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G protein-coupled receptors (GPCRs), which transduce extracellular signals into intracellular effector pathways by the activation of heterotrimeric G proteins, include around 900 members, representing the most prominent family of validated pharmacological targets in biomedicine. Both orphan and well-characterized GPCRs have been linked to cancer development, starting with the discovery in 1986 of the oncogene MAS, which encodes a functional GPCR for which the endogenous ligand is ANG1–7. Moreover, diverse GPCRs were found to be overexpressed in primary and metastatic tumor cells of head and neck squamous cell carcinoma (HNSCC), non-small cell lung cancer, breast, prostate and gastric tumors, melanoma and diffused large B cell lymphoma.
Further evidence confirmed that GPCRs are involved in the initiation and/or progression of cancer. For example, various GPCRs such as chemokines, thrombin, lysophosphatidic acid (LPA), gastrin-releasing peptide, endothelin and prostaglandin receptors have a key role in angiogenesis and metastasis as well as in inflammation-associated cancer. In addition, constitutively active GPCRs can be expressed from the genomes of human oncogenic viruses.
As more and more studies linking GPCRs to cancer emerge, the pharmacological manipulation of these receptors has become increasingly attractive for the development of novel strategies to target tumor progression and metastasis. Creative Biogene can offer a variety of GPCR related products including stable cell lines, viral particles and clones for your drug discovery projects in cancer.
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