CXCL12α   Click here for help

GtoPdb Ligand ID: 4358

Synonyms: CXCL12 α | SDF-1α | stromal cell-derived factor-1α
Immunopharmacology Ligand
Comment: CXCL12-1α and β were the first isoforms of this chemokine identified. Both proteins contain a signal peptide sequence that mediates their secretion via the canonical intracellular secretory pathway. CXCL12 participates in a variety of processes central to homeostasis and physiology, exerting its biological effects by binding to the chemokine receptors CXCR4 and CXCR7.
Species: Human
Click here for help
1. Adlere I, Sun S, Zarca A, Roumen L, Gozelle M, Viciano CP, Caspar B, Arimont M, Bebelman JP, Briddon SJ et al.. (2019)
Structure-based exploration and pharmacological evaluation of N-substituted piperidin-4-yl-methanamine CXCR4 chemokine receptor antagonists.
Eur J Med Chem, 162: 631-649. DOI: 10.1016/j.ejmech.2018.10.060 [PMID:30476826]
2. Gravel S, Malouf C, Boulais PE, Berchiche YA, Oishi S, Fujii N, Leduc R, Sinnett D, Heveker N. (2010)
The peptidomimetic CXCR4 antagonist TC14012 recruits beta-arrestin to CXCR7: roles of receptor domains.
J Biol Chem, 285 (49): 37939-43. [PMID:20956518]
3. Hesselgesser J, Liang M, Hoxie J, Greenberg M, Brass LF, Orsini MJ, Taub D, Horuk R. (1998)
Identification and characterization of the CXCR4 chemokine receptor in human T cell lines: ligand binding, biological activity, and HIV-1 infectivity.
J Immunol, 160 (2): 877-83. [PMID:9551924]
4. Hoellenriegel J, Zboralski D, Maasch C, Rosin NY, Wierda WG, Keating MJ, Kruschinski A, Burger JA. (2014)
The Spiegelmer NOX-A12, a novel CXCL12 inhibitor, interferes with chronic lymphocytic leukemia cell motility and causes chemosensitization.
Blood, 123 (7): 1032-9. [PMID:24277076]
5. Krikun G. (2018)
The CXL12/CXCR4/CXCR7 axis in female reproductive tract disease: Review.
Am J Reprod Immunol, 80 (5): e13028. [PMID:30106199]
6. Loetscher P, Gong JH, Dewald B, Baggiolini M, Clark-Lewis I. (1998)
N-terminal peptides of stromal cell-derived factor-1 with CXC chemokine receptor 4 agonist and antagonist activities.
J Biol Chem, 273 (35): 22279-83. [PMID:9712844]
7. Nagasawa T, Hirota S, Tachibana K, Takakura N, Nishikawa S, Kitamura Y, Yoshida N, Kikutani H, Kishimoto T. (1996)
Defects of B-cell lymphopoiesis and bone-marrow myelopoiesis in mice lacking the CXC chemokine PBSF/SDF-1.
Nature, 382 (6592): 635-8. [PMID:8757135]
8. Nguyen HH, Kim MB, Wilson RJ, Butch CJ, Kuo KM, Miller EJ, Tahirovic YA, Jecs E, Truax VM, Wang T et al.. (2018)
Design, Synthesis, and Pharmacological Evaluation of Second-Generation Tetrahydroisoquinoline-Based CXCR4 Antagonists with Favorable ADME Properties.
J Med Chem, 61 (16): 7168-7188. [PMID:30052039]
9. Patrussi L, Baldari CT. (2011)
The CXCL12/CXCR4 axis as a therapeutic target in cancer and HIV-1 infection.
Curr Med Chem, 18 (4): 497-512. [PMID:21143114]
10. Ray P, Stacer AC, Fenner J, Cavnar SP, Meguiar K, Brown M, Luker KE, Luker GD. (2015)
CXCL12-γ in primary tumors drives breast cancer metastasis.
Oncogene, 34 (16): 2043-51. [PMID:24909174]
11. Regenass P, Abboud D, Daubeuf F, Lehalle C, Gizzi P, Riché S, Hachet-Haas M, Rohmer F, Gasparik V, Boeglin D et al.. (2018)
Discovery of a Locally and Orally Active CXCL12 Neutraligand (LIT-927) with Anti-inflammatory Effect in a Murine Model of Allergic Airway Hypereosinophilia.
J Med Chem, 61 (17): 7671-7686. [PMID:30106292]
12. Sierro F, Biben C, Martínez-Muñoz L, Mellado M, Ransohoff RM, Li M, Woehl B, Leung H, Groom J, Batten M, Harvey RP, Martínez-A C, Mackay CR, Mackay F. (2007)
Disrupted cardiac development but normal hematopoiesis in mice deficient in the second CXCL12/SDF-1 receptor, CXCR7.
Proc Natl Acad Sci USA, 104 (37): 14759-64. [PMID:17804806]
13. Southern C, Cook JM, Neetoo-Isseljee Z, Taylor DL, Kettleborough CA, Merritt A, Bassoni DL, Raab WJ, Quinn E, Wehrman TS et al.. (2013)
Screening β-Arrestin Recruitment for the Identification of Natural Ligands for Orphan G-Protein-Coupled Receptors.
J Biomol Screen, 18 (5): 599-609. [PMID:23396314]
14. Tachibana K, Hirota S, Iizasa H, Yoshida H, Kawabata K, Kataoka Y, Kitamura Y, Matsushima K, Yoshida N, Nishikawa S et al.. (1998)
The chemokine receptor CXCR4 is essential for vascularization of the gastrointestinal tract.
Nature, 393 (6685): 591-4. [PMID:9634237]
15. Wang C, Chen W, Shen J. (2018)
CXCR7 Targeting and Its Major Disease Relevance.
Front Pharmacol, 9: 641. [PMID:29977203]
16. Weng Y, Siciliano SJ, Waldburger KE, Sirotina-Meisher A, Staruch MJ, Daugherty BL, Gould SL, Springer MS, DeMartino JA. (1998)
Binding and functional properties of recombinant and endogenous CXCR3 chemokine receptors.
J Biol Chem, 273 (29): 18288-91. [PMID:9660793]
17. Zou YR, Kottmann AH, Kuroda M, Taniuchi I, Littman DR. (1998)
Function of the chemokine receptor CXCR4 in haematopoiesis and in cerebellar development.
Nature, 393 (6685): 595-9. [PMID:9634238]