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Review Article

Small Molecule Antagonists Targeting Growth Factors/Receptors

[ Vol. 3 , Issue. 3 ]

Author(s):

Dajun Yang* and Shaomeng Wang   Pages 335 - 354 ( 20 )

Abstract:


Control of cell proliferation is regulated by interaction of soluble growth factors and cell membrane receptors. Studies of growth factors and their receptors provide a new approach to elucidate mechanisms of cancer progression, and more importantly, a unique potential for development of targeted anticancer therapy. A growth factor (ligand) binding to its receptor(s) triggers a complex series of intracellular signaling pathways that may culminate in a change in cell behavior. Considerable number of studies indicate that the inappropriate expression and/or activation of the growth factor/receptors can mediate abnormal cellular signaling and oncogenic transformation both in vitro and in vivo system. These results strongly support the hypothesis that growth factors/receptors plays an important role in the tumorigenesis of cancer.

A number of families of structurally related growth factors and receptors have been identified and were considered as potential targets for specific antitumor therapy. This review will focus on recent advances in drug discovery that have identified small organic molecules that affect ligand binding, kinase activity, and signaling transduction and alter cell function. Recent progress of small molecule-based drug discovery targeting several growth factor/receptor families is presented. Approach utilizing computer based 3D pharmacophore searches is discussed. These approaches to develop novel anticancer therapies focus on mechanisms different from conventional chemotherapeutic and radiotherapeutic regimens. These targeted anticancer therapies may be highly tumor cell specific, since they do not require host accessory factors. Furthermore, these potential small molecule drugs may have the capacity to synergistically or additively improve the presently available hormonal, radiation or chemotherapy of cancer.

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