RAS-targeted therapies: is the undruggable drugged?
AR Moore, SC Rosenberg, F McCormick… - Nature reviews Drug …, 2020 - nature.com
Abstract RAS (KRAS, NRAS and HRAS) is the most frequently mutated gene family in
cancers, and, consequently, investigators have sought an effective RAS inhibitor for more …
cancers, and, consequently, investigators have sought an effective RAS inhibitor for more …
Molecular dynamics simulations in drug discovery and pharmaceutical development
Molecular dynamics (MD) simulations have become increasingly useful in the modern drug
development process. In this review, we give a broad overview of the current application …
development process. In this review, we give a broad overview of the current application …
The KRASG12C Inhibitor MRTX849 Provides Insight toward Therapeutic Susceptibility of KRAS-Mutant Cancers in Mouse Models and Patients
J Hallin, LD Engstrom, L Hargis, A Calinisan, R Aranda… - Cancer discovery, 2020 - AACR
Despite decades of research, efforts to directly target KRAS have been challenging.
MRTX849 was identified as a potent, selective, and covalent KRASG12C inhibitor that …
MRTX849 was identified as a potent, selective, and covalent KRASG12C inhibitor that …
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 …
[HTML][HTML] Targeting the untargetable KRAS in cancer therapy
P Liu, Y Wang, X Li - Acta Pharmaceutica Sinica B, 2019 - Elsevier
RAS is one of the most well-known proto-oncogenes. Its gain-of-function mutations occur in
approximately 30% of all human cancers. As the most frequently mutated RAS isoform …
approximately 30% of all human cancers. As the most frequently mutated RAS isoform …
Suppression of the SLC7A11/glutathione axis causes synthetic lethality in KRAS-mutant lung adenocarcinoma
K Hu, K Li, J Lv, J Feng, J Chen, H Wu… - The Journal of …, 2020 - Am Soc Clin Investig
Oncogenic KRAS is a major driver in lung adenocarcinoma (LUAD) that has yet to be
therapeutically conquered. Here we report that the SLC7A11/glutathione axis displays …
therapeutically conquered. Here we report that the SLC7A11/glutathione axis displays …
Therapeutic strategies to target RAS-mutant cancers
MB Ryan, RB Corcoran - Nature reviews Clinical oncology, 2018 - nature.com
RAS genes are the most commonly mutated oncogenes in cancer, but effective therapeutic
strategies to target RAS-mutant cancers have proved elusive. A key aspect of this challenge …
strategies to target RAS-mutant cancers have proved elusive. A key aspect of this challenge …
A model for RAS mutation patterns in cancers: finding the sweet spot
S Li, A Balmain, CM Counter - Nature Reviews Cancer, 2018 - nature.com
The three RAS genes—HRAS, NRAS and KRAS—are collectively mutated in one-third of
human cancers, where they act as prototypic oncogenes. Interestingly, there are rather …
human cancers, where they act as prototypic oncogenes. Interestingly, there are rather …
KRAS interaction with RAF1 RAS-binding domain and cysteine-rich domain provides insights into RAS-mediated RAF activation
The first step of RAF activation involves binding to active RAS, resulting in the recruitment of
RAF to the plasma membrane. To understand the molecular details of RAS-RAF interaction …
RAF to the plasma membrane. To understand the molecular details of RAS-RAF interaction …
Oligomeric organization of membrane proteins from native membranes at nanoscale spatial and single-molecule resolution
The oligomeric organization of membrane proteins in native cell membranes is a critical
regulator of their function. High-resolution quantitative measurements of oligomeric …
regulator of their function. High-resolution quantitative measurements of oligomeric …