PROTACs: great opportunities for academia and industry (an update from 2020 to 2021)

M He, C Cao, Z Ni, Y Liu, P Song, S Hao, Y He… - … and Targeted Therapy, 2022 - nature.com
Abstract PROteolysis TArgeting Chimeras (PROTACs) technology is a new protein-
degradation strategy that has emerged in recent years. It uses bifunctional small molecules …

The journey from melanocytes to melanoma

PP Centeno, V Pavet, R Marais - Nature Reviews Cancer, 2023 - nature.com
Over the past decade, melanoma has led the field in new cancer treatments, with impressive
gains in on-treatment survival but more modest improvements in overall survival. Melanoma …

The MAPK and AMPK signalings: interplay and implication in targeted cancer therapy

J Yuan, X Dong, J Yap, J Hu - Journal of hematology & oncology, 2020 - Springer
Cancer is characterized as a complex disease caused by coordinated alterations of multiple
signaling pathways. The Ras/RAF/MEK/ERK (MAPK) signaling is one of the best-defined …

Targeting the RAS/RAF/MAPK pathway for cancer therapy: from mechanism to clinical studies

ME Bahar, HJ Kim, DR Kim - Signal transduction and targeted therapy, 2023 - nature.com
Metastatic dissemination of solid tumors, a leading cause of cancer-related mortality,
underscores the urgent need for enhanced insights into the molecular and cellular …

Targeting aberrant RAS/RAF/MEK/ERK signaling for cancer therapy

U Degirmenci, M Wang, J Hu - Cells, 2020 - mdpi.com
The RAS/RAF/MEK/ERK (MAPK) signaling cascade is essential for cell inter-and intra-
cellular communication, which regulates fundamental cell functions such as growth, survival …

Classifying BRAF alterations in cancer: new rational therapeutic strategies for actionable mutations

M Dankner, AAN Rose, S Rajkumar, PM Siegel… - Oncogene, 2018 - nature.com
Abstract The RAS–RAF–MEK–ERK signaling cascade is among the most frequently mutated
pathways in human cancer. Approximately 50% of melanoma patients possess a druggable …

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 …

Targeting RAS–ERK signalling in cancer: promises and challenges

AA Samatar, PI Poulikakos - Nature reviews Drug discovery, 2014 - nature.com
Abstract The RAS–RAF–MEK–ERK signalling pathway is hyperactivated in a high
percentage of tumours, most frequently owing to activating mutations of the KRAS, NRAS …

New perspectives for targeting RAF kinase in human cancer

Z Karoulia, E Gavathiotis, PI Poulikakos - Nature Reviews Cancer, 2017 - nature.com
The discovery that a subset of human tumours is dependent on mutationally deregulated
BRAF kinase intensified the development of RAF inhibitors to be used as potential …

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 …