Details of the BTS
| General Information of Binding Target of SBP (BTS) (ID: ST00078) | ||||||
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| BTS Name |
C-X-C chemokine receptor type 4
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| Synonyms |
CXC-R4; CXCR-4; FB22; Fusin; HM89; LCR1; Leukocyte-derived seven transmembrane domain receptor; LESTR; Lipopolysaccharide-associated protein 3; LAP-3; LPS-associated protein 3; NPYRL; Stromal cell-derived factor 1 receptor; SDF-1 receptor; CD antigen CD184
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| BTS Type |
Protein
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| Family |
G-protein coupled receptor 1 family
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| Gene Name |
CXCR4
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| Organism |
Homo sapiens (Human)
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| Function |
Receptor for the C-X-C chemokine CXCL12/SDF-1 that transduces a signal by increasing intracellular calcium ion levels and enhancing MAPK1/MAPK3 activation Involved in the AKT signaling cascade Plays a role in regulation of cell migration, e.g. during wound healing Acts as a receptor for extracellular ubiquitin; leading to enhanced intracellular calcium ions and reduced cellular cAMP levels Binds bacterial lipopolysaccharide (LPS) et mediates LPS-induced inflammatory response, including TNF secretion by monocytes Involved in hematopoiesis and in cardiac ventricular septum formation. Also plays an essential role in vascularization of the gastrointestinal tract, probably by regulating vascular branching and/or remodeling processes in endothelial cells. Involved in cerebellar development. In the CNS, could mediate hippocampal-neuron survival (By similarity).; (Microbial infection) Acts as a coreceptor (CD4 being the primary receptor) for human immunodeficiency virus-1/HIV-1 X4 isolates and as a primary receptor for some HIV-2 isolates. Promotes Env-mediated fusion of the virus
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| UniProt ID | ||||||
| UniProt Entry | ||||||
| PFam | ||||||
| Gene ID | ||||||
| Sequence |
MEGISIYTSDNYTEEMGSGDYDSMKEPCFREENANFNKIFLPTIYSIIFLTGIVGNGLVI
LVMGYQKKLRSMTDKYRLHLSVADLLFVITLPFWAVDAVANWYFGNFLCKAVHVIYTVNL YSSVLILAFISLDRYLAIVHATNSQRPRKLLAEKVVYVGVWIPALLLTIPDFIFANVSEA DDRYICDRFYPNDLWVVVFQFQHIMVGLILPGIVILSCYCIIISKLSHSKGHQKRKALKT TVILILAFFACWLPYYIGISIDSFILLEIIKQGCEFENTVHKWISITEALAFFHCCLNPI LYAFLGAKFKTSAQHALTSVSRGSSLKILSKGKRGGHSSVSTESESSSFHSS |
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| Sequence Length |
352
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| Synthetic Binding Protein (SBP) Targeting This BTS |
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| SBP Name | Highest Status | Mechanism | Affinity | Application | Details | Ref |
|---|---|---|---|---|---|---|
| Beta-Hairpin mimetic anti-CXCR4 POL2438 | Research | Inhibitor | N.A. | Human immunodeficiency virus infection (HIV infection) [ICD-11: 1C62.Z] | [1] | |
| Beta-Hairpin mimetic anti-CXCR4 POL3026 | Research | Inhibitor | N.A. | Human immunodeficiency virus infection (HIV infection) [ICD-11: 1C62.Z] | [1] | |
| Beta-Hairpin mimetic anti-CXCR4 POL5551 | Research | Inhibitor | N.A. | Inflammation [ICD-11: 1A00-CA43.1]; Asthma [ICD-11: CA23] | [2] | |
