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2000 1
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Page 1
Blockade of Nuclear beta-Catenin Signaling via Direct Targeting of RanBP3 with NU2058 Induces Cell Senescence to Suppress Colorectal Tumorigenesis.
Zheng CC, Liao L, Liu YP, Yang YM, He Y, Zhang GG, Li SJ, Liu T, Xu WW, Li B. Zheng CC, et al. Adv Sci (Weinh). 2022 Dec;9(34):e2202528. doi: 10.1002/advs.202202528. Epub 2022 Oct 21. Adv Sci (Weinh). 2022. PMID: 36270974 Free PMC article.
Mechanistically, NU2058 increases the interaction of RanBP3 and beta-catenin to promote nuclear export of beta-catenin, which further inhibits transcription of c-Myc and cyclin D1 to induce cell senescence. Collectively, NU2058 may serve as a promising therapeutic a …
Mechanistically, NU2058 increases the interaction of RanBP3 and beta-catenin to promote nuclear export of beta-catenin, which further …
The kinase inhibitor O6-cyclohexylmethylguanine (NU2058) potentiates the cytotoxicity of cisplatin by mechanisms that are independent of its effect upon CDK2.
Harrison LR, Ottley CJ, Pearson DG, Roche C, Wedge SR, Dolan ME, Newell DR, Tilby MJ. Harrison LR, et al. Biochem Pharmacol. 2009 May 15;77(10):1586-92. doi: 10.1016/j.bcp.2009.02.018. Epub 2009 Mar 5. Biochem Pharmacol. 2009. PMID: 19426695
The aim of this study was to investigate the mechanism of cisplatin potentiation by NU2058. SQ20b, head and neck cancer cells were treated for 2h with NU2058 (100 microM) and then for a further 2h with cisplatin and NU2058. ...Furthermore, NU6102 was >1000 …
The aim of this study was to investigate the mechanism of cisplatin potentiation by NU2058. SQ20b, head and neck cancer cells were tr …
Therapeutic potential of CDK inhibitor NU2058 in androgen-independent prostate cancer.
Rigas AC, Robson CN, Curtin NJ. Rigas AC, et al. Oncogene. 2007 Dec 6;26(55):7611-9. doi: 10.1038/sj.onc.1210586. Epub 2007 Jun 18. Oncogene. 2007. PMID: 17599054
We present the first investigation of the therapeutic potential of CDK inhibitors, using the guanine-based CDK inhibitor NU2058 (CDK2 IC(50)=17 microM, CDK1 IC(50)=26 microM), in comparison with the antiandrogen bicalutamide (Casodex) in AIPC cells. A panel of AIPC cells w …
We present the first investigation of the therapeutic potential of CDK inhibitors, using the guanine-based CDK inhibitor NU2058 (CDK2 …
N2-substituted O6-cyclohexylmethylguanine derivatives: potent inhibitors of cyclin-dependent kinases 1 and 2.
Hardcastle IR, Arris CE, Bentley J, Boyle FT, Chen Y, Curtin NJ, Endicott JA, Gibson AE, Golding BT, Griffin RJ, Jewsbury P, Menyerol J, Mesguiche V, Newell DR, Noble ME, Pratt DJ, Wang LZ, Whitfield HJ. Hardcastle IR, et al. J Med Chem. 2004 Jul 15;47(15):3710-22. doi: 10.1021/jm0311442. J Med Chem. 2004. PMID: 15239650
The adenosine 5'-triphosphate (ATP) competitive cyclin-dependent kinase inhibitor O(6)-cyclohexylmethylguanine (NU2058, 1) has been employed as the lead in a structure-based drug discovery program resulting in the discovery of the potent CDK1 and -2 inhibitor NU6102 (3, IC …
The adenosine 5'-triphosphate (ATP) competitive cyclin-dependent kinase inhibitor O(6)-cyclohexylmethylguanine (NU2058, 1) has been e …
Pre-clinical evaluation of cyclin-dependent kinase 2 and 1 inhibition in anti-estrogen-sensitive and resistant breast cancer cells.
Johnson N, Bentley J, Wang LZ, Newell DR, Robson CN, Shapiro GI, Curtin NJ. Johnson N, et al. Br J Cancer. 2010 Jan 19;102(2):342-50. doi: 10.1038/sj.bjc.6605479. Epub 2009 Dec 15. Br J Cancer. 2010. PMID: 20010939 Free PMC article.
