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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 …
distinction, unsuccessful attempts to target this protein have led to the characterization of …
New perspectives for targeting RAF kinase in human cancer
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 …
BRAF kinase intensified the development of RAF inhibitors to be used as potential …
The role of CRAF in cancer progression: from molecular mechanisms to precision therapies
M Riaud, J Maxwell, I Soria-Bretones… - Nature Reviews …, 2024 - nature.com
The RAF family of kinases includes key activators of the pro-tumourigenic mitogen-activated
protein kinase pathway. Hyperactivation of RAF proteins, particularly BRAF and CRAF …
protein kinase pathway. Hyperactivation of RAF proteins, particularly BRAF and CRAF …
[HTML][HTML] Dragging ras back in the ring
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 …
Vemurafenib: the first drug approved for BRAF-mutant cancer
G Bollag, J Tsai, J Zhang, C Zhang, P Ibrahim… - Nature reviews Drug …, 2012 - nature.com
The identification of driver oncogenes has provided important targets for drugs that can
change the landscape of cancer therapies. One such example is the BRAF oncogene, which …
change the landscape of cancer therapies. One such example is the BRAF oncogene, which …
Tumor adaptation and resistance to RAF inhibitors
RAF kinase inhibitors have substantial therapeutic effects in patients with BRAF-mutant
melanoma. However, only rarely do tumors regress completely, and the therapeutic effects …
melanoma. However, only rarely do tumors regress completely, and the therapeutic effects …
RAS interaction with PI3K: more than just another effector pathway
RAS proteins are small GTPases known for their involvement in oncogenesis: around 25%
of human tumors present mutations in a member of this family. RAS operates in a complex …
of human tumors present mutations in a member of this family. RAS operates in a complex …
Mitogen-activated protein (MAP) kinase pathways: regulation and physiological functions
G Pearson, F Robinson, T Beers Gibson, B Xu… - Endocrine …, 2001 - academic.oup.com
Mitogen-activated protein (MAP) kinases comprise a family of ubiquitous proline-directed,
protein-serine/threonine kinases, which participate in signal transduction pathways that …
protein-serine/threonine kinases, which participate in signal transduction pathways that …
Ras history: The saga continues
AD Cox, CJ Der - Small GTPases, 2010 - Taylor & Francis
Although the roots of Ras sprouted from the rich history of retrovirus research, it was the
discovery of mutationally activated RAS genes in human cancer in 1982 that stimulated an …
discovery of mutationally activated RAS genes in human cancer in 1982 that stimulated an …
RAS oncogenes: the first 30 years
From the pioneering work with acute transforming retroviruses to the current post-genomic
era, RAS genes have always been at the leading edge of signal transduction and molecular …
era, RAS genes have always been at the leading edge of signal transduction and molecular …