Target intelligence / Profile preview

Platelet-derived growth factor BB and AB (PDGF-BB/PDGF-AB)

Target
PDGF-BB/PDGF-AB
Molecular classification
Growth factor, Cytokine, Receptor ligand
01

Overview

Platelet-derived growth factor BB (PDGF-BB) and AB (PDGF-AB) are dimeric isoforms of the Platelet-derived growth factor (PDGF) family, serving as potent mitogens for mesenchymal cells such as fibroblasts and smooth muscle cells [2, 4]. PDGF-BB is a homodimer of two B-chains, while PDGF-AB is a heterodimer of A and B chains; both are released by platelets upon activation and play vital roles in wound healing, angiogenesis, and embryonic development [4, 5]. These ligands function by binding to and inducing the dimerization of PDGF receptors (PDGFR-alpha and PDGFR-beta), triggering intracellular signaling cascades like the MAPK and PI3K pathways [1, 17]. In clinical medicine, recombinant PDGF-BB (Becaplermin) is used topically to treat chronic diabetic foot ulcers by stimulating tissue repair [5, 11]. Conversely, overproduction or genetic rearrangements of the PDGFB gene, such as the COL1A1-PDGFB fusion in dermatofibrosarcoma protuberans, drive pathological cell proliferation and are therapeutic targets for tyrosine kinase inhibitors [1, 9].

Other names
Platelet-derived growth factor B chainPDGF-BPDGF-2c-SisBecaplerminProto-oncogene c-Sis
02

Mechanism of action

Binding to and activation of PDGF receptor-alpha and PDGF receptor-beta, leading to receptor dimerization, autophosphorylation, and activation of downstream signaling pathways such as MAPK, PI3K/Akt, and PLC-gamma.

03

Biological functions

Cell proliferationCell migrationAngiogenesisWound healingChemotaxisEmbryonic developmentMesenchymal cell mitogenesis
04

Disease associations

CancerFibrosisAtherosclerosisDiabetic ulcerNeurodegenerative diseaseCardiovascular disease
05

Safety considerations

Potential for tumor promotion with chronic exogenous administrationVascular calcification associated with high systemic levelsDermal irritation at application sitesIncreased risk of cancer mortality (historical black box warning for high-dose topical use)
06

Interacting drugs

Becaplermin

1 more in the full profile.

07

Biomarkers

PDGF-BB serum levelsCOL1A1-PDGFB fusion genePDGFB gene mutationsPDGF-BB urinary levels (arsenic exposure risk)

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