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 …

Abstract RAS (KRAS, NRAS and HRAS) is the most frequently mutated gene family in
cancers, and, consequently, investigators have sought an effective RAS inhibitor for more …

KRASG12D, the most common oncogenic KRAS mutation, is a promising target for the
treatment of solid tumors. However, when compared to KRASG12C, selective inhibition of …

Molecular dynamics (MD) simulations have become increasingly useful in the modern drug
development process. In this review, we give a broad overview of the current application …

Drugs that directly impede the function of driver oncogenes offer exceptional efficacy and a
therapeutic window. The recently approved mutant selective small-molecule cysteine …

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 …

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) …

RAS proteins are binary switches, cycling between ON and OFF states during signal
transduction. These switches are normally tightly controlled, but in RAS-related diseases …

The 3 human RAS genes, KRAS, NRAS, and HRAS, encode 4 different RAS proteins which
belong to the protein family of small GTPases that function as binary molecular switches …

After 20 years of sometimes quiet growth, fragment-based drug discovery (FBDD) has
become mainstream. More than 30 drug candidates derived from fragments have entered …