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| PMID | (29875397) | ||||||||||||
| Authors | Sun Y, Zhao X, Ding N, Gao H, Wu Y, Yang Y, Zhao M, Hwang J, Song Y, Liu W, Rao Y | ||||||||||||
| Title | PROTAC-induced BTK degradation as a novel therapy for mutated BTK C481S induced ibrutinib-resistant B-cell malignancies. | ||||||||||||
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| Molecular Profile | Treatment Approach |
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| Gene Name | Source | Synonyms | Protein Domains | Gene Description | Gene Role |
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| Therapy Name | Drugs | Efficacy Evidence | Clinical Trials |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
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| Gene | Variant | Impact | Protein Effect | Variant Description | Associated with drug Resistance |
|---|---|---|---|---|---|
| BTK | C481A | missense | unknown | BTK C481A lies within the protein kinase domain of the Btk protein (UniProt.org). C481A interferes with drug binding, leading to ibrutinib resistance (PMID: 24869597, PMID: 29875397), but has not been biochemically characterized and therefore, its effect on Btk protein function is unknown (PubMed, Jun 2025). | Y |
| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| BTK C481S | diffuse large B-cell lymphoma | resistant | Ibrutinib | Preclinical - Cell culture | Actionable | In a preclinical study, a diffuse large B-cell lymphoma cell line expressing BTK C481S was resistant to Imbruvica (ibrutinib) treatment in culture (PMID: 29875397). | 29875397 |