KRAS mutation: from undruggable to druggable in cancer
L Huang, Z Guo, F Wang, L Fu - Signal transduction and targeted …, 2021 - nature.com
Cancer is the leading cause of death worldwide, and its treatment and outcomes have been
dramatically revolutionised by targeted therapies. As the most frequently mutated oncogene …
dramatically revolutionised by targeted therapies. As the most frequently mutated oncogene …
The current state of the art and future trends in RAS-targeted cancer therapies
Despite being the most frequently altered oncogenic protein in solid tumours, KRAS has
historically been considered 'undruggable'owing to a lack of pharmacologically targetable …
historically been considered 'undruggable'owing to a lack of pharmacologically targetable …
Efficacy of a Small-Molecule Inhibitor of KrasG12D in Immunocompetent Models of Pancreatic Cancer
SB Kemp, N Cheng, N Markosyan, R Sor, IK Kim… - Cancer discovery, 2023 - AACR
Mutations in the KRAS oncogene are found in more than 90% of patients with pancreatic
ductal adenocarcinoma (PDAC), with Gly-to-Asp mutations (KRAS G12D) being the most …
ductal adenocarcinoma (PDAC), with Gly-to-Asp mutations (KRAS G12D) being the most …
Expanding the Reach of Precision Oncology by Drugging All KRAS Mutants
KRAS is the most frequently mutated oncogene, harboring mutations in approximately one
in seven cancers. Allele-specific KRASG12C inhibitors are currently changing the treatment …
in seven cancers. Allele-specific KRASG12C inhibitors are currently changing the treatment …
Sugemalimab versus placebo after concurrent or sequential chemoradiotherapy in patients with locally advanced, unresectable, stage III non-small-cell lung cancer in …
Q Zhou, M Chen, O Jiang, Y Pan, D Hu, Q Lin… - The Lancet …, 2022 - thelancet.com
Background A substantial proportion of patients with unresectable stage III non-small-cell
lung cancer (NSCLC) cannot either tolerate or access concurrent chemoradiotherapy, so …
lung cancer (NSCLC) cannot either tolerate or access concurrent chemoradiotherapy, so …
Drugging KRAS: current perspectives and state-of-art review
After decades of efforts, we have recently made progress into targeting KRAS mutations in
several malignancies. Known as the 'holy grail'of targeted cancer therapies, KRAS is the …
several malignancies. Known as the 'holy grail'of targeted cancer therapies, KRAS is the …
The KRAS-G12C inhibitor: activity and resistance
Although it has long been deemed “undruggable”, with the development of drugs specifically
binding the KRAS-G12C mutant protein, clinical trials that directly inhibit oncogenic RAS …
binding the KRAS-G12C mutant protein, clinical trials that directly inhibit oncogenic RAS …
The expanding role for small molecules in immuno-oncology
R Offringa, L Kötzner, B Huck, K Urbahns - Nature Reviews Drug …, 2022 - nature.com
The advent of immune checkpoint inhibition (ICI) using antibodies against PD1 and its
ligand PDL1 has prompted substantial efforts to develop complementary drugs. Although …
ligand PDL1 has prompted substantial efforts to develop complementary drugs. Although …
Adagrasib: first approval
S Dhillon - Drugs, 2023 - Springer
Adagrasib (KRAZATI™) is an orally available, potent, irreversible, small molecule inhibitor of
KRAS G12C mutant isoform being developed by Mirati Therapeutics for the treatment of …
KRAS G12C mutant isoform being developed by Mirati Therapeutics for the treatment of …
Co-targeting SOS1 enhances the antitumor effects of KRASG12C inhibitors by addressing intrinsic and acquired resistance
Combination approaches are needed to strengthen and extend the clinical response to
KRASG12C inhibitors (KRASG12Ci). Here, we assessed the antitumor responses of …
KRASG12C inhibitors (KRASG12Ci). Here, we assessed the antitumor responses of …