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Cytoskeleton consists of microfilament, microtubules and intermediate filaments. Microfilament determines the surface characteristics of the cells, enabling the cells to move and contract. Microtubules determine the position of the membranous organelles (membrane-enclosed organelle) and as the rail of the vesicular transport. Intermediate fiber makes the cells to have tension and anti-shear forces. Since the cytoskeleton is involved in virtually all cellular processes, abnormalities in this essential cellular component frequently result in disease. Drugs that modulate microtubule stability, inhibitors of posttranslational modifications of cytoskeletal components, specifically compounds affecting the levels of tubulin acetylation, and compounds targeting signaling molecules which regulate cytoskeleton dynamics, constitute the mostly addressed therapeutic interventions for the diseases including cancer and neurodegenerative disorders.