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Items: 1 to 20 of 157

1.

Development of novel dual binders as potent, selective, and orally bioavailable tankyrase inhibitors.

Hua Z, Bregman H, Buchanan JL, Chakka N, Guzman-Perez A, Gunaydin H, Huang X, Gu Y, Berry V, Liu J, Teffera Y, Huang L, Egge B, Emkey R, Mullady EL, Schneider S, Andrews PS, Acquaviva L, Dovey J, Mishra A, Newcomb J, Saffran D, Serafino R, Strathdee CA, Turci SM, Stanton M, Wilson C, Dimauro EF.

J Med Chem. 2013 Dec 27;56(24):10003-15. doi: 10.1021/jm401317z. Epub 2013 Dec 11.

PMID:
24294969
2.

Discovery of novel, induced-pocket binding oxazolidinones as potent, selective, and orally bioavailable tankyrase inhibitors.

Bregman H, Chakka N, Guzman-Perez A, Gunaydin H, Gu Y, Huang X, Berry V, Liu J, Teffera Y, Huang L, Egge B, Mullady EL, Schneider S, Andrews PS, Mishra A, Newcomb J, Serafino R, Strathdee CA, Turci SM, Wilson C, DiMauro EF.

J Med Chem. 2013 Jun 13;56(11):4320-42. doi: 10.1021/jm4000038. Epub 2013 May 23.

PMID:
23701517
3.

Identification of NVP-TNKS656: the use of structure-efficiency relationships to generate a highly potent, selective, and orally active tankyrase inhibitor.

Shultz MD, Cheung AK, Kirby CA, Firestone B, Fan J, Chen CH, Chen Z, Chin DN, Dipietro L, Fazal A, Feng Y, Fortin PD, Gould T, Lagu B, Lei H, Lenoir F, Majumdar D, Ochala E, Palermo MG, Pham L, Pu M, Smith T, Stams T, Tomlinson RC, Touré BB, Visser M, Wang RM, Waters NJ, Shao W.

J Med Chem. 2013 Aug 22;56(16):6495-511. doi: 10.1021/jm400807n. Epub 2013 Aug 13.

PMID:
23844574
4.

Novel binding mode of a potent and selective tankyrase inhibitor.

Gunaydin H, Gu Y, Huang X.

PLoS One. 2012;7(3):e33740. doi: 10.1371/journal.pone.0033740. Epub 2012 Mar 16.

5.

A novel tankyrase small-molecule inhibitor suppresses APC mutation-driven colorectal tumor growth.

Lau T, Chan E, Callow M, Waaler J, Boggs J, Blake RA, Magnuson S, Sambrone A, Schutten M, Firestein R, Machon O, Korinek V, Choo E, Diaz D, Merchant M, Polakis P, Holsworth DD, Krauss S, Costa M.

Cancer Res. 2013 May 15;73(10):3132-44. doi: 10.1158/0008-5472.CAN-12-4562. Epub 2013 Mar 28.

6.

Discovery of a class of novel tankyrase inhibitors that bind to both the nicotinamide pocket and the induced pocket.

Bregman H, Gunaydin H, Gu Y, Schneider S, Wilson C, DiMauro EF, Huang X.

J Med Chem. 2013 Feb 14;56(3):1341-5. doi: 10.1021/jm301607v. Epub 2013 Jan 23.

PMID:
23316926
7.

The Discovery and Characterization of K-756, a Novel Wnt/β-Catenin Pathway Inhibitor Targeting Tankyrase.

Okada-Iwasaki R, Takahashi Y, Watanabe Y, Ishida H, Saito J, Nakai R, Asai A.

Mol Cancer Ther. 2016 Jul;15(7):1525-34. doi: 10.1158/1535-7163.MCT-15-0938. Epub 2016 Apr 25.

8.

Discovery of potent and selective nonplanar tankyrase inhibiting nicotinamide mimics.

Nkizinkiko Y, Suneel Kumar BV, Jeankumar VU, Haikarainen T, Koivunen J, Madhuri C, Yogeeswari P, Venkannagari H, Obaji E, Pihlajaniemi T, Sriram D, Lehtiö L.

Bioorg Med Chem. 2015 Aug 1;23(15):4139-49. doi: 10.1016/j.bmc.2015.06.063. Epub 2015 Jul 2.

PMID:
26183543
9.

Molecular insights on TNKS1/TNKS2 and inhibitor-IWR1 interactions.

Kirubakaran P, Kothandan G, Cho SJ, Muthusamy K.