| beta-Hairpin mimetic Balixafortide | Phase III | Inhibitor | Kd: 2 nM | Multiple myeloma [ICD-11: 2A83.Y]; Breast cancer [ICD-11: 2C6Z]; Metastatic breast cancer in combination with eribulin [ICD-11: 2E0Y]; Acute myocardial infarction [ICD-11: BA41.Z]; Hematopoietic stem cell mobilization;SARS-CoV-2 infection (COVID-19) [ICD-11: XN109] | [3], [4] | |
| beta-Hairpin mimetic Murepavadin | Phase III | Inhibitor | N.A. | Bacterial pneumonia [ICD-11: CA40.0Z]; Pseudomonas aeruginosa [ICD-11: XN5L6] | [2], [5], [6] | |
| Cyclotide anti-CXCR4 MCo-CVX-5c | Research | Antagonist | N.A. | Human immunodeficiency virus type 1 infection [ICD-11: XN8LD]; Cancers [ICD-11: 2D4Z] | [7] | |
| I-body AD-214 | Phase I | Antagonist | N.A. | Fibrosis [ICD-11: CA25.Z]; Interstitial lung diseases [ICD-11: CB0Z]; Age related macular degeneration [ICD-11: 9B75.0] | [8] | |
| I-body anti-CXCR4 AD-114 | Research | Antagonist | Kd: 4.2-5.2 nM | Idiopathic pulmonary fibrosis [ICD-11: CB03.4] | [9], [8] | |
| I-body anti-CXCR4 AD-114 | Research | Blocker | N.A. | Chronic kidney disease [ICD-11: GB61] | [10] | |
| I-body anti-CXCR4 AD-114-Im7-FH | Research | Antagonist | Kd: 9.1 nM | Cancers [ICD-11: 2D4Z]; Fibrosis [ICD-11: CA25.Z] | [11] | |
| I-body anti-CXCR4 AD-114-Im7-FH-PEG (2 x 20K) | Research | Antagonist | Kd: 0.7 nM | Research tool | [11] | |
| I-body anti-CXCR4 AD-114-Im7-FH-PEG (30K) | Research | Antagonist | Kd: 0.7 nM | Research tool | [11] | |
| I-body anti-CXCR4 AD-114-PA600 | Research | Antagonist | Kd: 4.0 nM | Cancers [ICD-11: 2D4Z]; Fibrosis [ICD-11: CA25.Z] | [11] | |
| I-body anti-CXCR4 AD-114-PA600-6H | Research | Antagonist | Kd: 5.2 nM | Cancers [ICD-11: 2D4Z]; Fibrosis [ICD-11: CA25.Z] | [11] | |
| I-body anti-CXCR4 ADCX-99 | Research | Antagonist | Kd: 643 nM | Cancers [ICD-11: 2D4Z]; Fibrosis [ICD-11: CA25.Z] | [12] | |
| I-body anti-CXCR4 AM1-126 | Research | Antagonist | Kd: 27.2 nM | Cancers [ICD-11: 2D4Z]; Fibrosis [ICD-11: CA25.Z] | [12] | |
| I-body anti-CXCR4 AM1-320 | Research | Antagonist | Kd: 15.9 nM | Cancers [ICD-11: 2D4Z]; Fibrosis [ICD-11: CA25.Z] | [12] | |
| I-body anti-CXCR4 AM3-114 | Research | Antagonist | Kd: 4.2 nM | Human immunodeficiency virus infection (HIV infection) [ICD-11: 1C62.Z]; Cell migration; Leukocyte recruitment | [12] | |
| I-body anti-CXCR4 AM3-523 | Research | Antagonist | Kd: 9.2 nM | Human immunodeficiency virus infection (HIV infection) [ICD-11: 1C62.Z]; Cell migration; Leukocyte recruitment | [12] | |
| I-body anti-CXCR4 AM4-1121 | Research | Antagonist | Kd: 6.3 nM | Cancers [ICD-11: 2D4Z]; Fibrosis [ICD-11: CA25.Z] | [12] | |
| I-body anti-CXCR4 AM4-272 | Research | Antagonist | Kd: 1.8 nM | Human immunodeficiency virus infection (HIV infection) [ICD-11: 1C62.Z]; Cell migration; Leukocyte recruitment | [12] | |
| I-body anti-CXCR4 AM4-746 | Research | Antagonist | Kd: 4.0 nM | Cancers [ICD-11: 2D4Z]; Fibrosis [ICD-11: CA25.Z] | [12] | |
| I-body anti-CXCR4/HSA AD-114-Im7-FH-SA21 | Research | Antagonist | Kd: 9.2 nM | Cancers [ICD-11: 2D4Z]; Fibrosis [ICD-11: CA25.Z] | [11] | |
| Macrocyclic peptide anti-CXCR4 CVX15 | Research | Antagonist | N.A. | Cancer metastasis [ICD-11: 2E2Z]; Human immunodeficiency virus type 1 infection [ICD-11: XN8LD] | [13] | |
| References |
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