Missing content? – Request curation!
Request curation for specific Genes, Variants, or PubMed publications.
Have questions, comments, or suggestions? - Let us know!
Email us at : ckbsupport@genomenon.com
Gene | KEAP1 |
Variant | inact mut |
Impact List | unknown |
Protein Effect | loss of function |
Gene Variant Descriptions | KEAP1 inact mut indicates that this variant results in a loss of function of the Keap1 protein. However, the specific amino acid change has not been identified. |
Associated Drug Resistance | |
Category Variants Paths |
KEAP1 mutant KEAP1 inact mut |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
KEAP1 inact mut | gallbladder cancer | resistant | Fluorouracil | Preclinical | Actionable | In a preclinical study, gallbladder cancer cells harboring KEAP inactivating mutations had increased NRF2 activation and demonstrated resistance to Adrucil (fluorouracil) in culture (PMID: 18692501). | 18692501 |
KEAP1 inact mut | lung adenocarcinoma | sensitive | Carboplatin + MSU38225 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, MSU38225 and Paraplatin (carboplatin) combination treatment synergistically inhibited growth of a lung cancer cell line harboring a KEAP1 inactivating mutation in culture and slowed tumor growth in a cell line xenograft model compared to vehicle or Paraplatin (carboplatin) alone (PMID: 34158350). | 34158350 |
KEAP1 inact mut | lung adenocarcinoma | sensitive | MSU38225 | Preclinical - Cell culture | Actionable | In a preclinical study, MSU38225 inhibited Nrf2 transcriptional activity and downstream pathway activation, increased Nrf2 degradation, and inhibited growth of lung cancer cells harboring a KEAP1 inactivating mutation in 2D and 3D culture (PMID: 34158350). | 34158350 |
KEAP1 inact mut | lung adenocarcinoma | sensitive | Fluorouracil + MSU38225 | Preclinical - Cell culture | Actionable | In a preclinical study, MSU38225 and Adrucil (fluorouracil) combination treatment inhibited growth of a lung cancer cell line harboring a KEAP1 inactivating mutation in culture (PMID: 34158350). | 34158350 |