Skene RJ - Search Results

1

The dynamic conformational landscape of the protein methyltransferase SETD8.

Chen S, Wiewiora RP, Meng F, Babault N, Ma A, Yu W, Qian K, Hu H, Zou H, Wang J, Fan S, Blum G, Pittella-Silva F, Beauchamp KA, Tempel W, Jiang H, Chen K, Skene RJ, Zheng YG, Brown PJ, Jin J, Luo C, Chodera JD, Luo M. Chen S, et al. Among authors: skene rj. Elife. 2019 May 13;8:e45403. doi: 10.7554/eLife.45403. Elife. 2019. PMID: 31081496 Free PMC article.

2

Structural analysis of the mechanism of inhibition and allosteric activation of the kinase domain of HER2 protein.

Aertgeerts K, Skene R, Yano J, Sang BC, Zou H, Snell G, Jennings A, Iwamoto K, Habuka N, Hirokawa A, Ishikawa T, Tanaka T, Miki H, Ohta Y, Sogabe S. Aertgeerts K, et al. J Biol Chem. 2011 May 27;286(21):18756-65. doi: 10.1074/jbc.M110.206193. Epub 2011 Mar 30. J Biol Chem. 2011. PMID: 21454582 Free PMC article.

3

Structural basis for the autoinhibition and STI-571 inhibition of c-Kit tyrosine kinase.

Mol CD, Dougan DR, Schneider TR, Skene RJ, Kraus ML, Scheibe DN, Snell GP, Zou H, Sang BC, Wilson KP. Mol CD, et al. Among authors: skene rj. J Biol Chem. 2004 Jul 23;279(30):31655-63. doi: 10.1074/jbc.M403319200. Epub 2004 Apr 29. J Biol Chem. 2004. PMID: 15123710 Free article.

4

Efficient synthesis of tert-butyl 3-cyano-3-cyclopropyl-2-oxopyrrolidine-4-carboxylates: Highly functionalized 2-pyrrolidinone enabling access to novel macrocyclic Tyk2 inhibitors.

Sasaki Y, Tokuhara H, Ohba Y, Okabe A, Nakayama M, Nakagawa H, Skene R, Hoffman I, Zou H, Yoshida M. Sasaki Y, et al. Bioorg Med Chem Lett. 2020 Mar 1;30(5):126963. doi: 10.1016/j.bmcl.2020.126963. Epub 2020 Jan 13. Bioorg Med Chem Lett. 2020. PMID: 31980341

5

Discovery of TAK-960: an orally available small molecule inhibitor of polo-like kinase 1 (PLK1).

Nie Z, Feher V, Natala S, McBride C, Kiryanov A, Jones B, Lam B, Liu Y, Kaldor S, Stafford J, Hikami K, Uchiyama N, Kawamoto T, Hikichi Y, Matsumoto S, Amano N, Zhang L, Hosfield D, Skene R, Zou H, Cao X, Ichikawa T. Nie Z, et al. Bioorg Med Chem Lett. 2013 Jun 15;23(12):3662-6. doi: 10.1016/j.bmcl.2013.02.083. Epub 2013 Feb 27. Bioorg Med Chem Lett. 2013. PMID: 23664874 Clinical Trial.

6

Structure-based design and SAR development of 5,6-dihydroimidazolo[1,5-f]pteridine derivatives as novel Polo-like kinase-1 inhibitors.

Kiryanov A, Natala S, Jones B, McBride C, Feher V, Lam B, Liu Y, Honda K, Uchiyama N, Kawamoto T, Hikichi Y, Zhang L, Hosfield D, Skene R, Zou H, Stafford J, Cao X, Ichikawa T. Kiryanov A, et al. Bioorg Med Chem Lett. 2017 Mar 1;27(5):1311-1315. doi: 10.1016/j.bmcl.2016.10.009. Epub 2016 Oct 15. Bioorg Med Chem Lett. 2017. PMID: 28169164

7

Exploration of the HDAC2 foot pocket: Synthesis and SAR of substituted N-(2-aminophenyl)benzamides.

Bressi JC, Jennings AJ, Skene R, Wu Y, Melkus R, De Jong R, O'Connell S, Grimshaw CE, Navre M, Gangloff AR. Bressi JC, et al. Bioorg Med Chem Lett. 2010 May 15;20(10):3142-5. doi: 10.1016/j.bmcl.2010.03.091. Epub 2010 Mar 30. Bioorg Med Chem Lett. 2010. PMID: 20392638

8

1,2,4-Triazolo-[1,5-a]pyridine HIF Prolylhydroxylase Domain-1 (PHD-1) Inhibitors With a Novel Monodentate Binding Interaction.

Ahmed S, Ayscough A, Barker GR, Canning HE, Davenport R, Downham R, Harrison D, Jenkins K, Kinsella N, Livermore DG, Wright S, Ivetac AD, Skene R, Wilkens SJ, Webster NA, Hendrick AG. Ahmed S, et al. J Med Chem. 2017 Jul 13;60(13):5663-5672. doi: 10.1021/acs.jmedchem.7b00352. Epub 2017 Jun 24. J Med Chem. 2017. PMID: 28594552

9

Conformational flexibility in crystal structures of human 11beta-hydroxysteroid dehydrogenase type I provide insights into glucocorticoid interconversion and enzyme regulation.

Hosfield DJ, Wu Y, Skene RJ, Hilgers M, Jennings A, Snell GP, Aertgeerts K. Hosfield DJ, et al. Among authors: skene rj. J Biol Chem. 2005 Feb 11;280(6):4639-48. doi: 10.1074/jbc.M411104200. Epub 2004 Oct 28. J Biol Chem. 2005. PMID: 15513927 Free article.

10

Structure-based optimization of 1H-imidazole-2-carboxamides as Axl kinase inhibitors utilizing a Mer mutant surrogate.

Keung W, Boloor A, Brown J, Kiryanov A, Gangloff A, Lawson JD, Skene R, Hoffman I, Atienza J, Kahana J, De Jong R, Farrell P, Balakrishna D, Halkowycz P. Keung W, et al. Bioorg Med Chem Lett. 2017 Feb 15;27(4):1099-1104. doi: 10.1016/j.bmcl.2016.12.024. Epub 2016 Dec 20. Bioorg Med Chem Lett. 2017. PMID: 28082036

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