A C-X-C chemokine receptor type 4 that is encoded in the genome of human. [PRO:WCB, UniProtKB:P61073]
A fragment integrational approach to GPCR inhibition: Identification of a high affinity small molecule CXCR4 antagonist.European journal of medicinal chemistry, , Mar-05, Volume: 231, 2022
Amide-sulfamide modulators as effective anti-tumor metastatic agents targeting CXCR4/CXCL12 axis.European journal of medicinal chemistry, , Jan-01, Volume: 185, 2020
[no title available]European journal of medicinal chemistry, , Nov-01, Volume: 205, 2020
Structural optimization of aminopyrimidine-based CXCR4 antagonists.European journal of medicinal chemistry, , Feb-01, Volume: 187, 2020
Synthesis and evaluation of 2,5-diamino and 2,5-dianilinomethyl pyridine analogues as potential CXCR4 antagonists.Bioorganic & medicinal chemistry letters, , 01-15, Volume: 29, Issue:2, 2019
Development of CXCR4 modulators based on the lead compound RB-108.European journal of medicinal chemistry, , Jul-01, Volume: 173, 2019
Structure-based exploration and pharmacological evaluation of N-substituted piperidin-4-yl-methanamine CXCR4 chemokine receptor antagonists.European journal of medicinal chemistry, , Jan-15, Volume: 162, 2019
High affinity CXCR4 inhibitors generated by linking low affinity peptides.European journal of medicinal chemistry, , Jun-15, Volume: 172, 2019
Development of Stem-Cell-Mobilizing Agents Targeting CXCR4 Receptor for Peripheral Blood Stem Cell Transplantation and Beyond.Journal of medicinal chemistry, , 02-08, Volume: 61, Issue:3, 2018
Anti-inflammatory hybrids of secondary amines and amide-sulfamide derivatives.European journal of medicinal chemistry, , Apr-25, Volume: 150, 2018
Design, synthesis, and structure-activity-relationship of a novel series of CXCR4 antagonists.European journal of medicinal chemistry, , Apr-10, Volume: 149, 2018
Development of CXCR4 modulators by virtual HTS of a novel amide-sulfamide compound library.European journal of medicinal chemistry, , Jan-27, Volume: 126, 2017
An update on small molecules targeting CXCR4 as starting points for the development of anti-cancer therapeutics.European journal of medicinal chemistry, , Oct-20, Volume: 139, 2017
Novel anti-inflammatory agents targeting CXCR4: Design, synthesis, biological evaluation and preliminary pharmacokinetic study.European journal of medicinal chemistry, , Aug-18, Volume: 136, 2017
Structure-Activity Relationships and Biological Characterization of a Novel, Potent, and Serum Stable C-X-C Chemokine Receptor Type 4 (CXCR4) Antagonist.Journal of medicinal chemistry, , 12-14, Volume: 60, Issue:23, 2017
Symmetrical bis-tertiary amines as novel CXCR4 inhibitors.European journal of medicinal chemistry, , Aug-08, Volume: 118, 2016
Exploring the N-Terminal Region of C-X-C Motif Chemokine 12 (CXCL12): Identification of Plasma-Stable Cyclic Peptides As Novel, Potent C-X-C Chemokine Receptor Type 4 (CXCR4) Antagonists.Journal of medicinal chemistry, , Sep-22, Volume: 59, Issue:18, 2016
Design, synthesis, and biological characterization of novel PEG-linked dimeric modulators for CXCR4.Bioorganic & medicinal chemistry, , 11-01, Volume: 24, Issue:21, 2016
Chemokine receptor antagonists.Journal of medicinal chemistry, , Nov-26, Volume: 55, Issue:22, 2012
The novel CXCR4 antagonist KRH-3955 is an orally bioavailable and extremely potent inhibitor of human immunodeficiency virus type 1 infection: comparative studies with AMD3100.Antimicrobial agents and chemotherapy, , Volume: 53, Issue:7, 2009
64Cu-AMD3100--a novel imaging agent for targeting chemokine receptor CXCR4.Bioorganic & medicinal chemistry, , Feb-15, Volume: 17, Issue:4, 2009
Orally bioavailable isothioureas block function of the chemokine receptor CXCR4 in vitro and in vivo.Journal of medicinal chemistry, , Dec-25, Volume: 51, Issue:24, 2008
Allosteric transinhibition by specific antagonists in CCR2/CXCR4 heterodimers.The Journal of biological chemistry, , Oct-12, Volume: 282, Issue:41, 2007
Molecular mechanism of action of monocyclam versus bicyclam non-peptide antagonists in the CXCR4 chemokine receptor.The Journal of biological chemistry, , Sep-14, Volume: 282, Issue:37, 2007
Target | Category | Definition |
virus receptor activity | molecular function | Combining with a virus component and mediating entry of the virus into the cell. [GOC:bf, GOC:dph, PMID:7621403, UniProtKB-KW:KW-1183] |
actin binding | molecular function | Binding to monomeric or multimeric forms of actin, including actin filaments. [GOC:clt] |
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] |
coreceptor activity | molecular function | Combining with an extracellular or intracellular messenger, and in cooperation with a nearby primary receptor, initiating a change in cell activity. [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] |
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] |
ubiquitin protein ligase binding | molecular function | Binding to a ubiquitin protein ligase enzyme, any of the E3 proteins. [GOC:vp] |
myosin light chain binding | molecular function | Binding to a light chain of a myosin complex. [GOC:mah] |
small molecule binding | molecular function | Binding to a small molecule, any low molecular weight, monomeric, non-encoded molecule. [GOC:curators, GOC:pde, GOC:pm] |
C-X-C motif chemokine 12 receptor activity | molecular function | 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] |