Mol Biosyst. 2014 Feb;10(2):281-93. doi: 10.1039/c3mb70305c.

PMID:
24291818
10.

Insights into the binding of PARP inhibitors to the catalytic domain of human tankyrase-2.

Qiu W, Lam R, Voytyuk O, Romanov V, Gordon R, Gebremeskel S, Vodsedalek J, Thompson C, Beletskaya I, Battaile KP, Pai EF, Rottapel R, Chirgadze NY.

Acta Crystallogr D Biol Crystallogr. 2014 Oct;70(Pt 10):2740-53. doi: 10.1107/S1399004714017660. Epub 2014 Sep 27.

11.

Discovery of tankyrase inhibiting flavones with increased potency and isoenzyme selectivity.

Narwal M, Koivunen J, Haikarainen T, Obaji E, Legala OE, Venkannagari H, Joensuu P, Pihlajaniemi T, Lehtiö L.

J Med Chem. 2013 Oct 24;56(20):7880-9. doi: 10.1021/jm401463y. Epub 2013 Oct 11.

PMID:
24116873
12.

Tankyrase inhibitors as therapeutic targets for cancer.

Kamal A, Riyaz S, Srivastava AK, Rahim A.

Curr Top Med Chem. 2014;14(17):1967-76. Review.

PMID:
25262803
13.

Tankyrase Inhibitors Stimulate the Ability of Tankyrases to Bind Axin and Drive Assembly of β-Catenin Degradation-Competent Axin Puncta.

Martino-Echarri E, Brocardo MG, Mills KM, Henderson BR.

PLoS One. 2016 Mar 1;11(3):e0150484. doi: 10.1371/journal.pone.0150484. eCollection 2016.

14.

Tankyrase 1 Inhibitors with Drug-like Properties Identified by Screening a DNA-Encoded Chemical Library.

Samain F, Ekblad T, Mikutis G, Zhong N, Zimmermann M, Nauer A, Bajic D, Decurtins W, Scheuermann J, Brown PJ, Hall J, Gräslund S, Schüler H, Neri D, Franzini RM.

J Med Chem. 2015 Jun 25;58(12):5143-9. doi: 10.1021/acs.jmedchem.5b00432. Epub 2015 Jun 10.

PMID:
26061013
15.

Evidence for tankyrases as antineoplastic targets in lung cancer.

Busch AM, Johnson KC, Stan RV, Sanglikar A, Ahmed Y, Dmitrovsky E, Freemantle SJ.

BMC Cancer. 2013 Apr 28;13:211. doi: 10.1186/1471-2407-13-211.

16.

Tankyrases as drug targets.

Lehtiö L, Chi NW, Krauss S.

FEBS J. 2013 Aug;280(15):3576-93. doi: 10.1111/febs.12320. Epub 2013 Jun 18. Review.

17.

para-Substituted 2-phenyl-3,4-dihydroquinazolin-4-ones as potent and selective tankyrase inhibitors.

Haikarainen T, Koivunen J, Narwal M, Venkannagari H, Obaji E, Joensuu P, Pihlajaniemi T, Lehtiö L.

ChemMedChem. 2013 Dec;8(12):1978-85. doi: 10.1002/cmdc.201300337. Epub 2013 Oct 15.

PMID:
24130191
18.

Family-wide chemical profiling and structural analysis of PARP and tankyrase inhibitors.

Wahlberg E, Karlberg T, Kouznetsova E, Markova N, Macchiarulo A, Thorsell AG, Pol E, Frostell Å, Ekblad T, Öncü D, Kull B, Robertson GM, Pellicciari R, Schüler H, Weigelt J.

Nat Biotechnol. 2012 Feb 19;30(3):283-8. doi: 10.1038/nbt.2121.

PMID:
22343925
19.

A novel tankyrase inhibitor decreases canonical Wnt signaling in colon carcinoma cells and reduces tumor growth in conditional APC mutant mice.

Waaler J, Machon O, Tumova L, Dinh H, Korinek V, Wilson SR, Paulsen JE, Pedersen NM, Eide TJ, Machonova O, Gradl D, Voronkov A, von Kries JP, Krauss S.

Cancer Res. 2012 Jun 1;72(11):2822-32. doi: 10.1158/0008-5472.CAN-11-3336. Epub 2012 Mar 22.

20.

Structural basis of selective inhibition of human tankyrases.

Narwal M, Venkannagari H, Lehtiö L.

J Med Chem. 2012 Feb 9;55(3):1360-7. doi: 10.1021/jm201510p. Epub 2012 Jan 25.

PMID:
22233320

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