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tak-981

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Overview

NCI Definition [1]:
A small molecule inhibitor of sumoylation, with potential immune-activating and antineoplastic activities. Upon intravenous administration, TAK-981 targets and covalently binds to the small ubiquitin-like modifier (SUMO; small ubiquitin-related modifier) protein, forming an adduct with SUMO protein (TAK-981-SUMO adduct). This prevents the transfer of SUMO from the SUMO-activating enzyme (SAE) to SUMO-conjugating enzyme UBC9. This prevents SUMO conjugation to lysine residues on target proteins and abrogates many sumoylated protein-mediated cellular processes that play key roles in tumor cells, including proliferation, DNA repair, metastasis and survival. In addition, by preventing sumoylation, TAK-981 is able to increase the production of type 1 interferon (IFN), thereby increasing type 1 IFN-mediated signaling, activating innate effector cells and enhancing the antitumor innate immune responses. This may further increase tumor cell killing. Sumoylation, a post-translational modification that attaches the SUMO protein to target proteins, plays a key role in regulating their activity, function, subcellular localization and stability. Sumoylation also plays a key role in inhibiting innate immune responses, specifically by inhibiting the pattern recognition receptor (PRR) pathway and preventing type 1 IFN expression. Abnormal sumoylation of target proteins is associated with many cancers.

Clinical Trials

View Clinical Trials for tak-981

Tak-981 has been investigated in 5 clinical trials, of which 5 are open and 0 are closed. Of the trials investigating tak-981, 1 is early phase 1 (1 open) and 4 are phase 1/phase 2 (4 open).

MS4A1 Expression and Microsatellite Stable (MSS) are the most frequent biomarker inclusion criteria for tak-981 clinical trials.

Colorectal carcinoma, cervical adenocarcinoma, and cervical adenosquamous carcinoma are the most common diseases being investigated in tak-981 clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Tak-981
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating tak-981 and the cancer types associated with these biomarkers. These numbers are derived from a set of 5,956 clinical trials for which biomarker status defines treatment.

Drug Details

Synonyms [2]:
tak981, sumoylation inhibitor tak-981, tak 981
Drug Target(s) [2]:
SUMO1, SUMO2, SUMO3, SUMO4
NCIT ID [1]:
C156270

References

1. National Cancer Institute. NCI Thesaurus Version 18.11d. https://ncit.nci.nih.gov/ncitbrowser/. [2018-07-30] [2018-08-02].

2. All assertions and clinical trial landscape data are curated from primary sources. You can read more about the curation process here.