title: Targeting the unfolded protein response in cancer.
abstract: Cancer cells are exposed to various intrinsic and extrinsic factors that disrupt protein homeostasis, producing endoplasmic reticulum (ER) stress. To cope with these situations, cancer cells evoke a highly conserved adaptive mechanism called the unfolded protein response (UPR) to restore the ER homeostasis. Recently, several pharmacological agents have been found to exhibit anti-tumor activity by targeting the UPR components. The development of potent and specific compounds that target the UPR components has not only shed light on the regulation of the UPR in cancer cells, but also brought the field closer to clinical drug candidates. Here we present an overview of the milestones in the field of UPR biology in cancer with a focus on new strategies for pharmacological inhibition.
authors.affiliation: Department of Medicine and Abramson Cancer Center, University of Pennsylvania, United States.
authors.forename: Rani
authors.initials: R
authors.lastname: Ojha
authors.affiliation: Department of Medicine and Abramson Cancer Center, University of Pennsylvania, United States. Electronic address: Ravi.amaravadi@uphs.upenn.edu.
authors.forename: Ravi K
authors.initials: RK
authors.lastname: Amaravadi
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D055808:Drug Discovery / Q000379:methods; D059865:Endoplasmic Reticulum Stress / Q000187:drug effects; D006801:Humans; D058990:Molecular Targeted Therapy / Q000379:methods; D009369:Neoplasms / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D056811:Unfolded Protein Response / Q000187:drug effects*
chemical_list: D000970:Antineoplastic Agents
keywords: Anticancer therapy; Cancer; Endoplasmic reticulum stress; Unfolded protein response