Non-fucosylated Anti-Human PDGFRA (Olaratumab) Therapeutic Antibody (CAT#: BioBet-016ZP) Datasheet

PDGFRA

platelet derived growth factor receptor alpha

This gene encodes a cell surface tyrosine kinase receptor for members of the platelet-derived growth factor family. These growth factors are mitogens for cells of mesenchymal origin. The identity of the growth factor bound to a receptor monomer determines whether the functional receptor is a homodimer or a heterodimer, composed of both platelet-derived growth factor receptor alpha and beta polypeptides. Studies suggest that this gene plays a role in organ development, wound healing, and tumor progression. Mutations in this gene have been associated with idiopathic hypereosinophilic syndrome, somatic and familial gastrointestinal stromal tumors, and a variety of other cancers.

Platelet Derived Growth Factor Receptor Alpha; Platelet-Derived Growth Factor Receptor, Alpha Polypeptide; Alpha-Type Platelet-Derived Growth Factor Receptor; Platelet-Derived Growth Factor Receptor 2; CD140 Antigen-Like Family Member A; CD140a Antigen; PDGF-R-Alpha; EC 2.7.10.1; PDGFR-2;

Plasma membrane, Golgi apparatus

Diseases associated with PDGFRA include Gist-Plus Syndrome and Hypereosinophilic Syndrome, Idiopathic.

Its related pathways are RET signaling and Phospholipase D signaling pathway.

Tyrosine protein kinase, as the cell surface receptor of PDGFA, PDGFB and PDGFC, plays an important role in regulating embryonic development, cell proliferation, survival and chemotaxis. According to specific conditions, promote or inhibit cell proliferation and cell migration. It plays an important role in the differentiation of bone marrow mesenchymal stem cells. Necessary for normal bone development and cephalic closure during embryonic development. It is necessary for the normal development of the gastrointestinal mucosa, the recruitment of mesenchymal cells and the normal development of intestinal villi. It plays a role in cell migration and chemotaxis in wound healing. Play a role in platelet activation, platelet granule agonist secretion and thromboxane-induced platelet aggregation. The combination of its homo-ligand-homodimer PDGFA, homodimer PDGFB, heterodimer or homodimer PDGFC formed by PDGFA and PDGFB-leads to the activation of multiple signal cascades; the response depends on the binding The nature of the ligand is regulated by the formation of heterodimers between PDGFRA and PDGFRB. Phosphorylate PIK3R1, PLCG1 and PTPN11. Activation of PLCG1 leads to the production of cell signaling molecules diglyceride and inositol 1,4,5-trisphosphate, mobilization of cytosolic calcium (2+) and activation of protein kinase c to phosphorylate PIK3R1, the regulatory subunit of phosphatidylinositol 3- kinase, which mediates the activation of the AKT1 signaling pathway. Mediates the activation of HRAS and MAPK1/ERK2 and/or MAPK3/ERK1. Promote the activation of STAT family members STAT1, STAT3, STAT5A and/or STAT5B. Receptor signaling is down-regulated by protein phosphatase (dephosphorylation of the receptor and its downstream effectors) and rapid internalization of activated receptors.

Cancer antibody; Cell Biology and Cellular Response antibody; Signaling Transduction antibody

1.N-glycosylated. 2.Ubiquitinated, leading to its degradation. 3.Autophosphorylated on tyrosine residues upon ligand binding. Autophosphorylation occurs in trans, i.e. one subunit of the dimeric receptor phosphorylates tyrosine residues on the other subunit. Phosphorylation at Tyr-731 and Tyr-742 is important for interaction with PIK3R1. Phosphorylation at Tyr-720 and Tyr-754 is important for interaction with PTPN11. Phosphorylation at Tyr-762 is important for interaction with CRK. Phosphorylation at Tyr-572 and Tyr-574 is important for interaction with SRC and SRC family members. Phosphorylation at Tyr-988 and Tyr-1018 is important for interaction with PLCG1.

Protein Based Therapies
Monoclonal antibody (mAb)

IgG1

Olaratumab

Human

Human

Olaratumab is a fully human IgG1 monoclonal antibody that targets platelet-derived growth factor receptor alpha. It was developed by Eli Lilly and was approved in October 2016 (as Lartruvo) as the initial treatment for certain types of soft tissue sarcoma (STS) adults. Studies have shown that combining olaratumab with adriamycin can significantly reduce the proliferation of cancer cells and tumor growth.

Soft Tissue Sarcoma (STS)

IMC-3G3, LY-3012207

PDGFR signaling is a tyrosine kinase-mediated pathway that normally regulates cell growth, chemotaxis, and mesenchymal stem cell differentiation. Olaratumab is a fully human IgG1 monoclonal antibody with antitumor activity and can selectively bind to the outer domain of human platelet-derived growth factor receptor (PDGFR) -α with high affinity. Olaratumab blocks ligand-induced tumor cell proliferation and inhibits receptor autophosphorylation and ligand-induced phosphorylation of downstream signaling molecules protein kinase B (Akt) and mitogen-activated protein kinase 5.

Olaratumab in combination with adriamycin for the treatment of adult patients with advanced or metastatic soft tissue sarcoma (STS) of histological subtype