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 …
cancers, and, consequently, investigators have sought an effective RAS inhibitor for more …
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 …
strategies to target RAS-mutant cancers have proved elusive. A key aspect of this challenge …
[HTML][HTML] Targeting ERK, an Achilles' Heel of the MAPK pathway, in cancer therapy
The mitogen-activated protein kinases (MAPK) pathway, often known as the RAS-RAF-MEK-
ERK signal cascade, functions to transmit upstream signals to its downstream effectors to …
ERK signal cascade, functions to transmit upstream signals to its downstream effectors to …
First-in-class ERK1/2 inhibitor ulixertinib (BVD-523) in patients with MAPK mutant advanced solid tumors: results of a phase I dose-escalation and expansion study
RJ Sullivan, JR Infante, F Janku, DJL Wong… - Cancer discovery, 2018 - AACR
Abstract Ulixertinib (BVD-523) is an ERK1/2 kinase inhibitor with potent preclinical activity in
BRAF-and RAS-mutant cell lines. In this multicenter phase I trial (NCT01781429), 135 …
BRAF-and RAS-mutant cell lines. In this multicenter phase I trial (NCT01781429), 135 …
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 …
percentage of tumours, most frequently owing to activating mutations of the KRAS, NRAS …
MEK1 and MEK2 inhibitors and cancer therapy: the long and winding road
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 …
in which mutations in the receptor tyrosine kinases RAS, BRAF, CRAF, MEK1 or MEK2 drive …
[HTML][HTML] Targeting cancer with kinase inhibitors
S Gross, R Rahal, N Stransky… - The Journal of …, 2015 - Am Soc Clin Investig
Kinase inhibitors have played an increasingly prominent role in the treatment of cancer and
other diseases. Currently, more than 25 oncology drugs that target kinases have been …
other diseases. Currently, more than 25 oncology drugs that target kinases have been …
Discovery of a novel ERK inhibitor with activity in models of acquired resistance to BRAF and MEK inhibitors
EJ Morris, S Jha, CR Restaino, P Dayananth, H Zhu… - Cancer discovery, 2013 - AACR
The high frequency of activating RAS or BRAF mutations in cancer provides strong rationale
for targeting the mitogen-activated protein kinase (MAPK) pathway. Selective BRAF and …
for targeting the mitogen-activated protein kinase (MAPK) pathway. Selective BRAF and …
Targeting the MAPK signaling pathway in cancer: promising preclinical activity with the novel selective ERK1/2 inhibitor BVD-523 (ulixertinib)
UA Germann, BF Furey, W Markland, RR Hoover… - Molecular cancer …, 2017 - AACR
Aberrant activation of signaling through the RAS–RAF–MEK–ERK (MAPK) pathway is
implicated in numerous cancers, making it an attractive therapeutic target. Although BRAF …
implicated in numerous cancers, making it an attractive therapeutic target. Although BRAF …
Targeted therapies for triple-negative breast cancer: combating a stubborn disease
Triple-negative breast cancers (TNBCs) constitute a heterogeneous subtype of breast
cancers that have a poor clinical outcome. Although no approved targeted therapy is …
cancers that have a poor clinical outcome. Although no approved targeted therapy is …