The current state of the art and future trends in RAS-targeted cancer therapies
SR Punekar, V Velcheti, BG Neel… - Nature reviews Clinical …, 2022 - nature.com
Despite being the most frequently altered oncogenic protein in solid tumours, KRAS has
historically been considered 'undruggable'owing to a lack of pharmacologically targetable …
historically been considered 'undruggable'owing to a lack of pharmacologically targetable …
KRAS mutation: from undruggable to druggable in cancer
L Huang, Z Guo, F Wang, L Fu - Signal transduction and targeted …, 2021 - nature.com
Cancer is the leading cause of death worldwide, and its treatment and outcomes have been
dramatically revolutionised by targeted therapies. As the most frequently mutated oncogene …
dramatically revolutionised by targeted therapies. As the most frequently mutated oncogene …
Rational combinations of targeted cancer therapies: background, advances and challenges
H Jin, L Wang, R Bernards - Nature Reviews Drug Discovery, 2023 - nature.com
Over the past two decades, elucidation of the genetic defects that underlie cancer has
resulted in a plethora of novel targeted cancer drugs. Although these agents can initially be …
resulted in a plethora of novel targeted cancer drugs. Although these agents can initially be …
Clinical Acquired Resistance to KRASG12C Inhibition through a Novel KRAS Switch-II Pocket Mutation and Polyclonal Alterations Converging on RAS–MAPK …
Mutant-selective KRASG12C inhibitors, such as MRTX849 (adagrasib) and AMG 510
(sotorasib), have demonstrated efficacy in KRAS G12C-mutant cancers, including non–small …
(sotorasib), have demonstrated efficacy in KRAS G12C-mutant cancers, including non–small …
Acquired Resistance to KRASG12C Inhibition in Cancer
MM Awad, S Liu, II Rybkin, KC Arbour… - … England Journal of …, 2021 - Mass Medical Soc
Background Clinical trials of the KRAS inhibitors adagrasib and sotorasib have shown
promising activity in cancers harboring KRAS glycine-to-cysteine amino acid substitutions at …
promising activity in cancers harboring KRAS glycine-to-cysteine amino acid substitutions at …
Expanding the Reach of Precision Oncology by Drugging All KRAS Mutants
KRAS is the most frequently mutated oncogene, harboring mutations in approximately one
in seven cancers. Allele-specific KRASG12C inhibitors are currently changing the treatment …
in seven cancers. Allele-specific KRASG12C inhibitors are currently changing the treatment …
Targeting KRAS mutant cancers: from druggable therapy to drug resistance
C Zhu, X Guan, X Zhang, X Luan, Z Song, X Cheng… - Molecular cancer, 2022 - Springer
Abstract Kirsten Rat Sarcoma Viral Oncogene Homolog (KRAS) is the most frequently
mutated oncogene, occurring in a variety of tumor types. Targeting KRAS mutations with …
mutated oncogene, occurring in a variety of tumor types. Targeting KRAS mutations with …
The MAPK and AMPK signalings: interplay and implication in targeted cancer therapy
J Yuan, X Dong, J Yap, J Hu - Journal of hematology & oncology, 2020 - Springer
Cancer is characterized as a complex disease caused by coordinated alterations of multiple
signaling pathways. The Ras/RAF/MEK/ERK (MAPK) signaling is one of the best-defined …
signaling pathways. The Ras/RAF/MEK/ERK (MAPK) signaling is one of the best-defined …
Chemical remodeling of a cellular chaperone to target the active state of mutant KRAS
CJ Schulze, KJ Seamon, Y Zhao, YC Yang, J Cregg… - Science, 2023 - science.org
The discovery of small-molecule inhibitors requires suitable binding pockets on protein
surfaces. Proteins that lack this feature are considered undruggable and require innovative …
surfaces. Proteins that lack this feature are considered undruggable and require innovative …
The path to the clinic: a comprehensive review on direct KRASG12C inhibitors
The RAS oncogene is both the most frequently mutated oncogene in human cancer and the
first confirmed human oncogene to be discovered in 1982. After decades of research, in …
first confirmed human oncogene to be discovered in 1982. After decades of research, in …