Advances in Cancer Research, volume 153 provides a timely review of the biology, biochemistry, and current approaches to therapeutically target the RAS oncoprotein, the most frequently mutated oncogene family in human cancers. 2021 saw the approval of the first direct RAS inhibitor (sotorasib) for use in treating non-small cell lung cancers harboring KRAS(G12C) mutations. The successful approval and use of this drug highlights that the once undruggable? RAS is indeed pharmacologically tractable. This volume provides an overview of efforts to develop additional approaches to therapeutically target oncogenic RAS. In addition, the reader will find excellent reviews on the history and research efforts to understand the biochemistry and oncogenic activity of RAS in human cancers. Overview of the history and development of efforts to pharmacologically inhibit RAS. Discussion of the biochemistry and biology of different RAS mutant proteins and how this might be effectively leveraged in the development of anti-RAS therapies. Up-to-date reviews of the cutting-edge approaches to develop new anti-RAS pharmacologics. INDICE: 1. A brief history of RAS and the RAS InitiativeFrank McCormick2. Not all RAS mutations are equal: A detailed review of the functional diversity of RAS hot spot mutationsRachel A. Burge and G. Aaron Hobbs3. Drug targeting opportunities en route to Ras nanoclustersKarolina Pavic, Rohan Chippalkatti, and Daniel Abankwa4. Targeting the ERK mitogen-activated protein kinase cascade for the treatment of KRAS-mutant pancreatic cancerJ. Nathaniel Diehl, Priya S. Hibshman, Irem Ozkan-Dagliyan, Craig M. Goodwin, Sarah V. Howard, Adrienne D. Cox, and Channing J. Der5. Pan-RAS inhibitors: Hitting multiple RAS isozymes with one stoneAlexander B. Coley, Antonio Ward, Adam B. Keeton, Xi Chen, Yulia Maxuitenko, Aishwarya Prakash, Feng Li, Jeremy B. Foote, Donald J. Buchsbaum, and Gary A. Piazza6. Targeting RAS oncogenesis with SOS1 inhibitorsRoman Christian Hillig and Benjamin Bader7. Inhibition of SHP2 as an approach to block RAS-driven cancersYu-Ting Chou and Trever G. Bivona8. Targeting the undruggable? RAS with biologicsMichael Whaby, Imran Khan, and John P. O'Bryan9. Unraveling and targeting RAS-driven metabolic signaling for therapeutic gainJonathan M. DeLiberty, Ryan Robb, Claire E. Gates, and Kirsten L. Bryant10. The RASopathies: Biology, genetics and therapeutic optionsJody Fromm Longo and Steven L. Carroll
- ISBN: 978-0-12-824485-2
- Editorial: Academic Press
- Encuadernacion: Cartoné
- Páginas: 356
- Fecha Publicación: 04/02/2022
- Nº Volúmenes: 1
- Idioma: Inglés