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 …
of the RAS oncoproteins have reached the clinic, prompting the widely held perception that …
Ras family signaling: therapeutic targeting
AD Cox, CJ Der - Cancer biology & therapy, 2002 - Taylor & Francis
Mutationally activated and oncogenic versions of the ras genes were first identified in human
tumors in 1982. This discovery prompted great interest in the development of anti-Ras …
tumors in 1982. This discovery prompted great interest in the development of anti-Ras …
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 …
Direct inhibition of RAS: Quest for the Holy Grail?
R Spencer-Smith, JP O'Bryan - Seminars in cancer biology, 2019 - Elsevier
Abstract RAS GTPases (H-, K-, and N-RAS) are the most frequently mutated oncoprotein
family in human cancer. However, the relatively smooth surface architecture of RAS and its …
family in human cancer. However, the relatively smooth surface architecture of RAS and its …
The RAS–effector interaction as a drug target
About a third of all human cancers harbor mutations in one of the K-, N-, or HRAS genes that
encode an abnormal RAS protein locked in a constitutively activated state to drive malignant …
encode an abnormal RAS protein locked in a constitutively activated state to drive malignant …
[HTML][HTML] Therapeutic targeting of RAS: New hope for drugging the “undruggable”
I Khan, JM Rhett, JP O'Bryan - … et Biophysica Acta (BBA)-Molecular Cell …, 2020 - Elsevier
RAS is the most frequently mutated oncogene in cancer and a critical driver of oncogenesis.
Therapeutic targeting of RAS has been a goal of cancer research for more than 30 years …
Therapeutic targeting of RAS has been a goal of cancer research for more than 30 years …
Targeting the RAS oncogene
A Takashima, DV Faller - Expert opinion on therapeutic targets, 2013 - Taylor & Francis
Introduction: The Ras proteins (K-Ras, N-Ras, and H-Ras) are GTPases that function as
molecular switches for a variety of critical cellular activities and their function is tightly and …
molecular switches for a variety of critical cellular activities and their function is tightly and …
[HTML][HTML] Dragging ras back in the ring
AG Stephen, D Esposito, RK Bagni, F McCormick - Cancer cell, 2014 - cell.com
Ras proteins play a major role in human cancers but have not yielded to therapeutic attack.
Ras-driven cancers are among the most difficult to treat and often excluded from therapies …
Ras-driven cancers are among the most difficult to treat and often excluded from therapies …
Pharmacological targeting of RAS: recent success with direct inhibitors
JP O'Bryan - Pharmacological research, 2019 - Elsevier
RAS has long been viewed as undruggable due to its lack of deep pockets for binding of
small molecule inhibitors. However, recent successes in the development of direct RAS …
small molecule inhibitors. However, recent successes in the development of direct RAS …
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 …