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 …

PI3K/Akt/mTOR and Ras/Raf/MEK/ERK signaling pathways inhibitors as anticancer agents: Structural and pharmacological perspectives

V Asati, DK Mahapatra, SK Bharti - European journal of medicinal chemistry, 2016 - Elsevier
The protein kinases regulate cellular functions such as transcription, translation,
proliferation, growth and survival by the process of phosphorylation. Over activation of …

Targeting MAPK signaling in cancer: mechanisms of drug resistance and sensitivity

S Lee, J Rauch, W Kolch - International journal of molecular sciences, 2020 - mdpi.com
Mitogen-activated protein kinase (MAPK) pathways represent ubiquitous signal transduction
pathways that regulate all aspects of life and are frequently altered in disease. Here, we …

Small molecule stabilization of the KSR inactive state antagonizes oncogenic Ras signalling

NS Dhawan, AP Scopton, AC Dar - Nature, 2016 - nature.com
Deregulation of the Ras–mitogen activated protein kinase (MAPK) pathway is an early event
in many different cancers and a key driver of resistance to targeted therapies. Sustained …

Targeting extracellular signal-regulated protein kinase 1/2 (ERK1/2) in cancer: an update on pharmacological small-molecule inhibitors

L Fu, S Chen, G He, Y Chen, B Liu - Journal of medicinal chemistry, 2022 - ACS Publications
Extracellular signal-regulated protein kinase 1/2 (ERK1/2), the only known substrate of
MEK1/2, is located downstream of the RAS-RAF-MEK-ERK (MAPK) pathway and is …

[HTML][HTML] Raf kinases: function, regulation and role in human cancer

DT Leicht, V Balan, A Kaplun, V Singh-Gupta… - … et Biophysica Acta (BBA …, 2007 - Elsevier
The Ras-Raf-MAPK pathway regulates diverse physiological processes by transmitting
signals from membrane based receptors to various nuclear, cytoplasmic and membrane …

Molecular Pathways: Targeting NRAS in Melanoma and Acute Myelogenous Leukemia

DB Johnson, KSM Smalley, JA Sosman - Clinical Cancer Research, 2014 - AACR
Successful targeting of specific oncogenic “driver” mutations with small-molecule inhibitors
has represented a major advance in cancer therapeutics over the past 10 to 15 years. The …

RAS-mediated oncogenic signaling pathways in human malignancies

AQ Khan, S Kuttikrishnan, KS Siveen, KS Prabhu… - Seminars in cancer …, 2019 - Elsevier
Abnormally activated RAS proteins are the main oncogenic driver that governs the
functioning of major signaling pathways involved in the initiation and development of human …

Targeting the ERK signaling pathway in cancer therapy

M Kohno, J Pouyssegur - Annals of medicine, 2006 - Taylor & Francis
The extracellular signal‐regulated kinase (ERK) signaling pathway is a major determinant in
the control of diverse cellular processes such as proliferation, survival, differentiation and …

The Raf/MEK/ERK signal transduction cascade as a target for chemotherapeutic intervention in leukemia

JT Lee Jr, JA McCubrey - Leukemia, 2002 - nature.com
Abstract The Raf/MEK/ERK (MAPK) signal transduction cascade is a vital mediator of a
number of cellular fates including growth, proliferation and survival, among others. The focus …