ubiquitin binding | molecular function | Binding to ubiquitin, a protein that when covalently bound to other cellular proteins marks them for proteolytic degradation. [GOC:ecd] |
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] |
Target | Category | Definition |
response to hypoxia | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a stimulus indicating lowered oxygen tension. Hypoxia, defined as a decline in O2 levels below normoxic levels of 20.8 - 20.95%, results in metabolic adaptation at both the cellular and organismal level. [GOC:hjd] |
neuron migration | biological process | The characteristic movement of an immature neuron from germinal zones to specific positions where they will reside as they mature. [CL:0000540, GOC:go_curators] |
epithelial cell development | biological process | The process whose specific outcome is the progression of an epithelial cell over time, from its formation to the mature structure. An epithelial cell is a cell usually found in a two-dimensional sheet with a free surface. [GOC:dph] |
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] |
apoptotic process | biological process | A programmed cell death process which begins when a cell receives an internal (e.g. DNA damage) or external signal (e.g. an extracellular death ligand), and proceeds through a series of biochemical events (signaling pathway phase) which trigger an execution phase. The execution phase is the last step of an apoptotic process, and is typically characterized by rounding-up of the cell, retraction of pseudopodes, reduction of cellular volume (pyknosis), chromatin condensation, nuclear fragmentation (karyorrhexis), plasma membrane blebbing and fragmentation of the cell into apoptotic bodies. When the execution phase is completed, the cell has died. [GOC:cjm, GOC:dhl, GOC:ecd, GOC:go_curators, GOC:mtg_apoptosis, GOC:tb, ISBN:0198506732, PMID:18846107, PMID:21494263] |
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] |
G protein-coupled receptor signaling pathway | biological process | The series of molecular signals initiated by a ligand binding to its receptor, in which the activated receptor promotes the exchange of GDP for GTP on the alpha-subunit of an associated heterotrimeric G-protein complex. The GTP-bound activated alpha-G-protein then dissociates from the beta- and gamma-subunits to further transmit the signal within the cell. The pathway begins with receptor-ligand interaction, and ends with regulation of a downstream cellular process. The pathway can start from the plasma membrane, Golgi or nuclear membrane. [GOC:bf, GOC:mah, PMID:16902576, PMID:24568158, Wikipedia:G_protein-coupled_receptor] |
neuron recognition | biological process | The process in which a neuronal cell in a multicellular organism interprets its surroundings. [GOC:go_curators] |
response to virus | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a stimulus from a virus. [GOC:hb] |
response to activity | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an activity stimulus. [GOC:mtg_muscle] |
telencephalon cell migration | biological process | The orderly movement of a cell from one site to another at least one of which is located in the telencephalon. [GO_REF:0000021, GOC:cls, GOC:curators, GOC:dgh, GOC:dph, GOC:jid] |
regulation of cell adhesion | biological process | Any process that modulates the frequency, rate or extent of attachment of a cell to another cell or to the extracellular matrix. [GOC:mah] |
positive regulation of cell migration | biological process | Any process that activates or increases the frequency, rate or extent of cell migration. [GOC:go_curators] |
positive regulation of vascular wound healing | biological process | Any process that increases the rate, frequency, or extent of blood vessel formation when new vessels emerge from the proliferation of pre-existing blood vessels and contribute to the series of events that restore integrity to damaged vasculature. [GOC:rph] |
CXCL12-activated CXCR4 signaling pathway | biological process | The series of molecular signals initiated by the binding of the C-X-C chemokine CXCL12 to a C-X-C chemokine type 4 receptor (CXCR4) on the surface of a target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:nhn] |
regulation of programmed cell death | biological process | Any process that modulates the frequency, rate or extent of programmed cell death, cell death resulting from activation of endogenous cellular processes. [GOC:jl] |
myelin maintenance | biological process | The process of preserving the structure and function of mature myelin. This includes maintaining the compact structure of myelin necessary for its electrical insulating characteristics as well as the structure of non-compact regions such as Schmidt-Lantermann clefts and paranodal loops. This does not include processes responsible for maintaining the nodes of Ranvier, which are not part of the myelin sheath. [GOC:dgh] |
endothelial cell differentiation | biological process | The process in which a mesodermal, bone marrow or neural crest cell acquires specialized features of an endothelial cell, a thin flattened cell. A layer of such cells lines the inside surfaces of body cavities, blood vessels, and lymph vessels, making up the endothelium. [CL:0000115, GOC:go_curators] |
symbiont entry into host cell | biological process | The process by which a symbiont breaches the plasma membrane or cell envelope and enters the host cell. The process ends when the symbiont or its genome is released into the host cell. [GOC:jl] |
