein is located in 8 target(s):
| Target | Category | Definition |
|---|
| nucleoplasm | cellular component | That part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653] |
| 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] |
| cell surface | cellular component | The external part of the cell wall and/or plasma membrane. [GOC:jl, GOC:mtg_sensu, GOC:sm] |
| microtubule cytoskeleton | cellular component | The part of the cytoskeleton (the internal framework of a cell) composed of microtubules and associated proteins. [GOC:jl, ISBN:0395825172] |
| membrane | cellular component | A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194] |
| secretory granule membrane | cellular component | The lipid bilayer surrounding a secretory granule. [GOC:mah] |
| mast cell granule | cellular component | Coarse, bluish-black staining cytoplasmic granules, bounded by a plasma membrane and found in mast cells and basophils. Contents include histamine, heparin, chondroitin sulfates, chymase and tryptase. [GOC:jl, http://www.ijp-online.com/archives/1969/001/02/r0000-0000tc.htm, PMID:12360215] |
| mitotic spindle | cellular component | A spindle that forms as part of mitosis. Mitotic and meiotic spindles contain distinctive complements of proteins associated with microtubules. [GOC:mah, GOC:vw, PMID:11408572, PMID:18367542, PMID:8027178] |
Active In
This protein is active in 1 target(s):
| Target | Category | Definition |
|---|
| 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] |
Involved In
This protein is involved in 16 target(s):
| Target | Category | Definition |
|---|
| 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] |
| 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] |
| 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] |
| cellular defense response | biological process | A defense response that is mediated by cells. [GOC:ebc] |
| signal transduction | biological process | The cellular process in which a signal is conveyed to trigger a change in the activity or state of a cell. Signal transduction begins with reception of a signal (e.g. a ligand binding to a receptor or receptor activation by a stimulus such as light), or for signal transduction in the absence of ligand, signal-withdrawal or the activity of a constitutively active receptor. Signal transduction ends with regulation of a downstream cellular process, e.g. regulation of transcription or regulation of a metabolic process. Signal transduction covers signaling from receptors located on the surface of the cell and signaling via molecules located within the cell. For signaling between cells, signal transduction is restricted to events at and within the receiving cell. [GOC:go_curators, GOC:mtg_signaling_feb11] |
| 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] |
| phospholipase C-activating G protein-coupled receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation of phospholipase C (PLC) and a subsequent increase in the intracellular concentration of inositol trisphosphate (IP3) and diacylglycerol (DAG). [GOC:dph, GOC:mah, GOC:signaling, GOC:tb, ISBN:0815316194] |
| positive regulation of cell population proliferation | biological process | Any process that activates or increases the rate or extent of cell proliferation. [GOC:go_curators] |
| neutrophil chemotaxis | biological process | The directed movement of a neutrophil cell, the most numerous polymorphonuclear leukocyte found in the blood, in response to an external stimulus, usually an infection or wounding. [GOC:jl, ISBN:0198506732] |
| receptor internalization | biological process | A receptor-mediated endocytosis process that results in the movement of receptors from the plasma membrane to the inside of the cell. The process begins when cell surface receptors are monoubiquitinated following ligand-induced activation. Receptors are subsequently taken up into endocytic vesicles from where they are either targeted to the lysosome or vacuole for degradation or recycled back to the plasma membrane. [GOC:bf, GOC:mah, GOC:signaling, PMID:15006537, PMID:19643732] |
| interleukin-8-mediated signaling pathway | biological process | The series of molecular signals initiated by interleukin-8 binding to its receptor on the surface of a cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:nhn, GOC:signaling] |
| neutrophil activation | biological process | The change in morphology and behavior of a neutrophil resulting from exposure to a cytokine, chemokine, cellular ligand, or soluble factor. [GOC:mgi_curators, ISBN:0781735149] |
| 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] |
| calcium-mediated signaling | biological process | Any intracellular signal transduction in which the signal is passed on within the cell via calcium ions. [GOC:signaling] |
| 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] |