CX3CL1   Click here for help

GtoPdb Ligand ID: 856

Synonyms: fractalkine | neurotactin
Immunopharmacology Ligand
Compound class: Endogenous peptide in human, mouse or rat
Comment: This is the only member of the CX3C chemokine family [1].
Species: Human
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Ligand Activity Visualisation Charts

These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.

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View interactive charts of activity data across species
References
1. Bazan JF, Bacon KB, Hardiman G, Wang W, Soo K, Rossi D, Greaves DR, Zlotnik A, Schall TJ. (1997)
A new class of membrane-bound chemokine with a CX3C motif.
Nature, 385 (6617): 640-4. [PMID:9024663]
2. Chen D, Chen Q, Qin X, Tong P, Peng L, Zhang T, Xia C. (2023)
Development and evolution of human glutaminyl cyclase inhibitors (QCIs): an alternative promising approach for disease-modifying treatment of Alzheimer's disease.
Front Aging Neurosci, 15: 1209863. [PMID:37600512]
3. Coimbra JR, Sobral PJ, Santos AE, Moreira PI, Salvador JA. (2019)
An overview of glutaminyl cyclase inhibitors for Alzheimer's disease.
Future Med Chem, 11 (24): 3179-3194. [PMID:31838899]
4. Coimbra JRM, Moreira PI, Santos AE, Salvador JAR. (2023)
Therapeutic potential of glutaminyl cyclases: Current status and emerging trends.
Drug Discov Today, 28 (10): 103644. [PMID:37244566]
5. Garin A, Tarantino N, Faure S, Daoudi M, Lécureuil C, Bourdais A, Debré P, Deterre P, Combadiere C. (2003)
Two novel fully functional isoforms of CX3CR1 are potent HIV coreceptors.
J Immunol, 171 (10): 5305-12. [PMID:14607932]
6. Imai T, Hieshima K, Haskell C, Baba M, Nagira M, Nishimura M, Kakizaki M, Takagi S, Nomiyama H, Schall TJ et al.. (1997)
Identification and molecular characterization of fractalkine receptor CX3CR1, which mediates both leukocyte migration and adhesion.
Cell, 91 (4): 521-30. [PMID:9390561]
7. Imai T, Yasuda N. (2016)
Therapeutic intervention of inflammatory/immune diseases by inhibition of the fractalkine (CX3CL1)-CX3CR1 pathway.
Inflamm Regen, 36: 9. [PMID:29259682]
8. Kehlen A, Haegele M, Böhme L, Cynis H, Hoffmann T, Demuth HU. (2017)
N-terminal pyroglutamate formation in CX3CL1 is essential for its full biologic activity.
Biosci Rep, 37 (4). [PMID:28739588]
9. Maciejewski-Lenoir D, Chen S, Feng L, Maki R, Bacon KB. (1999)
Characterization of fractalkine in rat brain cells: migratory and activation signals for CX3CR-1-expressing microglia.
J Immunol, 163 (3): 1628-35. [PMID:10415068]
10. Tabuchi H, Katsurabara T, Mori M, Aoyama M, Obara T, Yasuda N, Kawano T, Imai T, Ieiri I, Kumagai Y. (2019)
Pharmacokinetics, Pharmacodynamics, and Safety of E6011, a Novel Humanized Antifractalkine (CX3CL1) Monoclonal Antibody: A Randomized, Double-Blind, Placebo-Controlled Single-Ascending-Dose Study.
J Clin Pharmacol, 59 (5): 688-701. [PMID:30575978]
11. Tanaka Y, Takeuchi T, Umehara H, Nanki T, Yasuda N, Tago F, Kawakubo M, Kitahara Y, Hojo S, Kawano T et al.. (2018)
Safety, pharmacokinetics, and efficacy of E6011, an antifractalkine monoclonal antibody, in a first-in-patient phase 1/2 study on rheumatoid arthritis.
Mod Rheumatol, 28 (1): 58-65. [PMID:28681650]
12. Van Manh N, Hoang VH, Ngo VTH, Ann J, Jang TH, Ha JH, Song JY, Ha HJ, Kim H, Kim YH et al.. (2021)
Discovery of highly potent human glutaminyl cyclase (QC) inhibitors as anti-Alzheimer's agents by the combination of pharmacophore-based and structure-based design.
Eur J Med Chem, 226: 113819. [PMID:34536669]
13. Zhang Y, Wang Y, Zhao Z, Peng W, Wang P, Xu X, Zhao C. (2022)
Glutaminyl cyclases, the potential targets of cancer and neurodegenerative diseases.
Eur J Pharmacol, 931: 175178. [PMID:35948163]