Page last updated: 2024-11-12

tn14003

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth

Description

TN14003: synthetic antagonist 14-mer peptide inhibiting metastasis in an animal model [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID16130647
MeSH IDM0470342

Synonyms (10)

Synonym
h-arg-arg-nal-cys-tyr-cit-lys-dlys-pro-tyr-arg-cit-cys-arg-nh2
tn14003
tn-14003
unii-1tw3ft746i
l-argininamide, l-arginyl-l-arginyl-3-(2-naphthalenyl)-l-alanyl-l-cysteinyl-l-tyrosyl-n5-(aminocarbonyl)-l-ornithyl-l-lysyl-d-lysyl-l-prolyl-l-tyrosyl-l-arginyl-n5-(aminocarbonyl)-l-ornithyl-l-cysteinyl-, cyclic (4->13)-disulfide
368874-31-1
1tw3ft746i ,
us9205085, msx-207
bdbm194584
Q27252880
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
C-X-C chemokine receptor type 4Homo sapiens (human)IC50 (µMol)0.00060.00030.28766.2000AID303360
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (44)

Processvia Protein(s)Taxonomy
calcium-mediated signalingC-X-C chemokine receptor type 4Homo sapiens (human)
response to hypoxiaC-X-C chemokine receptor type 4Homo sapiens (human)
neuron migrationC-X-C chemokine receptor type 4Homo sapiens (human)
epithelial cell developmentC-X-C chemokine receptor type 4Homo sapiens (human)
dendritic cell chemotaxisC-X-C chemokine receptor type 4Homo sapiens (human)
apoptotic processC-X-C chemokine receptor type 4Homo sapiens (human)
inflammatory responseC-X-C chemokine receptor type 4Homo sapiens (human)
G protein-coupled receptor signaling pathwayC-X-C chemokine receptor type 4Homo sapiens (human)
neuron recognitionC-X-C chemokine receptor type 4Homo sapiens (human)
response to virusC-X-C chemokine receptor type 4Homo sapiens (human)
response to activityC-X-C chemokine receptor type 4Homo sapiens (human)
telencephalon cell migrationC-X-C chemokine receptor type 4Homo sapiens (human)
regulation of cell adhesionC-X-C chemokine receptor type 4Homo sapiens (human)
positive regulation of cell migrationC-X-C chemokine receptor type 4Homo sapiens (human)
positive regulation of vascular wound healingC-X-C chemokine receptor type 4Homo sapiens (human)
CXCL12-activated CXCR4 signaling pathwayC-X-C chemokine receptor type 4Homo sapiens (human)
regulation of programmed cell deathC-X-C chemokine receptor type 4Homo sapiens (human)
myelin maintenanceC-X-C chemokine receptor type 4Homo sapiens (human)
endothelial cell differentiationC-X-C chemokine receptor type 4Homo sapiens (human)
symbiont entry into host cellC-X-C chemokine receptor type 4Homo sapiens (human)
positive regulation of oligodendrocyte differentiationC-X-C chemokine receptor type 4Homo sapiens (human)
regulation of viral processC-X-C chemokine receptor type 4Homo sapiens (human)
regulation of chemotaxisC-X-C chemokine receptor type 4Homo sapiens (human)
positive regulation of chemotaxisC-X-C chemokine receptor type 4Homo sapiens (human)
detection of temperature stimulus involved in sensory perception of painC-X-C chemokine receptor type 4Homo sapiens (human)
detection of mechanical stimulus involved in sensory perception of painC-X-C chemokine receptor type 4Homo sapiens (human)
regulation of calcium ion transportC-X-C chemokine receptor type 4Homo sapiens (human)
cardiac muscle contractionC-X-C chemokine receptor type 4Homo sapiens (human)
endothelial tube morphogenesisC-X-C chemokine receptor type 4Homo sapiens (human)
cellular response to cytokine stimulusC-X-C chemokine receptor type 4Homo sapiens (human)
cellular response to organonitrogen compoundC-X-C chemokine receptor type 4Homo sapiens (human)
cellular response to xenobiotic stimulusC-X-C chemokine receptor type 4Homo sapiens (human)
positive regulation of cold-induced thermogenesisC-X-C chemokine receptor type 4Homo sapiens (human)
response to tacrolimusC-X-C chemokine receptor type 4Homo sapiens (human)
positive regulation of dendrite extensionC-X-C chemokine receptor type 4Homo sapiens (human)
positive regulation of vasculature developmentC-X-C chemokine receptor type 4Homo sapiens (human)
positive regulation of mesenchymal stem cell migrationC-X-C chemokine receptor type 4Homo sapiens (human)
response to ultrasoundC-X-C chemokine receptor type 4Homo sapiens (human)
positive regulation of macrophage migration inhibitory factor signaling pathwayC-X-C chemokine receptor type 4Homo sapiens (human)
neurogenesisC-X-C chemokine receptor type 4Homo sapiens (human)
cell chemotaxisC-X-C chemokine receptor type 4Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationC-X-C chemokine receptor type 4Homo sapiens (human)
immune responseC-X-C chemokine receptor type 4Homo sapiens (human)
brain developmentC-X-C chemokine receptor type 4Homo sapiens (human)
calcium-mediated signalingC-X-C chemokine receptor type 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (13)

