The current state of the art and future trends in RAS-targeted cancer therapies

SR Punekar, V Velcheti, BG Neel… - Nature reviews Clinical …, 2022 - nature.com
Despite being the most frequently altered oncogenic protein in solid tumours, KRAS has
historically been considered 'undruggable'owing to a lack of pharmacologically targetable …

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 …

Molecular targeted therapy for anticancer treatment

HY Min, HY Lee - Experimental & molecular medicine, 2022 - nature.com
Since the initial clinical approval in the late 1990s and remarkable anticancer effects for
certain types of cancer, molecular targeted therapy utilizing small molecule agents or …

Recent advances in targeting the “undruggable” proteins: from drug discovery to clinical trials

X **e, T Yu, X Li, N Zhang, LJ Foster, C Peng… - Signal transduction and …, 2023 - nature.com
Undruggable proteins are a class of proteins that are often characterized by large, complex
structures or functions that are difficult to interfere with using conventional drug design …

Role of oncogenic KRAS in the diagnosis, prognosis and treatment of pancreatic cancer

L Buscail, B Bournet, P Cordelier - Nature reviews Gastroenterology & …, 2020 - nature.com
Pancreatic ductal adenocarcinoma (PDAC) is predicted to be the second most common
cause of death within the next 10 years. The prognosis for this disease is poor despite …

Chemical acylation of an acquired serine suppresses oncogenic signaling of K-Ras (G12S)

Z Zhang, KZ Guiley, KM Shokat - Nature chemical biology, 2022 - nature.com
Drugs that directly impede the function of driver oncogenes offer exceptional efficacy and a
therapeutic window. The recently approved mutant selective small-molecule cysteine …

Drugging KRAS: current perspectives and state-of-art review

K Parikh, G Banna, SV Liu, A Friedlaender… - Journal of hematology & …, 2022 - Springer
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 …

[HTML][HTML] Targeting KRAS mutant cancers with a covalent G12C-specific inhibitor

MR Janes, J Zhang, LS Li, R Hansen, U Peters, X Guo… - Cell, 2018 - cell.com
Summary KRAS G12C was recently identified to be potentially druggable by allele-specific
covalent targeting of Cys-12 in vicinity to an inducible allosteric switch II pocket (S-IIP) …

Emerging strategies to target RAS signaling in human cancer therapy

K Chen, Y Zhang, L Qian, P Wang - Journal of hematology & oncology, 2021 - Springer
Abstract RAS mutations (HRAS, NRAS, and KRAS) are among the most common
oncogenes, and around 19% of patients with cancer harbor RAS mutations. Cells harboring …

KRAS: the critical driver and therapeutic target for pancreatic cancer

AM Waters, CJ Der - Cold Spring Harbor …, 2018 - perspectivesinmedicine.cshlp.org
RAS genes (HRAS, KRAS, and NRAS) comprise the most frequently mutated oncogene
family in human cancer. With the highest RAS mutation frequencies seen with the top three …