positive regulation of oligodendrocyte differentiation | biological process | Any process that activates or increases the frequency, rate or extent of oligodendrocyte differentiation. [GOC:vp, PMID:15139015] |
regulation of viral process | biological process | Any process that modulates the rate or extent of the viral life cycle, the set of processes by which a virus reproduces and spreads among hosts. [GOC:go_curators, GOC:tb] |
regulation of chemotaxis | biological process | Any process that modulates the frequency, rate or extent of the directed movement of a motile cell or organism in response to a specific chemical concentration gradient. [GOC:ai] |
positive regulation of chemotaxis | biological process | Any process that activates or increases the frequency, rate or extent of the directed movement of a motile cell or organism in response to a specific chemical concentration gradient. [GOC:ai] |
detection of temperature stimulus involved in sensory perception of pain | biological process | The series of events involved in the perception of pain in which a temperature stimulus is received and converted into a molecular signal. [GOC:ai, GOC:dos] |
detection of mechanical stimulus involved in sensory perception of pain | biological process | The series of events involved in the perception of pain in which a mechanical stimulus is received and converted into a molecular signal. [GOC:ai, GOC:dos] |
regulation of calcium ion transport | biological process | Any process that modulates the frequency, rate or extent of the directed movement of calcium ions into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. [GOC:ai] |
cardiac muscle contraction | biological process | Muscle contraction of cardiac muscle tissue. [GOC:dph] |
endothelial tube morphogenesis | biological process | The process in which the anatomical structures of a tube are generated and organized from an endothelium. Endothelium refers to the layer of cells lining blood vessels, lymphatics, the heart, and serous cavities, and is derived from bone marrow or mesoderm. Corneal endothelium is a special case, derived from neural crest cells. [GOC:dph, GOC:yaf] |
cellular response to cytokine stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a cytokine stimulus. [GOC:mah] |
cellular response to organonitrogen compound | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an organonitrogen stimulus. An organonitrogen compound is formally a compound containing at least one carbon-nitrogen bond. [GOC:mah] |
cellular response to xenobiotic stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a stimulus from a xenobiotic, a compound foreign to the organism exposed to it. It may be synthesized by another organism (like ampicilin) or it can be a synthetic chemical. [GOC:krc, GOC:mah] |
positive regulation of cold-induced thermogenesis | biological process | Any process that activates or increases the frequency, rate or extent of cold-induced thermogenesis. [PMID:27876809] |
response to tacrolimus | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a tacrolimus stimulus. [GOC:TermGenie] |
positive regulation of dendrite extension | biological process | Any process that activates or increases the frequency, rate or extent of dendrite extension. [GO_REF:0000058, GOC:pad, GOC:PARL, GOC:TermGenie, PMID:24898855] |
positive regulation of vasculature development | biological process | Any process that activates or increases the frequency, rate or extent of vasculature development. [GO_REF:0000058, GOC:TermGenie, PMID:21472453] |
positive regulation of mesenchymal stem cell migration | biological process | Any process that activates or increases the frequency, rate or extent of mesenchymal stem cell migration. [GO_REF:0000058, GOC:TermGenie, PMID:26846297] |
response to ultrasound | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an ultrasonic stimulus. [PMID:20950932] |
positive regulation of macrophage migration inhibitory factor signaling pathway | biological process | Any process that activates or increases the frequency, rate or extent of macrophage migration inhibitory factor signaling pathway. [GOC:obol] |
neurogenesis | biological process | Generation of cells within the nervous system. [GO_REF:0000021, GOC:cls, GOC:curators, GOC:dgh, GOC:dph, GOC:jid] |
cell chemotaxis | biological process | The directed movement of a motile cell guided by a specific chemical concentration gradient. Movement may be towards a higher concentration (positive chemotaxis) or towards a lower concentration (negative chemotaxis). [GOC:dph] |
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] |
brain development | biological process | The process whose specific outcome is the progression of the brain over time, from its formation to the mature structure. Brain development begins with patterning events in the neural tube and ends with the mature structure that is the center of thought and emotion. The brain is responsible for the coordination and control of bodily activities and the interpretation of information from the senses (sight, hearing, smell, etc.). [GOC:dph, GOC:jid, GOC:tb, UBERON:0000955] |
calcium-mediated signaling | biological process | Any intracellular signal transduction in which the signal is passed on within the cell via calcium ions. [GOC:signaling] |