Design Strategies, Structures and Molecular Interactions of Small Molecule Src Inhibitors

Anti-cancer Agents in Medicinal Chemistry
Sureyya Olgen

Abstract

In recent years, several small molecules approved by FDA for clinical studies are promising anti-cancer agent. Among the kinases, Abelson Leukaemia (Abl), sarcoma (Src), epidermal growth factor receptor (EGFR) and vascular endotelhial growth factor receptor (VEGFR) are considered as primary molecular targets for selective inhibition and the best successful targeted therapy of tyrosine kinase inhibitors (TKIs) has been achieved in the treatment of Bcr (break point cluster)-Abl leukemia. The majority of type 1 kinase inhibitors target the active conformation of ATP binding site. In consequence of intensive studies on kinases, type 2, type 3 (allosteric) and type 4 (covalent) inhibitors have been discovered beyond the type 1 inhibitors. Although the selectivity is a major problem for type 1 inhibitors, these new type of inhibitors are promising for finding new selective compounds, which may provide other therapeutic options for cancer therapy. They may also be a solution to overcome drug resistance that remains unresolved yet. Threedimensional structural determination provides the development of specific and highly binding properties of compounds. Studying the prediction of a binding mode of inhibitors, homology model developments...Continue Reading

Citations

Sep 12, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Yi ZhangFan-Hao Meng
Jan 30, 2019·Nature Reviews. Nephrology·Patrick Ming-Kuen TangHui-Yao Lan
Dec 15, 2020·Investigational New Drugs·Mohamed E M SaeedThomas Efferth

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