METHODS: The cellular effects of CDK2/1 siRNA knockdown and purine-based CDK2/1 inhibitors, NU2058 and NU6102, were measured in anti-estrogen-sensitive and resistant breast cancer cell lines. ...In contrast to tamoxifen, which only affected hormone-sensitive cells, NU20 …
METHODS: The cellular effects of CDK2/1 siRNA knockdown and purine-based CDK2/1 inhibitors, NU2058 and NU6102, were measured in anti- …
Identification of novel purine and pyrimidine cyclin-dependent kinase inhibitors with distinct molecular interactions and tumor cell growth inhibition profiles.
Arris CE, Boyle FT, Calvert AH, Curtin NJ, Endicott JA, Garman EF, Gibson AE, Golding BT, Grant S, Griffin RJ, Jewsbury P, Johnson LN, Lawrie AM, Newell DR, Noble ME, Sausville EA, Schultz R, Yu W. Arris CE, et al. J Med Chem. 2000 Jul 27;43(15):2797-804. doi: 10.1021/jm990628o. J Med Chem. 2000. PMID: 10956187
Substituted guanines and pyrimidines were tested as inhibitors of cyclin B1/CDK1 and cyclin A3/CDK2 and soaked into crystals of monomeric CDK2. O6-Cyclohexylmethylguanine (NU2058) was a competitive inhibitor of CDK1 and CDK2 with respect to ATP (Ki values: CDK1, 5 +/- 1 mi …
Substituted guanines and pyrimidines were tested as inhibitors of cyclin B1/CDK1 and cyclin A3/CDK2 and soaked into crystals of monomeric CD …
The development of a CDK2-docking site peptide that inhibits p53 and sensitizes cells to death.
Ferguson M, Luciani MG, Finlan L, Rankin EM, Ibbotson S, Fersht A, Hupp TR. Ferguson M, et al. Cell Cycle. 2004 Jan;3(1):80-9. Cell Cycle. 2004. PMID: 14657672
Cyclin-dependent protein kinases play important roles in cell cycle progression and are attractive targets for the design of anti-proliferative drugs. Two distinct synthetic CDK1/2 inhibitors, Roscovitine and NU2058, are pharmacologically distinct in their ability to modif …
Cyclin-dependent protein kinases play important roles in cell cycle progression and are attractive targets for the design of anti-proliferat …
Probing the ATP ribose-binding domain of cyclin-dependent kinases 1 and 2 with O(6)-substituted guanine derivatives.
Gibson AE, Arris CE, Bentley J, Boyle FT, Curtin NJ, Davies TG, Endicott JA, Golding BT, Grant S, Griffin RJ, Jewsbury P, Johnson LN, Mesguiche V, Newell DR, Noble ME, Tucker JA, Whitfield HJ. Gibson AE, et al. J Med Chem. 2002 Aug 1;45(16):3381-93. doi: 10.1021/jm020056z. J Med Chem. 2002. PMID: 12139449
Structure-based design generated (R)-(2-amino-9H-purin-6-yloxymethyl)pyrrolidin-2-one (56), which reproduces the reported hydrogen bonds formed between ATP and Asp86 and Gln131 but failed to improve inhibitory potency. Thus, the parent compound O(6)-cyclohexylmethylguanine (NU …
Structure-based design generated (R)-(2-amino-9H-purin-6-yloxymethyl)pyrrolidin-2-one (56), which reproduces the reported hydrogen bonds for …
Substituted purine analogues define a novel structural class of catalytic topoisomerase II inhibitors.
Jensen LH, Thougaard AV, Grauslund M, Søkilde B, Carstensen EV, Dvinge HK, Scudiero DA, Jensen PB, Shoemaker RH, Sehested M. Jensen LH, et al. Cancer Res. 2005 Aug 15;65(16):7470-7. doi: 10.1158/0008-5472.CAN-05-0707. Cancer Res. 2005. PMID: 16103101
In contrast, NSC35866 as well as two O6-substituted guanine analogues, O6-benzylguanine and NU2058, could inhibit topoisomerase II ATPase activity in the presence of DTT, indicating that they have a different mechanism of inhibition. ...
In contrast, NSC35866 as well as two O6-substituted guanine analogues, O6-benzylguanine and NU2058, could inhibit topoisomerase II AT …
Cyclin-dependent kinase 5 mediates pleiotrophin-induced endothelial cell migration.
Lampropoulou E, Logoviti I, Koutsioumpa M, Hatziapostolou M, Polytarchou C, Skandalis SS, Hellman U, Fousteris M, Nikolaropoulos S, Choleva E, Lamprou M, Skoura A, Megalooikonomou V, Papadimitriou E. Lampropoulou E, et al. Sci Rep. 2018 Apr 12;8(1):5893. doi: 10.1038/s41598-018-24326-x. Sci Rep. 2018. PMID: 29651006 Free PMC article.
13 results