MEK1 and MEK2 inhibitors and cancer therapy: the long and winding road

CJ Caunt, MJ Sale, PD Smith, SJ Cook - Nature Reviews Cancer, 2015 - nature.com
The role of the ERK signalling pathway in cancer is thought to be most prominent in tumours
in which mutations in the receptor tyrosine kinases RAS, BRAF, CRAF, MEK1 or MEK2 drive …

[HTML][HTML] Artificial intelligence in pharmaceutical sciences

M Lu, J Yin, Q Zhu, G Lin, M Mou, F Liu, Z Pan, N You… - Engineering, 2023 - Elsevier
Drug discovery and development affects various aspects of human health and dramatically
impacts the pharmaceutical market. However, investments in a new drug often go …

[HTML][HTML] Targeting KRAS mutant cancers with a covalent G12C-specific inhibitor

MR Janes, J Zhang, LS Li, R Hansen, U Peters, X Guo… - Cell, 2018 - cell.com
Summary KRAS G12C was recently identified to be potentially druggable by allele-specific
covalent targeting of Cys-12 in vicinity to an inducible allosteric switch II pocket (S-IIP) …

lncRNA MIR100HG-derived miR-100 and miR-125b mediate cetuximab resistance via Wnt/β-catenin signaling

Y Lu, X Zhao, Q Liu, C Li, R Graves-Deal, Z Cao… - Nature medicine, 2017 - nature.com
De novo and acquired resistance, which are largely attributed to genetic alterations, are
barriers to effective anti-epidermal-growth-factor-receptor (EGFR) therapy. To generate …

The Cancer Cell Line Encyclopedia enables predictive modelling of anticancer drug sensitivity

J Barretina, G Caponigro, N Stransky, K Venkatesan… - Nature, 2012 - nature.com
The systematic translation of cancer genomic data into knowledge of tumour biology and
therapeutic possibilities remains challenging. Such efforts should be greatly aided by robust …

Systematic identification of genomic markers of drug sensitivity in cancer cells

MJ Garnett, EJ Edelman, SJ Heidorn, CD Greenman… - Nature, 2012 - nature.com
Clinical responses to anticancer therapies are often restricted to a subset of patients. In
some cases, mutated cancer genes are potent biomarkers for responses to targeted agents …

Tumor genomic profiling guides patients with metastatic gastric cancer to targeted treatment: the VIKTORY umbrella trial

J Lee, ST Kim, K Kim, H Lee, I Kozarewa… - Cancer discovery, 2019 - AACR
The VIKTORY (targeted agent eValuation In gastric cancer basket KORea) trial was
designed to classify patients with metastatic gastric cancer based on clinical sequencing …

MAPK inhibitor sensitivity scores predict sensitivity driven by the immune infiltration in pediatric low-grade gliomas

R Sigaud, TK Albert, C Hess, T Hielscher… - Nature …, 2023 - nature.com
Pediatric low-grade gliomas (pLGG) show heterogeneous responses to MAPK inhibitors
(MAPKi) in clinical trials. Thus, more complex stratification biomarkers are needed to identify …

The clinical development of MEK inhibitors

Y Zhao, AA Adjei - Nature reviews Clinical oncology, 2014 - nature.com
Aberrant activation of the RAS–RAF–MEK–ERK1/2 pathway occurs in more than 30% of
human cancers. As part of this pathway, MEK1 and MEK2 have crucial roles in …

Dual‐specificity MAP kinase phosphatases (MKPs) Shaping the outcome of MAP kinase signalling

CJ Caunt, SM Keyse - The FEBS journal, 2013 - Wiley Online Library
Dual‐specificity MAP kinase phosphatases (MKPs) provide a complex negative regulatory
network that acts to shape the duration, magnitude and spatiotemporal profile of MAP kinase …