Drugging the undruggable RAS: Mission possible?

AD Cox, SW Fesik, AC Kimmelman, J Luo… - Nature reviews Drug …, 2014 - nature.com
Despite more than three decades of intensive effort, no effective pharmacological inhibitors
of the RAS oncoproteins have reached the clinic, prompting the widely held perception that …

Ras superfamily GEFs and GAPs: validated and tractable targets for cancer therapy?

D Vigil, J Cherfils, KL Rossman, CJ Der - Nature Reviews Cancer, 2010 - nature.com
There is now considerable and increasing evidence for a causal role for aberrant activity of
the Ras superfamily of small GTPases in human cancers. These GTPases function as GDP …

Rapid non-uniform adaptation to conformation-specific KRAS (G12C) inhibition

JY Xue, Y Zhao, J Aronowitz, TT Mai, A Vides, B Qeriqi… - Nature, 2020 - nature.com
KRAS GTPases are activated in one-third of cancers, and KRAS (G12C) is one of the most
common activating alterations in lung adenocarcinoma,. KRAS (G12C) inhibitors, are in …

Targeting protein prenylation for cancer therapy

N Berndt, AD Hamilton, SM Sebti - Nature Reviews Cancer, 2011 - nature.com
Protein farnesylation and geranylgeranylation, together referred to as prenylation, are lipid
post-translational modifications that are required for the transforming activity of many …

Ras history: The saga continues

AD Cox, CJ Der - Small GTPases, 2010 - Taylor & Francis
Although the roots of Ras sprouted from the rich history of retrovirus research, it was the
discovery of mutationally activated RAS genes in human cancer in 1982 that stimulated an …

Aurora A kinase (AURKA) in normal and pathological cell division

AS Nikonova, I Astsaturov, IG Serebriiskii… - Cellular and Molecular …, 2013 - Springer
Temporally and spatially controlled activation of the Aurora A kinase (AURKA) regulates
centrosome maturation, entry into mitosis, formation and function of the bipolar spindle, and …

Inhibition of Ras for cancer treatment: the search continues

AT Baines, D Xu, CJ Der - Future medicinal chemistry, 2011 - Taylor & Francis
The RAS oncogenes (HRAS, NRAS and KRAS) comprise the most frequently mutated class
of oncogenes in human cancers (33%), thus stimulating intensive effort in developing anti …

RALA and RALBP1 regulate mitochondrial fission at mitosis

DF Kashatus, KH Lim, DC Brady, NLK Pershing… - Nature cell …, 2011 - nature.com
Mitochondria exist as dynamic interconnected networks that are maintained through a
balance of fusion and fission. Equal distribution of mitochondria to daughter cells during …

An integrative approach unveils FOSL1 as an oncogene vulnerability in KRAS-driven lung and pancreatic cancer

A Vallejo, N Perurena, E Guruceaga, PK Mazur… - Nature …, 2017 - nature.com
KRAS mutated tumours represent a large fraction of human cancers, but the vast majority
remains refractory to current clinical therapies. Thus, a deeper understanding of the …

Calmodulin activation of Aurora-A kinase (AURKA) is required during ciliary disassembly and in mitosis

OV Plotnikova, AS Nikonova, YV Loskutov… - Molecular biology of …, 2012 - Am Soc Cell Biol
The centrosomal Aurora-A kinase (AURKA) regulates mitotic progression, and
overexpression and hyperactivation of AURKA commonly promotes genomic instability in …