The tankyrase inhibitor OM-153 demonstrates antitumor efficacy and a therapeutic window in mouse models
SA Brinch, E Amundsen-Isaksen, S Espada… - Cancer Research …, 2022 - AACR
The catalytic enzymes tankyrase 1 and 2 (TNKS1/2) alter protein turnover by poly-ADP-
ribosylating target proteins, which earmark them for degradation by the ubiquitin–
proteasomal system. Prominent targets of the catalytic activity of TNKS1/2 include AXIN
proteins, resulting in TNKS1/2 being attractive biotargets for addressing of oncogenic WNT/β-
catenin signaling. Although several potent small molecules have been developed to inhibit
TNKS1/2, there are currently no TNKS1/2 inhibitors available in clinical practice. The …
ribosylating target proteins, which earmark them for degradation by the ubiquitin–
proteasomal system. Prominent targets of the catalytic activity of TNKS1/2 include AXIN
proteins, resulting in TNKS1/2 being attractive biotargets for addressing of oncogenic WNT/β-
catenin signaling. Although several potent small molecules have been developed to inhibit
TNKS1/2, there are currently no TNKS1/2 inhibitors available in clinical practice. The …
The tankyrase inhibitor OM-153 demonstrates updates antitumor efficacy and a therapeutic window in mouse models
SA Brinch, E Amundsen-Isaksen, S Espada… - 2022 - oulurepo.oulu.fi
The catalytic enzymes tankyrase 1 and 2 (TNKS1/2) alter protein turnover by poly-ADP-
ribosylating target proteins, which earmark them for degradation by the ubiquitin–
proteasomal system. Prominent targets of the catalytic activity of TNKS1/2 include AXIN
proteins, resulting in TNKS1/2 being attractive biotargets for addressing of oncogenic WNT/β-
catenin signaling. Although several potent small molecules have been developed to inhibit
TNKS1/2, there are currently no TNKS1/2 inhibitors available in clinical practice. The …
ribosylating target proteins, which earmark them for degradation by the ubiquitin–
proteasomal system. Prominent targets of the catalytic activity of TNKS1/2 include AXIN
proteins, resulting in TNKS1/2 being attractive biotargets for addressing of oncogenic WNT/β-
catenin signaling. Although several potent small molecules have been developed to inhibit
TNKS1/2, there are currently no TNKS1/2 inhibitors available in clinical practice. The …
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