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 …

Drugging KRAS: current perspectives and state-of-art review

K Parikh, G Banna, SV Liu, A Friedlaender… - Journal of hematology & …, 2022 - Springer
After decades of efforts, we have recently made progress into targeting KRAS mutations in
several malignancies. Known as the 'holy grail'of targeted cancer therapies, KRAS is the …

RAS proteins and their regulators in human disease

DK Simanshu, DV Nissley, F McCormick - Cell, 2017 - cell.com
RAS proteins are binary switches, cycling between ON and OFF states during signal
transduction. These switches are normally tightly controlled, but in RAS-related diseases …

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 …

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 …

Direct small-molecule inhibitors of KRAS: from structural insights to mechanism-based design

JML Ostrem, KM Shokat - Nature reviews Drug discovery, 2016 - nature.com
KRAS is the most frequently mutated oncogene in human cancer. In addition to holding this
distinction, unsuccessful attempts to target this protein have led to the characterization of …

The MEK/ERK network as a therapeutic target in human cancer

R Barbosa, LA Acevedo, R Marmorstein - Molecular Cancer Research, 2021 - AACR
Abstract The RAS–RAF–MEK–ERK pathway is the most well-studied of the MAPK cascades
and is critical for cell proliferation, differentiation, and survival. Abnormalities in regulation …

Single-molecule fluorescence microscopy review: shedding new light on old problems

S Shashkova, MC Leake - Bioscience reports, 2017 - portlandpress.com
Fluorescence microscopy is an invaluable tool in the biosciences, a genuine workhorse
technique offering exceptional contrast in conjunction with high specificity of labelling with …

Single-cell analysis targeting the proteome

M Labib, SO Kelley - Nature Reviews Chemistry, 2020 - nature.com
The existence of cellular heterogeneity and its central relevance to biological phenomena
provides a strong rationale for a need for analytical methods that enable analysis at the …

Oligomeric organization of membrane proteins from native membranes at nanoscale spatial and single-molecule resolution

G Walker, C Brown, X Ge, S Kumar… - Nature …, 2024 - nature.com
The oligomeric organization of membrane proteins in native cell membranes is a critical
regulator of their function. High-resolution quantitative measurements of oligomeric …