Ontology highlight
ABSTRACT:
SUBMITTER: Hocker HJ
PROVIDER: S-EPMC3690838 | biostudies-literature | 2013 Jun
REPOSITORIES: biostudies-literature
Hocker Harrison J HJ Cho Kwang-Jin KJ Chen Chung-Ying K CY Rambahal Nandini N Sagineedu Sreenivasa Rao SR Shaari Khozirah K Stanslas Johnson J Hancock John F JF Gorfe Alemayehu A AA
Proceedings of the National Academy of Sciences of the United States of America 20130604 25
Aberrant signaling by oncogenic mutant rat sarcoma (Ras) proteins occurs in ∼15% of all human tumors, yet direct inhibition of Ras by small molecules has remained elusive. Recently, several small-molecule ligands have been discovered that directly bind Ras and inhibit its function by interfering with exchange factor binding. However, it is unclear whether, or how, these ligands could lead to drugs that act against constitutively active oncogenic mutant Ras. Using a dynamics-based pocket identifi ...[more]