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 …

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

G Zhu, L Pei, H Xia, Q Tang, F Bi - Molecular cancer, 2021 - Springer
Colorectal cancer (CRC) is a heterogeneous disease at the cellular and molecular levels.
Kirsten rat sarcoma (KRAS) is a commonly mutated oncogene in CRC, with mutations in …

Expanding the Reach of Precision Oncology by Drugging All KRAS Mutants

MH Hofmann, D Gerlach, S Misale, M Petronczki… - Cancer Discovery, 2022 - AACR
KRAS is the most frequently mutated oncogene, harboring mutations in approximately one
in seven cancers. Allele-specific KRASG12C inhibitors are currently changing the treatment …

Targeting KRAS mutant cancers: from druggable therapy to drug resistance

C Zhu, X Guan, X Zhang, X Luan, Z Song, X Cheng… - Molecular cancer, 2022 - Springer
Abstract Kirsten Rat Sarcoma Viral Oncogene Homolog (KRAS) is the most frequently
mutated oncogene, occurring in a variety of tumor types. Targeting KRAS mutations with …

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

X Xie, 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 …

Targeting the RAS/RAF/MAPK pathway for cancer therapy: from mechanism to clinical studies

ME Bahar, HJ Kim, DR Kim - Signal transduction and targeted therapy, 2023 - nature.com
Metastatic dissemination of solid tumors, a leading cause of cancer-related mortality,
underscores the urgent need for enhanced insights into the molecular and cellular …

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 …

The KRAS-G12C inhibitor: activity and resistance

J Liu, R Kang, D Tang - Cancer gene therapy, 2022 - nature.com
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 …

[HTML][HTML] Oncogenic driver mutations in non-small cell lung cancer: Past, present and future

M Chevallier, M Borgeaud, A Addeo… - World Journal of …, 2021 - ncbi.nlm.nih.gov
Lung cancer, of which non-small lung cancer is the most common subtype, represents the
leading cause of cancer related-death worldwide. It is now recognized that a significant …

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 …