Processvia Protein(s)Taxonomy
virus receptor activityC-X-C chemokine receptor type 4Homo sapiens (human)
actin bindingC-X-C chemokine receptor type 4Homo sapiens (human)
G protein-coupled receptor activityC-X-C chemokine receptor type 4Homo sapiens (human)
protein bindingC-X-C chemokine receptor type 4Homo sapiens (human)
coreceptor activityC-X-C chemokine receptor type 4Homo sapiens (human)
C-X-C chemokine receptor activityC-X-C chemokine receptor type 4Homo sapiens (human)
C-C chemokine bindingC-X-C chemokine receptor type 4Homo sapiens (human)
ubiquitin protein ligase bindingC-X-C chemokine receptor type 4Homo sapiens (human)
myosin light chain bindingC-X-C chemokine receptor type 4Homo sapiens (human)
small molecule bindingC-X-C chemokine receptor type 4Homo sapiens (human)
C-X-C motif chemokine 12 receptor activityC-X-C chemokine receptor type 4Homo sapiens (human)
ubiquitin bindingC-X-C chemokine receptor type 4Homo sapiens (human)
C-C chemokine receptor activityC-X-C chemokine receptor type 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (12)

Processvia Protein(s)Taxonomy
lysosomeC-X-C chemokine receptor type 4Homo sapiens (human)
early endosomeC-X-C chemokine receptor type 4Homo sapiens (human)
cytoplasmC-X-C chemokine receptor type 4Homo sapiens (human)
lysosomeC-X-C chemokine receptor type 4Homo sapiens (human)
early endosomeC-X-C chemokine receptor type 4Homo sapiens (human)
late endosomeC-X-C chemokine receptor type 4Homo sapiens (human)
plasma membraneC-X-C chemokine receptor type 4Homo sapiens (human)
cell surfaceC-X-C chemokine receptor type 4Homo sapiens (human)
cell leading edgeC-X-C chemokine receptor type 4Homo sapiens (human)
cytoplasmic vesicleC-X-C chemokine receptor type 4Homo sapiens (human)
extracellular exosomeC-X-C chemokine receptor type 4Homo sapiens (human)
anchoring junctionC-X-C chemokine receptor type 4Homo sapiens (human)
protein-containing complexC-X-C chemokine receptor type 4Homo sapiens (human)
external side of plasma membraneC-X-C chemokine receptor type 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (9)

Assay IDTitleYearJournalArticle
AID604431Antiinflammatory activity in C57BL/6L mouse assessed as inhibition of carrageenan-induced paw edema at 300 ug/kg, ip administered 30 mins before carrageenan challenge measured after 76 hrs2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Dipyrimidine amines: a novel class of chemokine receptor type 4 antagonists with high specificity.
AID303361Cytotoxicity against MDA-MB-231 cells2007Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23
Discovery of small molecule CXCR4 antagonists.
AID303362Selectivity index, ratio of IC50 for CXCR4 to CC50 for MDA-MB-231 cells2007Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23
Discovery of small molecule CXCR4 antagonists.
AID604437Protection against bleomycin-induced lung injury in mouse assessed as decrease in alveolar structural distortion at 300 ug/kg, ip administered 1 day before bleomycin treatment and daily for 20 days by hematoxylin and eosin staining2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Dipyrimidine amines: a novel class of chemokine receptor type 4 antagonists with high specificity.
AID604441Antimetastatic activity against HGF/TGF-beta/CXCR4/MMP2 expressing human OMM 2.3 cells xenografted in nude mouse eye assessed as decrease in number of hepatic micrometastases at 300 ug/kg, ip administered 3 days after tumor implantation QD for 28 days by 2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Dipyrimidine amines: a novel class of chemokine receptor type 4 antagonists with high specificity.
AID604436Protection against bleomycin-induced lung injury in mouse assessed as decrease in interstitial structural distortion at 300 ug/kg, ip administered 1 day before bleomycin treatment and daily for 20 days by hematoxylin and eosin staining2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Dipyrimidine amines: a novel class of chemokine receptor type 4 antagonists with high specificity.
AID303360Inhibition of CXCR4 in MDA-MB-231 cells2007Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23
Discovery of small molecule CXCR4 antagonists.
AID604439Protection against bleomycin-induced lung injury in mouse assessed as decrease in lung fibrosis at 300 ug/kg, ip administered 1 day before bleomycin treatment and daily for 20 days by hematoxylin and eosin staining2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Dipyrimidine amines: a novel class of chemokine receptor type 4 antagonists with high specificity.
AID604433Antiangiogenic activity against human MDA-MB-231 cells xenografted in nude mouse assessed as hemoglobin level at 300 ug/kg, sc measured after 10 days by ELISA based madrigal plug assay2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Dipyrimidine amines: a novel class of chemokine receptor type 4 antagonists with high specificity.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (20)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's10 (50.00)29.6817
2010's9 (45.00)24.3611
2020's1 (5.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (5.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other19 (95.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]