CTCE-0214

This drug entry is a stub and has not been fully annotated. It is scheduled to be annotated soon.

Identification

Generic Name
CTCE-0214
DrugBank Accession Number
DB05934
Background

CTCE-0214 is a stable peptide agonist of stromal cell-derived factor-1 (SDF-1), a key signaling molecule in the proliferation, homing, engraftment and expansion of hematopoietic stem cells and white blood cells.

Type
Small Molecule
Groups
Investigational
Synonyms
Not Available
External IDs
  • CT-0214
  • CTCE 0214
  • CTCE-0214

Pharmacology

Indication

Investigated for use/treatment in adverse effects (chemotherapy), blood (blood forming organ disorders, unspecified), cancer/tumors (unspecified), neutropenics, and vascular diseases.

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Contraindications & Blackbox Warnings
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Pharmacodynamics

Not Available

Mechanism of action

CTCE-0214 mimics the activity of the natural chemokine SDF-1 by increasing the level of white blood cells (neutrophils), bleeding prevention cells (platelets) and stem cells (primitive blood forming cells) in the blood. SDF-1 is also believed to work as a traffic controller for infection-fighting white blood cells and progenitor cell migration providing an essential function to combat immunosuppression.

TargetActionsOrganism
UStromal cell-derived factor 1Not AvailableHumans
Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism
Not Available
Route of elimination

Not Available

Half-life

Not Available

Clearance

Not Available

Adverse Effects
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Toxicity

Not Available

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Not Available
Food Interactions
Not Available

Categories

Drug Categories
Classification
Not classified
Affected organisms
Not Available

Chemical Identifiers

UNII
VOY9490C9O
CAS number
577782-52-6

References

General References
  1. Faber A, Roderburg C, Wein F, Saffrich R, Seckinger A, Horsch K, Diehlmann A, Wong D, Bridger G, Eckstein V, Ho AD, Wagner W: The many facets of SDF-1alpha, CXCR4 agonists and antagonists on hematopoietic progenitor cells. J Biomed Biotechnol. 2007;2007(3):26065. Epub 2007 Apr 23. [Article]
  2. Li K, Chuen CK, Lee SM, Law P, Fok TF, Ng PC, Li CK, Wong D, Merzouk A, Salari H, Gu GJ, Yuen PM: Small peptide analogue of SDF-1alpha supports survival of cord blood CD34+ cells in synergy with other cytokines and enhances their ex vivo expansion and engraftment into nonobese diabetic/severe combined immunodeficient mice. Stem Cells. 2006 Jan;24(1):55-64. Epub 2005 Aug 25. [Article]
  3. Perez LE, Alpdogan O, Shieh JH, Wong D, Merzouk A, Salari H, O'Reilly RJ, van den Brink MR, Moore MA: Increased plasma levels of stromal-derived factor-1 (SDF-1/CXCL12) enhance human thrombopoiesis and mobilize human colony-forming cells (CFC) in NOD/SCID mice. Exp Hematol. 2004 Mar;32(3):300-7. [Article]
Not Available

Clinical Trials

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Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
Not Available
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available
Chromatographic Properties
Collision Cross Sections (CCS)
Not Available

Targets

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Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Chemoattractant active on T-lymphocytes and monocytes but not neutrophils. Activates the C-X-C chemokine receptor CXCR4 to induce a rapid and transient rise in the level of intracellular calcium ions and chemotaxis. SDF-1-beta(3-72) and SDF-1-alpha(3-67) show a reduced chemotactic activity. Binding to cell surface proteoglycans seems to inhibit formation of SDF-1-alpha(3-67) and thus to preserve activity on local sites. Also binds to atypical chemokine receptor ACKR3, which activates the beta-arrestin pathway and acts as a scavenger receptor for SDF-1. Binds to the allosteric site (site 2) of integrins and activates integrins ITGAV:ITGB3, ITGA4:ITGB1 and ITGA5:ITGB1 in a CXCR4-independent manner (PubMed:29301984). Acts as a positive regulator of monocyte migration and a negative regulator of monocyte adhesion via the LYN kinase. Stimulates migration of monocytes and T-lymphocytes through its receptors, CXCR4 and ACKR3, and decreases monocyte adherence to surfaces coated with ICAM-1, a ligand for beta-2 integrins. SDF1A/CXCR4 signaling axis inhibits beta-2 integrin LFA-1 mediated adhesion of monocytes to ICAM-1 through LYN kinase. Inhibits CXCR4-mediated infection by T-cell line-adapted HIV-1. Plays a protective role after myocardial infarction. Induces down-regulation and internalization of ACKR3 expressed in various cells. Has several critical functions during embryonic development; required for B-cell lymphopoiesis, myelopoiesis in bone marrow and heart ventricular septum formation. Stimulates the proliferation of bone marrow-derived B-cell progenitors in the presence of IL7 as well as growth of stromal cell-dependent pre-B-cells (By similarity)
Specific Function
chemokine activity
Gene Name
CXCL12
Uniprot ID
P48061
Uniprot Name
Stromal cell-derived factor 1
Molecular Weight
10665.75 Da

Drug created at November 18, 2007 18:28 / Updated at June 12, 2020 16:52