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Small Molecule Inhibitors

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The Molecular Basis of Human Cancer

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Abstract

Before the biomedical community had had any understanding of the molecular mechanisms that drive tumorigenesis, the discovery of cancer chemotherapy exclusively focused on the development of novel cytotoxic compounds targeting DNA processing and cell division including DNA alkylating and cross-linking agents, antimetabolites, topoisomerase inhibitors, and anti-tubulin agents. Although these drugs can be very efficacious in killing tumor cells, serious side effects accompanied due to the lack of selectivity for tumor cells versus normal cells. The side effects, such as bone marrow suppression and gastrointestinal, cardiac, hepatic, and renal toxicities, significantly limit their use. In addition, drug resistance was frequently observed after initial stabilization or regression of the disease.

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Authors and Affiliations

  1. Department of Pharmacology, School of Medicine, University of North Carolina at Chapel Hill, 120 Mason Farm Road, Chapel Hill, NC, 27599, USA

    Xin Chen Ph.D.

  2. Departments of Structural and Chemical Biology, Oncological Sciences, and Pharmacology and Systems Therapeutics, Icahn School of Medicine at Mount Sinai, New York, NY, USA

    Jian Jin Ph.D.

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  1. Department of Pathology and Laboratory Medicine, Curriculum in Toxicology, UNC Program in Translational Medicine, UNC Lineberger Comprehensive Center, University of North Carolina School of Medicine, Chapel Hill, North Carolina, USA

    William B. Coleman

  2. Laboratory for Clinical Genomics and Advanced Technology (CGAT), Department of Pathology and Laboratory Medicine, Dartmouth-Hitchcock Medical Center, Norris Cotton Cancer Center, Geisel School of Medicine at Dartmouth, Lebanon, Hanover, New Hampshire, USA

    Gregory J. Tsongalis

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Chen, X., Jin, J. (2017). Small Molecule Inhibitors. In: Coleman, W., Tsongalis, G. (eds) The Molecular Basis of Human Cancer. Humana Press, New York, NY. https://doi.org/10.1007/978-1-59745-458-2_40

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