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Year Number of Results
2013 2
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2017 8
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Page 1
APC/PIK3CA mutations and β-catenin status predict tankyrase inhibitor sensitivity of patient-derived colorectal cancer cells.
Chen M, Mashima T, Oishi T, Muramatsu Y, Seto Y, Takamatsu M, Kawata N, Morino S, Nakamura A, Inaba S, Yuan X, Maruyama K, Suzuki M, Sato A, Yoshida H, Jang MK, Mizutani A, Takeuchi K, Yamaguchi K, Shirai F, Nagayama S, Katayama R, Seimiya H. Chen M, et al. Br J Cancer. 2024 Jan;130(1):151-162. doi: 10.1038/s41416-023-02484-8. Epub 2023 Nov 15. Br J Cancer. 2024. PMID: 37968472
METHODS: Using 47 CRC patient-derived cells (PDCs), we examined correlations between the sensitivity to tankyrase inhibitors (G007-LK and RK-582), driver mutations, and the expressions of signaling factors. ...
METHODS: Using 47 CRC patient-derived cells (PDCs), we examined correlations between the sensitivity to tankyrase inhibitors (G007- …
Design, synthesis, and biological activity evaluation of new tankyrase-2 directed inhibitors.
Zhang X, Pang W, Li T, Lin T, Yuan J, Xu S. Zhang X, et al. Chem Biol Drug Des. 2024 Jan;103(1):e14360. doi: 10.1111/cbdd.14360. Epub 2023 Oct 10. Chem Biol Drug Des. 2024. PMID: 37814809
Among them, compound 14e showed better inhibition potency against TNKS2 in comparison with G007-LK, one of the most potent preclinical stage TNKS inhibitor. ...
Among them, compound 14e showed better inhibition potency against TNKS2 in comparison with G007-LK, one of the most potent pre …
Differential requirement of Hippo cascade during CTNNB1 or AXIN1 mutation-driven hepatocarcinogenesis.
Liang B, Wang H, Qiao Y, Wang X, Qian M, Song X, Zhou Y, Zhang Y, Shang R, Che L, Chen Y, Huang Z, Wu H, Monga SP, Zeng Y, Calvisi DF, Chen X, Chen X. Liang B, et al. Hepatology. 2023 Jun 1;77(6):1929-1942. doi: 10.1002/hep.32693. Epub 2022 Oct 18. Hepatology. 2023. PMID: 35921500
Hepatocyte-specific inducible TTR-CreER T2KO system was applied to evaluate the role of Yap;Taz during tumor progression. Cabozantinib and G007-LK combinational treatment were tested in vitro and in vivo . ...Genetic deletion of YAP/TAZ suppresses already formed c-M …
Hepatocyte-specific inducible TTR-CreER T2KO system was applied to evaluate the role of Yap;Taz during tumor progression. Cabozantinib and …
Tankyrase-selective inhibitor STP1002 shows preclinical antitumour efficacy without on-target toxicity in the gastrointestinal tract.
Kim DY, Kwon YJ, Seo WY, Kim UI, Ahn S, Choi SM, Bang HT, Kim K, Kim JS. Kim DY, et al. Eur J Cancer. 2022 Sep;173:41-51. doi: 10.1016/j.ejca.2022.06.031. Epub 2022 Jul 15. Eur J Cancer. 2022. PMID: 35849876
STP1002 showed no significant on-target toxicity in the GI tract compared to G007-LK, which shows severe ileum toxicity in preclinical animal models. ...
STP1002 showed no significant on-target toxicity in the GI tract compared to G007-LK, which shows severe ileum toxicity in pre …
Identification of response signatures for tankyrase inhibitor treatment in tumor cell lines.
Mygland L, Brinch SA, Strand MF, Olsen PA, Aizenshtadt A, Lund K, Solberg NT, Lycke M, Thorvaldsen TE, Espada S, Misaghian D, Page CM, Agafonov O, Nygård S, Chi NW, Lin E, Tan J, Yu Y, Costa M, Krauss S, Waaler J. Mygland L, et al. iScience. 2021 Jul 1;24(7):102807. doi: 10.1016/j.isci.2021.102807. eCollection 2021 Jul 23. iScience. 2021. PMID: 34337362 Free PMC article.
Here, we characterized the response signatures and the in-depth mechanisms for the antiproliferative effect of tankyrase inhibition (TNKSi). The TNKS1/2-specific inhibitor G007-LK was used to screen 537 human tumor cell lines and a panel of particularly TNKSi-sensit …
Here, we characterized the response signatures and the in-depth mechanisms for the antiproliferative effect of tankyrase inhibition (TNKSi). …
Targeting of canonical WNT signaling ameliorates experimental sclerodermatous chronic graft-versus-host disease.
