title: Drugging RAS: Know the enemy.
abstract: The three RAS oncogenes make up the most frequently mutated gene family in human cancer. The well-validated role of mutationally activated RAS genes in driving cancer development and growth has stimulated comprehensive efforts to develop therapeutic strategies to block mutant RAS function for cancer treatment. Disappointingly, despite more than three decades of research effort, clinically effective anti-RAS therapies have remained elusive, prompting a perception that RAS may be undruggable. However, with a greater appreciation of the complexities of RAS that thwarted past efforts, and armed with new technologies and directions, the field is experiencing renewed excitement that mutant RAS may finally be conquered. Here we summarize where these efforts stand.
authors.affiliation: Lineberger Comprehensive Cancer Center, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.
authors.forename: Bjoern
authors.identifier: 0000-0001-8156-7508
authors.initials: B
authors.lastname: Papke
authors.affiliation: Lineberger Comprehensive Cancer Center, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA. cjder@med.unc.edu.
authors.forename: Channing J
authors.identifier: 0000-0002-7751-2747
authors.initials: CJ
authors.lastname: Der
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D002462:Cell Membrane / Q000201:enzymology; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D006801:Humans; D058990:Molecular Targeted Therapy; D009154:Mutation; D009369:Neoplasms / Q000188:drug therapy* / Q000235:genetics*; D018631:ras Proteins / Q000037:antagonists & inhibitors* / Q000235:genetics*
chemical_list: D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D018631:ras Proteins