title: Caspase activity modulators as anticancer agents.
abstract: Proteolytic caspase enzymes play a central role in cell apoptosis, or programmed cell death, often as integrating elements of different stimuli leading to the cell death. Since blockade of apoptotic pathways are fundamental for cell survival and proliferation, particularly in cancer cells, the activation of caspases is an attractive target for anticancer therapy. This review describes some of the druggable therapeutic targets thus far identified within the core apoptotic machinery, the corresponding drugs that have been developed, their effects on caspase-dependent apoptotic pathways and their potential impact on the therapy of cancer. With several successful anticancer drugs on the market and numerous compounds in preclinical and clinical developments, modulators of caspase-dependent apoptotic pathways belong to the most important category of anticancer agents.
authors.affiliation: ChemDiv, Inc. San Diego, CA 92121, USA. iokun@chemdiv.com
authors.forename: Ilya
authors.initials: I
authors.lastname: Okun
authors.forename: Konstantin V
authors.initials: KV
authors.lastname: Balakin
authors.forename: Sergey E
authors.initials: SE
authors.lastname: Tkachenko
authors.forename: Alexandre V
authors.initials: AV
authors.lastname: Ivachtchenko
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology* / Q000627:therapeutic use; D017209:Apoptosis / Q000187:drug effects / Q000502:physiology; D051017:Apoptosis Regulatory Proteins / Q000187:drug effects; D061945:Caspase Inhibitors; D020169:Caspases / Q000378:metabolism*; D004789:Enzyme Activation / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000494:pharmacology* / Q000627:therapeutic use; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy* / Q000201:enzymology*; D015398:Signal Transduction / Q000187:drug effects
chemical_list: D000970:Antineoplastic Agents; D051017:Apoptosis Regulatory Proteins; D061945:Caspase Inhibitors; D004791:Enzyme Inhibitors; D020169:Caspases