BACKGROUND: The ubiquitin-proteasomal degradation pathway plays a critical role in protein degradation and regulates a wide variety of cellular functions. This highly conserved post-translational modification of proteolytic processes is mainly carried out by substrate-specific E3 ligases. The deregulation of E3 ligases contributes to cancer development and their overexpression is often associated with poor prognosis. OBJECTIVES: We review the current understanding of E3 ligases, their functional role in cancer pathogenesis, current progress and development of certain ubiquitin E3 ligases as targets for therapeutic intervention. METHODS: Preclinical and clinical data for E3 ligase inhibitors available in the public domain are discussed. CONCLUSIONS: With the growing understanding of their role in cancer development and progression, E3 ligases have emerged as potential anticancer targets for therapeutic intervention.
BACKGROUND: The ubiquitin-proteasomal degradation pathway plays a critical role in protein degradation and regulates a wide variety of cellular functions. This highly conserved post-translational modification of proteolytic processes is mainly carried out by substrate-specific E3 ligases. The deregulation of E3 ligases contributes to cancer development and their overexpression is often associated with poor prognosis. OBJECTIVES: We review the current understanding of E3 ligases, their functional role in cancer pathogenesis, current progress and development of certain ubiquitin E3 ligases as targets for therapeutic intervention. METHODS: Preclinical and clinical data for E3 ligase inhibitors available in the public domain are discussed. CONCLUSIONS: With the growing understanding of their role in cancer development and progression, E3 ligases have emerged as potential anticancer targets for therapeutic intervention.
Authors: John K Morrow; Lei Du-Cuny; Lu Chen; Emmanuelle J Meuillet; Eugene A Mash; Garth Powis; Shuxing Zhang Journal: Recent Pat Anticancer Drug Discov Date: 2011-01 Impact factor: 4.169
Authors: Tomas Kirchhoff; Zhang-qun Chen; Bert Gold; Prodipto Pal; Mia M Gaudet; Kristi Kosarin; Douglas A Levine; Peter Gregersen; Sara Spencer; Megan Harlan; Mark Robson; Robert J Klein; Clifford A Hudis; Larry Norton; Michael Dean; Kenneth Offit Journal: Cancer Epidemiol Biomarkers Prev Date: 2009-08-18 Impact factor: 4.254
Authors: Ali Flores-Pérez; Laurence A Marchat; Sergio Rodríguez-Cuevas; Verónica Piña Bautista; Lizeth Fuentes-Mera; Diana Romero-Zamora; Anabel Maciel-Dominguez; Olga Hernández de la Cruz; Miguel Fonseca-Sánchez; Erika Ruíz-García; Horacio Astudillo-de la Vega; César López-Camarillo Journal: BMC Cancer Date: 2016-07-04 Impact factor: 4.430