Platelet-derived growth factor (PDGF) and its receptor (PDGFR) have multiple biological functions. They can form both heterodimers and homodimers. Ligand binding promotes receptor dimerization, autophosphorylation, and activation of multiple downstream intracellular signaling cascades. These cascades stimulate processes such as actin filament rearrangement, gap junction communication disruption, gene transcription initiation, and cell survival. They play key roles in regulating cell proliferation, differentiation, growth, development, and many diseases, including cancer. Based on the diverse activities of PDGFR, a number of anti-PDGFR antibodies have been developed. They play a significant role in the treatment of cancer and other diseases. Based on our rich field experience and advanced technology platform, Creative Biolabs provides comprehensive services for custom agonistic antibody and agonistic autoantibody discovery to support agonistic antibody therapy development.

Fig 1. Platelet-derived growth factor receptor A protein.

Anti-PDGFR Antibody

PDGF is a pro-angiogenic factor. It is a potent mitogen and important vascular growth factor for a variety of mesenchymal cells, such as fibroblasts, vascular smooth muscle cells, glomerular vascular cells, glial cells, and endothelial cells. PDGF is generally produced by platelets, histiocytes, and some tumor cells. PDGFR, on the other hand, is a member of the receptor tyrosine protein kinase family that promotes cell chemotaxis, division, and proliferation. It plays an active and important role in the growth and development of the body, trauma repair, and other physiological processes. PDGF and PDGFR are closely related to the occurrence and development of cancer. Their binding triggers the formation of a dimerization complex of the receptor, which phosphorylates the receptor and activates downstream signaling molecules to produce a series of biological effects. This, in turn, induces the formation of tumor neovascularization, which directly or indirectly promotes tumor cell proliferation and migration.

PDGFR is a receptor tyrosine kinase transmembrane glycoprotein dimerization molecule. It is found in a wide range of cells, including normal endothelial, smooth muscle, and fibroblast cells, as well as neuronal cells, and is highly expressed in a variety of human tumor cells. PDGFR consists of two structurally similar receptor isoforms, PDGFR-alpha and PDGFR-beta. The ligand molecule of the dimer causes the receptor molecule to form a homodimer or heterodimer with the receptor molecule. The receptor dimer results from the autophosphorylation and activation of receptor tyrosine kinase by the PDGFR. Specific binding of PDGF to the receptor results in receptor dimerization, leading to receptor autophosphorylation and activation of receptor tyrosine kinases, which activate intracellular signaling pathways by exposing tyrosine residues to SH2 domain and PTB domain binding sites and substrate protein molecules.

The PDGF/PDGFR signaling pathway is closely associated with a variety of diseases, like fibrotic diseases. Fibrosis is a repair response that occurs after tissue injury. It is characterized by a massive deposition of extracellular matrix resulting from the activation of fibroblasts. Moderate repair after tissue injury is beneficial, but when injured tissue is over-repaired, fibrotic disease occurs. The PDGF/PDGFR signaling pathway is involved in fibrotic pathological processes, including myocardial fibrosis, renal fibrosis, hepatic fibrosis, and dermatofibrosis. PDGFs promote the proliferation and differentiation of fibroblasts, collagen production, and cell adhesion, and are involved in the development of fibrotic disease. The activation of PDGFR promotes downstream signaling, which is involved in the regulation of extracellular matrix production and promotes the development of fibrotic diseases. And anti-PDGFR antibodies can treat fibrotic diseases from two perspectives. On the one hand, anti-PDGF neutralizing antibodies isolate the ligand and impede ligand-receptor binding. On the other hand, there is the development of PDGFR receptor-specific blocking antibodies. In addition, PDGFR plays an equally important role in tumorigenesis and development.

Tumor growth is angiogenesis-dependent, and tumor cells can produce a variety of pro-angiogenic factors, which play an important role in tumorigenesis, progression, invasion, and metastasis. PDGF is one of the important factors for angiogenesis, and in a variety of tumors, the expression of PDGF is closely correlated with the angiogenesis of tumors. Tumor cells are pro-angiogenic through the release of PDGF, and PDGF also upregulates the expression of vascular endothelial growth factor (VEGF), which is also an important pro-angiogenic factor that indirectly mediates angiogenesis. Currently, anti-PDGFR antibodies for cancer therapy are hotly researched. They inhibit cancer development by blocking PDGFR, thus inhibiting cancer development.

Creative Biolabs has a wealth of knowledge and experience in custom agonistic autoantibody. We would be happy to share with you our knowledge and experience in anti-PDGFR antibodies by phage display.

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