Annotation Detail
Information
- Associated Genes
- ABL1
- Associated Variants
-
ABL1 p.Arg351Trp (p.R351W)
(
ENST00000318560.6,
ENST00000372348.9 )
ABL1 p.Arg351Trp (p.R351W) ( ENST00000318560.6, ENST00000372348.9 ) - Associated Disease
- lung non-small cell carcinoma
- Source Database
- CIViC Evidence
- Description
- In this in vitro study, the H1915 non-small cell lung cancer cell line (homozygous for a R351W mutation) was shown to be susceptible to imatinib. This line showed a significant reduction in colony formation (P = 0.0004) and MTT assay, which tests for NADH activity (P < 0.001), with imatinib vs vehicle treatment. There was no significant difference in a lung cancer cell line without a known driver (H2126) nor in an immortalized bronchial epithelial line (Beas-2B) with either drug treatment in colony forming and MTT assays. Additionally, reduction in cell viability upon kinase inhibitor treatment was rescued with tetracycline-induced overexpression of resistant ABL1-T315I (P < 0.001) confirming the genetic dependency of this cell line on ABL1. Moreover, siRNA facilitated depletion of ABL1 expression resulted in significantly increased cytotoxicity (P < 0.004) with no significant change in H2126 or Beas-2B lines for 2/3 siRNAs supporting ABL1 as the primary drug target. Significant tumor reduction was observed in murine NSCLC xenografts of the H1915 cell line treated with imatinib compared to vehicle treatment (P = 0.0016). No change in tumor growth was observed in xenografts of the H650 cell line containing a wildtype ABL1 locus. In both in vitro and in vivo experiments, doxycycline-inducible expression of drug-resistant ABL1-T315I rescued imatinib-mediated inhibitory effects supporting the specificity of drug responses.
- Variant Origin
- somatic
- Variant Origin
- Somatic
- Evidence URL
- https://civic.genome.wustl.edu/links/evidence_items/6376
- Gene URL
- https://civic.genome.wustl.edu/links/genes/4
- Variant URL
- https://civic.genome.wustl.edu/links/variants/1656
- Rating
- 5
- Evidence Type
- Predictive
- Disease
- Lung Non-small Cell Carcinoma
- Evidence Direction
- Supports
- Drug
- Imatinib
- Evidence Level
- D
- Clinical Significance
- Sensitivity/Response
- Pubmed
- 26758680
Drugs
Drug Name | Sensitivity | Supported |
---|---|---|
Imatinib | Sensitivity | true |