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 …

New insight into circRNAs: characterization, strategies, and biomedical applications

XY Feng, SX Zhu, KJ Pu, HJ Huang, YQ Chen… - … Hematology & Oncology, 2023 - Springer
Circular RNAs (circRNAs) are a class of covalently closed, endogenous ncRNAs. Most
circRNAs are derived from exonic or intronic sequences by precursor RNA back-splicing …

Anti-tumor efficacy of HRS-4642 and its potential combination with proteasome inhibition in KRAS G12D-mutant cancer

C Zhou, C Li, L Luo, X Li, K Jia, N He, S Mao, W Wang… - Cancer Cell, 2024 - cell.com
Summary KRAS G12D is the most frequently mutated oncogenic KRAS subtype in solid
tumors and remains undruggable in clinical settings. Here, we developed a high affinity …

Annual review of KRAS inhibitors in 2022

H Wang, L Chi, F Yu, H Dai, C Gao, X Si, Z Wang… - European Journal of …, 2023 - Elsevier
Kirsten rat sarcoma viral (KRAS) oncogene is the most commonly mutated isoform of RAS,
accounting for 85% of RAS-driven human cancers. KRAS functioning as a signaling hub …

Recent advances in the development of inhibitors targeting KRAS-G12C and its related pathways

D Zhao, Y Liu, F Yi, X Zhao, K Lu - European Journal of Medicinal …, 2023 - Elsevier
The RAS gene, also known as the mouse sarcoma virus, includes three genes (KRAS,
HRAS, and NRAS) that are associated with human tumors. Among them, KRAS has the …

Targeting KRAS in colorectal cancer: a bench to bedside review

F Bteich, M Mohammadi, T Li, MA Bhat… - International Journal of …, 2023 - mdpi.com
Colorectal cancer (CRC) is a heterogeneous disease with a myriad of alterations at the
cellular and molecular levels. Kristen rat sarcoma (KRAS) mutations occur in up to 40% of …

Cancer immune evasion through KRAS and PD-L1 and potential therapeutic interventions

A Watterson, MA Coelho - Cell Communication and Signaling, 2023 - Springer
Oncogenic driver mutations have implications that extend beyond cancer cells themselves.
Aberrant tumour cell signalling has various effects on the tumour microenvironment and anti …

A Potent SOS1 PROTAC Degrader with Synergistic Efficacy in Combination with KRASG12C Inhibitor

Y Lv, Z Yang, Y Chen, X Ma, M Guo… - Journal of Medicinal …, 2024 - ACS Publications
AMG510, as the first approved inhibitor for KRASG12C mutation, has shown promising
efficacy in nonsmall-cell lung cancer and colorectal cancer harboring KRASG12C mutation …

Multiple strategies to develop small molecular KRAS directly bound inhibitors

X Zhou, Y Ji, J Zhou - Molecules, 2023 - mdpi.com
KRAS gene mutation is widespread in tumors and plays an important role in various
malignancies. Targeting KRAS mutations is regarded as the “holy grail” of targeted cancer …

New prospectives on treatment opportunities in RASopathies

BD Gelb, ME Yohe, C Wolf… - American Journal of …, 2022 - Wiley Online Library
The RASopathies are a group of clinically defined developmental syndromes caused by
germline variants of the RAS/mitogen‐activated protein (MAPK) cascade. The prototypic …