Machine learning driven drug repurposing strategy for identification of potential RET inhibitors against non-small cell lung cancer - Medical Oncology
Source : https://link.springer.com/article/10.1007/s12032-022-01924-4
Non-small cell lung cancer (NSCLC) remains the leading cause of mortality and morbidity worldwide accounting about 85% of total lung cancer cases. The receptor REarranged during Transfection (RET) plays an...
Conclusions: The simulation study highlights the potency of DB00471 (Montelukast) as potential RET inhibitor among the investigated compounds. In the end, the half-minimal inhibitory activity of montelukast was also predicted against RET protein expressing LC-2/ad cell lines demonstrated significant anticancer activity. Collective analysis from...
Tumour-agnostic efficacy and safety of selpercatinib in patients with RET fusion-positive solid tumours other than lung or thyroid tumours (LIBRETTO-001): a phase 1/2, open-label, basket trial
Source : https://www.thelancet.com/journals/lanonc/article/PIIS1470-2045(22)00541-1/fulltext
Selpercatinib showed clinically meaningful activity in the RET fusion-positive tumour-agnostic population, with a safety profile consistent with that observed in other indications. Comprehensive genomic testing that includes RET fusions will...
Conclusions: Interpretation: Selpercatinib showed clinically meaningful activity in the RET fusion-positive tumour-agnostic population, with a safety profile consistent with that observed in other indications. Comprehensive genomic testing that includes RET fusions will be crucial for identifying patients who might benefit from selpercatinib.
RET Proto-Oncogene-Not Such an Obvious Starting Point in Cancer Therapy - PubMed
Source : https://pubmed.ncbi.nlm.nih.gov/36358717/
Mutations and fusions of RET (rearranged during transfection) gene are detected in a few common types of tumors including thyroid or non-small cells lung cancers. Multiple kinase inhibitors (MKIs) do...
Conclusions: This review presents the function of the normal RET receptor, types of molecular disturbances of the RET gene in patients with various cancers, methods of detecting these abnormalities, and the effectiveness of modern anticancer therapies (ranging from immunotherapies, through MKIs, to RET-specific inhibitors).
Targeting RET alterations in cancer: Recent progress and future directions
Source : https://www.sciencedirect.com/science/article/abs/pii/S1040842822003067?via=ihub
Genomic alterations in the receptor tyrosine kinase RET represent actionable driver events in several cancer types. Activation of the kinase domain by point mutations represents a pathognomonic event in medullary...
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Conclusions: An important mechanism of eventual resistance to RET inhibitors is the emergence of secondary drug resistance mutations, particularly in the solvent front, and several promising compounds are in development to overcome these mutations. Mechanisms of acquired resistance that bypass RET signaling altogether have also been...