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EGFR family involved in cancer by kate edson
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EGFR family involved in cancer |
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Education
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EGFR family involved in cancer It is well known that epidermal growth factor receptors (EGFR or ErbB/Her) belong to the receptor tyrosine kinase superfamily. The EGFR subclass consisted of four closely related members: EGFR/ErbB1/Her1, ErbB2/Her2/Neu, ErbB3/Her3, ErbB4/Her4. Formation of homodimers or heterodimers of ErbB receptors is induced after binding to EGF-related growth factors. Upon activation, autophosphorylation of tyrosine residues within the cytoplasmic domains of EGFR/ErbB receptors induce intracellular signaling transduction pathways, including the phosphatidylinosithol-3-kinase (PI3K) signaling pathway, the Shc- and/or Grb2-mediated mitogen-activated protein kinase (MAPK)-ERK1/2 signlaing pathway(s), the protein kinase C (PKC) signaling pathway, and other signaling pathways implicated in proliferation response. Because of the pivotal roles of aberrant EGFR signaling pathways in the development of different kinds of malignant human cancers, the receptor tyrosine kinase superfamily is well-studied. Overexpression of ErbB2 is verified in about 30% of breast cancer patients and is associated with poor prognosis. Among the ErbB receptors, ErbB2 lacks its own ligands; therefore, ErbB2 forms heterodimers with EGFR, ErbB3 or ErbB4, or even with other family members, such as Insulin-like growth factor-1 receptor (IGF-1R). Findings such as these suggest that the ErbBs may be good molecular targets for various malignancies, including breast cancer.[1] Tyrosine kinase inhibitor: lapatinib Lapatinib (Tykerb or GW-572016), like imatinib and gefitinib, is also a small-molecule, tyrosine kinase inhibitor which targets both ErbB1 and ErbB2. Due to its specificity to EGFR family members, applicability to oral administration, and seemingly few adverse effects, lapatinib has received considerable attention and is undergoing clinical trials for treatment of various solid tumors, including breast, head and neck, vulva, colon, prostate, and stomach. Lapatinib shows promise as a therapy in combination with capecitabine for patients with Her2-overexpressing advanced or metastatic breast cancer that fails to respond to anthracycline, taxane, and the anti-Her2 monoclonal antibody transtuzumab. As yet, however, no hematological malignancies have been included in laboratory or clinical investigations of lapatinib. To date, agents possessing cytotoxicity, targeted therapeutic activity and differentiation-inducing capacity have proven most effective for treating leukemia, the most common hematological cancer.[2] Chronic myelogenous leukemia Chronic myelogenous leukemia (CML) is a clonal disease characterized by the presence of the Philadelphia chromosome and resultant BCR-Abl gene fusion with constitutively active tyrosine kinase in >90% of patients. CML cells generating BCR-Abl fusion protein, such as the K562 cell line, are important experimental models because they allow the assessment of multiple cellular and molecular events simultaneously, including various modes of cell death, differentiation toward the erythroid/macrophage/megakaryocyte lineages, and downegulation of BCR-Abl tyrosine kinase.In recent years, molecular target-based cancer therapy has been successfully applied to improve the efficacy and ameliorate the adverse effects of several conventional chemotherapeutic drugs. The pharmacological activities of novel targeted therapeutics may not be limited to currently recognized targets. For example, the EGFR inhibitor erlotinib overcame drug resistance, and PKC412 gave rise to megakaryocytic differentiation in K562 cells. Lapatinib caused multiple cellular events simultaneously including apoptosis, autophagic cell death, and megakaryocytic differentiation in human CML K562 cells. Apoptosis was likely triggered by a caspase-dependent pathway and autophagic cell death was likely induced via an ATG6-dependent pathway. We has established long-term and stable relationships with more than 10,000 customers from pharmaceutical and biotech companies, universities and research institutions. We have high quality inhibitors like Capecitabine, Lenalidomide, FTY720 & more. We have headquarters in both United States and Europe, and also has 38 distributors worldwide. We provide overnight delivery in North America and Europe.
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