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Ref Type
PMID
Authors Michael A. Milhollen, Judi Shi, Tary Traore, Jessica Huck, Darshan Sappal, Jennifer Duffy, Eric Lightcap, Yuko Ishii, Jeff Ciavarri, Paul Fleming, Neil Bence and Marc L. Hyer
Title Abstract A164: The small molecule UAE inhibitor TAK-243 (MLN7243) prevents DNA damage repair and reduces cell viability/tumor growth when combined with radiation, carboplatin and docetaxel
Journal Molecular Cancer Therapeutics
Vol
Issue
Date
URL http://mct.aacrjournals.org/content/14/12_Supplement_2/A164
Abstract Text Mol Cancer Ther 2015;14(12 Suppl 2):Abstract nr A164.

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Molecular Profile Treatment Approach
Gene Name Source Synonyms Protein Domains Gene Description Gene Role
Therapy Name Drugs Efficacy Evidence Clinical Trials
Drug Name Trade Name Synonyms Drug Classes Drug Description
TAK-243 MLN7243 TAK-243 (MLN7243) is an inhibitor that selectively targets the ubiquitin activating enzyme, UBA1, which may result in inhibition of ubiquitination related processes such as cell cycle progression, apoptotic regulation, and DNA damage response (Mol Cancer Ther 2015;14(12 Suppl 2):Abstract nr A164).
Gene Variant Impact Protein Effect Variant Description Associated with drug Resistance
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
Unknown unknown Advanced Solid Tumor not applicable Radiotherapy + TAK-243 Preclinical - Cell culture Actionable In a preclinical study, the combination of TAK-243 (MLN7243) and radiotherapy resulted in elevated levels of DNA damage and growth inhibition in cancer cell lines in vitro (Mol Cancer Ther 2015;14(12 Suppl 2):Abstract nr A164). detail...
Unknown unknown Advanced Solid Tumor not applicable Docetaxel + TAK-243 Preclinical - Cell line xenograft Actionable In a preclinical study, the combination of Taxotere (docetaxel) and TAK-243 (MLN7243) resulted in synergistic and additive effects, demonstrating anti-tumor activity in xenograft tumor models (Mol Cancer Ther 2015;14(12 Suppl 2):Abstract nr A164). detail...
Unknown unknown Advanced Solid Tumor not applicable Carboplatin + TAK-243 Preclinical - Cell line xenograft Actionable In a preclinical study, the combination of Paraplatin (carboplatin) and TAK-243 (MLN7243) resulted in synergistic and additive effects, demonstrating anti-tumor activity in xenograft tumor models (Mol Cancer Ther 2015;14(12 Suppl 2):Abstract nr A164). detail...