Target type: molecularfunction
Combining with the C-X-C motif chemokine 12 (CXCL12) and transmitting the signal from one side of the membrane to the other to initiate a change in cell activity. [GOC:bf, PMID:22204316]
CXCR12 receptor activity, also known as CXCR4 receptor activity, is a molecular function associated with the CXCR4 protein, a G protein-coupled receptor (GPCR). This receptor plays a crucial role in various cellular processes, particularly in the immune system, development, and cancer. CXCR12, the ligand for CXCR4, binds to the receptor triggering a signaling cascade that involves the activation of downstream signaling pathways such as the Gαi protein and the mitogen-activated protein kinase (MAPK) pathway. CXCR12 receptor activity is essential for the chemotaxis, migration, and homing of various cell types, including hematopoietic stem cells, lymphocytes, and endothelial cells. The interaction of CXCR12 and CXCR4 is critical for the development and maintenance of the hematopoietic system, as it regulates the mobilization, trafficking, and differentiation of hematopoietic stem and progenitor cells. CXCR4 is also involved in the formation of the immune system by directing the migration of lymphocytes to secondary lymphoid tissues. In addition, CXCR4 plays a crucial role in the development of the nervous system, particularly in the migration and differentiation of neurons. CXCR4 receptor activity has also been implicated in several pathological processes, including cancer, inflammation, and autoimmune diseases. In cancer, CXCR4 acts as a key mediator of tumor growth, metastasis, and angiogenesis. CXCR4 is overexpressed in many cancers, and its interaction with CXCR12 promotes tumor cell survival, proliferation, and invasion. CXCR4 is also involved in the development of inflammatory diseases by attracting inflammatory cells to sites of inflammation. Furthermore, CXCR4 receptor activity is linked to autoimmune diseases, as it contributes to the migration and activation of immune cells that attack healthy tissues. In summary, CXCR12 receptor activity is a complex molecular function that plays a pivotal role in various physiological and pathological processes. Understanding the intricate mechanisms underlying CXCR4 signaling is crucial for developing novel therapeutic strategies for treating diseases associated with aberrant CXCR4 receptor activity.'
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| Protein | Definition | Taxonomy |
|---|---|---|
| C-X-C chemokine receptor type 4 | A C-X-C chemokine receptor type 4 that is encoded in the genome of human. [PRO:WCB, UniProtKB:P61073] | Homo sapiens (human) |
| Compound | Definition | Classes | Roles |
|---|---|---|---|
| zalcitabine | zalcitabine : A pyrimidine 2',3'-dideoxyribonucleoside compound having cytosine as the nucleobase. Zalcitabine: A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by a hydrogen. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. The compound is a potent inhibitor of HIV replication at low concentrations, acting as a chain-terminator of viral DNA by binding to reverse transcriptase. Its principal toxic side effect is axonal degeneration resulting in peripheral neuropathy. | pyrimidine 2',3'-dideoxyribonucleoside | antimetabolite; antiviral drug; HIV-1 reverse transcriptase inhibitor |
| plerixafor | plerixafor : An azamacrocycle consisting of two cyclam rings connected by a 1,4-phenylenebis(methylene) linker. It is a CXCR4 chemokine receptor antagonist and a hematopoietic stem cell mobilizer. It is used in combination with grulocyte-colony stimulating factor (G-CSF) to mobilize hematopoietic stem cells to the perpheral blood for collection and subsequent autologous transplantation in patients with non-Hodgkin's lymphoma and multiple myeloma. plerixafor: a bicyclam derivate, highly potent & selective inhibitor of HIV-1 & HIV-2 | azacycloalkane; azamacrocycle; benzenes; crown amine; secondary amino compound; tertiary amino compound | anti-HIV agent; antineoplastic agent; C-X-C chemokine receptor type 4 antagonist; immunological adjuvant |
| benzylaniline | benzylaniline: major metabolite of antazoline; RN given refers to parent cpd | ||
| terephthalamide | benzenedicarboxamide | ||
| krh 1636 | KRH 1636: structure in first source | ||
| amd 8664 | |||
| cyclo(d-tyrosyl-arginyl-arginyl-3-(2-naphthyl)alanyl-glycyl) | oligopeptide | ||
| amd 070 | mavorixafor: a derivative of AMD3100; a CXCR4 blocker | aminoquinoline | |
| wz 811 | |||
| tn14003 | TN14003: synthetic antagonist 14-mer peptide inhibiting metastasis in an animal model |