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Identification
Name Becaplermin
Accession Number DB00102 (BIOD00053, BTD00053)
Type biotech
Groups approved
Description

Becaplermin is produced by recombinant DNA technology by insertion of the gene for the B chain of platelet derived growth factor (PDGF) into the yeast, Saccharomyces cerevisiae. Becaplermin has a molecular weight of approximately 25 KD and is a homodimer composed of two identical polypeptide chains that are bound together by disulfide bonds
Protein structure Db00102
Display: 3D Structure
Protein chemical formula C532H892N162O153S9
Protein average weight 12294.4000
Sequences 
>DB00102 sequence
SLGSLTIAEPAMIAECKTRTEVFEISRRLIDRTNANFLVWPPCVEVQRCSGCCNNRNVQC
RPTQVQLRPVQVRKIEIVRKKPIFKKATVTLEDHLACKCETVAAARPVT

FASTA
Synonyms
c-sis
PDGF B-chain
PDGF-2
Platelet-derived growth factor B chain precursor
Platelet-derived growth factor beta polypeptide
Salts Not Available
Brand names
Name Company
Regranex
Regranex (OMJ Pharmaceuticals)
Brand mixtures Not Available
Categories
  • Anti-Ulcer Agents
  • Topical
CAS number 165101-51-9
Taxonomy
Kingdom Not Available
Classes Not Available
Substructures Not Available
Pharmacology
Indication For topical treatment of skin ulcers (from diabetes)
Pharmacodynamics Used for the topical treatment of skin ulcers, Regranex has a biological activity similar to that of endogenous platelet-derived growth factor, which includes promoting the chemotactic recruitment and proliferation of cells involved in wound repair and enhancing the formation of granulation tissue.
Mechanism of action Binds to the beta platelet-derived growth factor (PDGF) receptor, a tyrosine kinase receptor. PDGF is known to exist as a dimer, and activates its signaling pathway by a ligand induced receptor dimerization and autophosphorylation. PDGF receptors also contain many auto-phosphorylation sites, which serve to mediate binding of SH2 sites and subsequently signal corresponding pathways. There are five different isoforms of PDGF that activate through two different receptors (alpha and beta).
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
Toxicity Not Available
Affected organisms
  • Humans and other mammals
Pathways Not Available
Pharmacoeconomics
Manufacturers Not Available
Packagers
Dosage forms
Form Route Strength
Gel Topical
Prices
Unit description Cost Unit
Regranex 0.01% Gel 15 gm Tube 723.82 USD tube
Regranex 0.01% gel 46.4 USD g
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Country Patent Number Approved Expires (estimated)
Canada 1340846 1999-12-07 2015-12-15
Properties
State liquid
Experimental Properties
Property Value Source
hydrophobicity -0.160 Not Available
isoelectric point 9.38 Not Available
References
Synthesis Reference Not Available
General Reference Not Available
External Links
Resource Link
UniProt P01127 Link_out
Genbank K01401 Link_out
PharmGKB PA164749511 Link_out
Drug Product Database 2239405 Link_out
RxList http://www.rxlist.com/cgi/generic2/becapler.htm Link_out
Drugs.com http://www.drugs.com/cdi/becaplermin.html Link_out
Wikipedia http://en.wikipedia.org/wiki/Becaplermin Link_out
ATC Codes
  • D03AX06
  • A01AD08
AHFS Codes
  • 84:16.00
PDB Entries
FDA label show (248 KB)
MSDS Not Available
Interactions
Drug Interactions Searched, but no interactions found.
Food Interactions Not Available
Targets

1. Beta platelet-derived growth factor receptor

Pharmacological action: yes

Receptor that binds specifically to PDGFB and PDGFD and has a tyrosine-protein kinase activity. Phosphorylates Tyr residues at the C-terminus of PTPN11 creating a binding site for the SH2 domain of GRB2

Organism class: human
UniProt ID: P09619 Link_out
Gene: PDGFRB Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Papanas N, Maltezos E: Becaplermin gel in the treatment of diabetic neuropathic foot ulcers. Clin Interv Aging. 2008;3(2):233-40. Pubmed

2. Alpha platelet-derived growth factor receptor

Pharmacological action: unknown

Receptor that binds both PDGFA and PDGFB and has a tyrosine-protein kinase activity

Organism class: human
UniProt ID: P16234 Link_out
Gene: PDGFRA Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Abdiu A, Walz TM, Nishikawa BK, Wingren S, Larsson SE, Wasteson A: Human malignant fibrous histiocytomas in vitro: growth characteristics and their association with expression of mRNA for platelet-derived growth factor, transforming growth factor-alpha and their receptors. Eur J Cancer. 1998 Dec;34(13):2094-100. Pubmed
  2. Ebert M, Yokoyama M, Friess H, Kobrin MS, Buchler MW, Korc M: Induction of platelet-derived growth factor A and B chains and over-expression of their receptors in human pancreatic cancer. Int J Cancer. 1995 Sep 4;62(5):529-35. Pubmed
  3. Miller-Kasprzak E, Niemir ZI, Czekalski S: [Structure and function of PDGF-R-alpha and its expression in normal kidney and kidney diseases] Przegl Lek. 2002;59(10):826-31. Pubmed
  4. Heidaran MA, Pierce JH, Lombardi D, Ruggiero M, Gutkind JS, Matsui T, Aaronson SA: Deletion or substitution within the alpha platelet-derived growth factor receptor kinase insert domain: effects on functional coupling with intracellular signaling pathways. Mol Cell Biol. 1991 Jan;11(1):134-42. Pubmed
  5. Yu J, Liu XW, Kim HR: Platelet-derived growth factor (PDGF) receptor-alpha-activated c-Jun NH2-terminal kinase-1 is critical for PDGF-induced p21WAF1/CIP1 promoter activity independent of p53. J Biol Chem. 2003 Dec 5;278(49):49582-8. Epub 2003 Sep 23. Pubmed

3. Alpha-2-macroglobulin

Pharmacological action: unknown

Is able to inhibit all four classes of proteinases by a unique 'trapping' mechanism. This protein has a peptide stretch, called the 'bait region' which contains specific cleavage sites for different proteinases. When a proteinase cleaves the bait region, a conformational change is induced in the protein which traps the proteinase. The entrapped enzyme remains active against low molecular weight substrates (activity against high molecular weight substrates is greatly reduced). Following cleavage in the bait region a thioester bond is hydrolyzed and mediates the covalent binding of the protein to the proteinase

Organism class: human
UniProt ID: P01023 Link_out
Gene: A2M Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Lizonova A, Bizik J, Grofova M, Vaheri A: Coexpression of tumor-associated alpha 2-macroglobulin and growth factors in human melanoma cell lines. J Cell Biochem. 1990 Aug;43(4):315-25. Pubmed
  2. Bonner JC, Osornio-Vargas AR: Differential binding and regulation of platelet-derived growth factor A and B chain isoforms by alpha 2-macroglobulin. J Biol Chem. 1995 Jul 7;270(27):16236-42. Pubmed
Comments
Drug created on June 13, 2005 07:24 / Updated on September 03, 2011 16:08