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Current Opinion in Chemical Biology, 2021
The protein KRAS has for decades been considered a holy grail of cancer drug discovery. For most of that time, it has also been considered undruggable. Since 2018, five compounds have entered the clinic targeting a single mutant form of KRAS, G12C. Here, we review each of these compounds along with additional approaches to targeting this and other ...
Daniel A, Erlanson, Kevin R, Webster
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The protein KRAS has for decades been considered a holy grail of cancer drug discovery. For most of that time, it has also been considered undruggable. Since 2018, five compounds have entered the clinic targeting a single mutant form of KRAS, G12C. Here, we review each of these compounds along with additional approaches to targeting this and other ...
Daniel A, Erlanson, Kevin R, Webster
openaire +2 more sources
Therapeutics Targeting Mutant KRAS
Annual Review of Medicine, 2021Aberrations in rat sarcoma (RAS) viral oncogene are the most prevalent and best-known genetic alterations identified in human cancers. Indeed, RAS drives tumorigenesis as one of the downstream effectors of EGFR activation, regulating cellular switches and functions and triggering intracellular signaling cascades such as the MAPK and PI3K pathways.
Kyaw Z, Thein +2 more
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European Journal of Cancer, 2009
The anti-epidermal growth factor receptor (EGFR) antibodies cetuximab and panitumumab have been demonstrated to be efficient in the treatment of irinotecan-resistant and chemorefractory metastatic colorectal cancer (mCRC) respectively. However, these costly and potentially toxic treatments are only efficient in a small proportion of patients.
Pierre, Laurent-Puig +2 more
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The anti-epidermal growth factor receptor (EGFR) antibodies cetuximab and panitumumab have been demonstrated to be efficient in the treatment of irinotecan-resistant and chemorefractory metastatic colorectal cancer (mCRC) respectively. However, these costly and potentially toxic treatments are only efficient in a small proportion of patients.
Pierre, Laurent-Puig +2 more
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KRAS mutations: Analytical considerations
Clinica Chimica Acta, 2014Colorectal cancer (CRC) is the third most common cancer and the second most common cause of cancer death globally. Significant improvements in survival have been made in patients with metastasis by new therapies. For example, Cetuximab and Panitumumab are monoclonal antibodies that inhibit the epidermal growth receptor (EGFR).
Marta Herreros-Villanueva +4 more
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Nature Medicine
RAS family variants-most of which involve KRAS-are the most commonly occurring hotspot mutations in human cancers and are associated with a poor prognosis. For almost four decades, KRAS has been considered undruggable, in part due to its structure, which lacks small-molecule binding sites.
Anupriya Singhal +2 more
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RAS family variants-most of which involve KRAS-are the most commonly occurring hotspot mutations in human cancers and are associated with a poor prognosis. For almost four decades, KRAS has been considered undruggable, in part due to its structure, which lacks small-molecule binding sites.
Anupriya Singhal +2 more
openaire +2 more sources