Zhang Y, Shen L, Dreißigacker K, Zhu H, Trinh-Minh T, Meng X, Tran-Manh C, Dees C, Matei AE, Chen CW, Ditschkowski M, Krauss S, Winkler J, Wolff D, Ziemer M, Beilhack A, Karrer S, Herr W, Mackensen A, Schett G, Spriewald BM, Distler JHW. Zhang Y, et al. Blood. 2021 Apr 29;137(17):2403-2416. doi: 10.1182/blood.2020008720. Blood. 2021. PMID: 33529322 Free article.
WNT signaling was activated in human sclGVHD with increased nuclear accumulation of the transcription factor beta-catenin and a WNT-biased gene expression signature in lesional skin. Treatment with the highly selective tankryase inhibitor G007-LK, the CK1alpha agoni …
WNT signaling was activated in human sclGVHD with increased nuclear accumulation of the transcription factor beta-catenin and a WNT-biased g …
A Small-Molecule Tankyrase Inhibitor Reduces Glioma Stem Cell Proliferation and Sphere Formation.
Kierulf-Vieira KS, Sandberg CJ, Waaler J, Lund K, Skaga E, Saberniak BM, Panagopoulos I, Brandal P, Krauss S, Langmoen IA, Vik-Mo EO. Kierulf-Vieira KS, et al. Cancers (Basel). 2020 Jun 19;12(6):1630. doi: 10.3390/cancers12061630. Cancers (Basel). 2020. PMID: 32575464 Free PMC article.
Treatment with G007-LK decreased in vitro proliferation and sphere formation in all four primary GSC cultures in a dose-dependent manner. G007-LK treatment altered the expression of key downstream WNT/beta-catenin and Hippo signaling pathway-related pr …
Treatment with G007-LK decreased in vitro proliferation and sphere formation in all four primary GSC cultures in a dose-depend …
Tankyrase inhibition sensitizes melanoma to PD-1 immune checkpoint blockade in syngeneic mouse models.
Waaler J, Mygland L, Tveita A, Strand MF, Solberg NT, Olsen PA, Aizenshtadt A, Fauskanger M, Lund K, Brinch SA, Lycke M, Dybing E, Nygaard V, Bøe SL, Heintz KM, Hovig E, Hammarström C, Corthay A, Krauss S. Waaler J, et al. Commun Biol. 2020 Apr 24;3(1):196. doi: 10.1038/s42003-020-0916-2. Commun Biol. 2020. PMID: 32332858 Free PMC article.
Here we show that a specific small-molecule tankyrase inhibitor, G007-LK, decreases WNT/beta-catenin and YAP signaling in the syngeneic murine B16-F10 and Clone M-3 melanoma models and sensitizes the tumors to anti-PD-1 immune checkpoint therapy. ...
Here we show that a specific small-molecule tankyrase inhibitor, G007-LK, decreases WNT/beta-catenin and YAP signaling in the …
Tankyrase inhibition ameliorates lipid disorder via suppression of PGC-1α PARylation in db/db mice.
Wang H, Kuusela S, Rinnankoski-Tuikka R, Dumont V, Bouslama R, Ramadan UA, Waaler J, Linden AM, Chi NW, Krauss S, Pirinen E, Lehtonen S. Wang H, et al. Int J Obes (Lond). 2020 Aug;44(8):1691-1702. doi: 10.1038/s41366-020-0573-z. Epub 2020 Apr 21. Int J Obes (Lond). 2020. PMID: 32317752 Free PMC article.
OBJECTIVE: Human TNKS, encoding tankyrase 1 (TNKS1), localizes to a susceptibility locus for obesity and type 2 diabetes mellitus (T2DM). Here, we addressed the therapeutic potential of G007-LK, a TNKS-specific inhibitor, for obesity and T2DM. METHODS: We administer …
OBJECTIVE: Human TNKS, encoding tankyrase 1 (TNKS1), localizes to a susceptibility locus for obesity and type 2 diabetes mellitus (T2DM). He …
Tankyrase disrupts metabolic homeostasis and promotes tumorigenesis by inhibiting LKB1-AMPK signalling.
Li N, Wang Y, Neri S, Zhen Y, Fong LWR, Qiao Y, Li X, Chen Z, Stephan C, Deng W, Ye R, Jiang W, Zhang S, Yu Y, Hung MC, Chen J, Lin SH. Li N, et al. Nat Commun. 2019 Sep 25;10(1):4363. doi: 10.1038/s41467-019-12377-1. Nat Commun. 2019. PMID: 31554794 Free PMC article.
LKB1 activation by tankyrase inhibitors induces AMPK activation and suppresses tumorigenesis. Similarly, the tankyrase inhibitor G007-LK effectively regulates liver metabolism and glycemic control in diabetic mice in a LKB1-dependent manner. ...
LKB1 activation by tankyrase inhibitors induces AMPK activation and suppresses tumorigenesis. Similarly, the tankyrase inhibitor G007 …
29 results