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Items: 35

1.

Design, Synthesis, and Biological Evaluation of Retinoic Acid-Related Orphan Receptor γt (RORγt) Agonist Structure-Based Functionality Switching Approach from In House RORγt Inverse Agonist to RORγt Agonist.

Yukawa T, Nara Y, Kono M, Sato A, Oda T, Takagi T, Sato T, Banno Y, Taya N, Imada T, Shiokawa Z, Negoro N, Kawamoto T, Koyama R, Uchiyama N, Skene R, Hoffman I, Chen CH, Sang B, Snell G, Katsuyama R, Yamamoto S, Shirai J.

J Med Chem. 2019 Feb 4. doi: 10.1021/acs.jmedchem.8b01181. [Epub ahead of print]

PMID:
30652849
2.

Discovery of [ cis-3-({(5 R)-5-[(7-Fluoro-1,1-dimethyl-2,3-dihydro-1 H-inden-5-yl)carbamoyl]-2-methoxy-7,8-dihydro-1,6-naphthyridin-6(5 H)-yl}carbonyl)cyclobutyl]acetic Acid (TAK-828F) as a Potent, Selective, and Orally Available Novel Retinoic Acid Receptor-Related Orphan Receptor γt Inverse Agonist.

Kono M, Ochida A, Oda T, Imada T, Banno Y, Taya N, Masada S, Kawamoto T, Yonemori K, Nara Y, Fukase Y, Yukawa T, Tokuhara H, Skene R, Sang BC, Hoffman ID, Snell GP, Uga K, Shibata A, Igaki K, Nakamura Y, Nakagawa H, Tsuchimori N, Yamasaki M, Shirai J, Yamamoto S.

J Med Chem. 2018 Apr 12;61(7):2973-2988. doi: 10.1021/acs.jmedchem.8b00061. Epub 2018 Mar 14.

PMID:
29510038
3.

Identification of novel quinazolinedione derivatives as RORγt inverse agonist.

Fukase Y, Sato A, Tomata Y, Ochida A, Kono M, Yonemori K, Koga K, Okui T, Yamasaki M, Fujitani Y, Nakagawa H, Koyama R, Nakayama M, Skene R, Sang BC, Hoffman I, Shirai J, Yamamoto S.

Bioorg Med Chem. 2018 Feb 1;26(3):721-736. doi: 10.1016/j.bmc.2017.12.039. Epub 2017 Dec 28.

PMID:
29342416
4.

Discovery of orally efficacious RORγt inverse agonists, part 1: Identification of novel phenylglycinamides as lead scaffolds.

Shirai J, Tomata Y, Kono M, Ochida A, Fukase Y, Sato A, Masada S, Kawamoto T, Yonemori K, Koyama R, Nakagawa H, Nakayama M, Uga K, Shibata A, Koga K, Okui T, Shirasaki M, Skene R, Sang B, Hoffman I, Lane W, Fujitani Y, Yamasaki M, Yamamoto S.

Bioorg Med Chem. 2018 Jan 15;26(2):483-500. doi: 10.1016/j.bmc.2017.12.006. Epub 2017 Dec 9.

PMID:
29262987
5.

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.

J Med Chem. 2017 Jul 13;60(13):5663-5672. doi: 10.1021/acs.jmedchem.7b00352. Epub 2017 Jun 24.

PMID:
28594552
6.

Discovery of a novel prolyl-tRNA synthetase inhibitor and elucidation of its binding mode to the ATP site in complex with l-proline.

Adachi R, Okada K, Skene R, Ogawa K, Miwa M, Tsuchinaga K, Ohkubo S, Henta T, Kawamoto T.

Biochem Biophys Res Commun. 2017 Jun 24;488(2):393-399. doi: 10.1016/j.bbrc.2017.05.064. Epub 2017 May 10.

PMID:
28501621
7.

Identification of a new class of potent Cdc7 inhibitors designed by putative pharmacophore model: Synthesis and biological evaluation of 2,3-dihydrothieno[3,2-d]pyrimidin-4(1H)-ones.

Kurasawa O, Oguro Y, Miyazaki T, Homma M, Mori K, Iwai K, Hara H, Skene R, Hoffman I, Ohashi A, Yoshida S, Ishikawa T, Cho N.

Bioorg Med Chem. 2017 Apr 1;25(7):2133-2147. doi: 10.1016/j.bmc.2017.02.021. Epub 2017 Feb 16.

PMID:
28284870
8.

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.

Bioorg Med Chem Lett. 2017 Mar 1;27(5):1311-1315. doi: 10.1016/j.bmcl.2016.10.009. Epub 2016 Oct 15.

PMID:
28169164
9.

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.

Bioorg Med Chem Lett. 2017 Feb 15;27(4):1099-1104. doi: 10.1016/j.bmcl.2016.12.024. Epub 2016 Dec 20.

PMID:
28082036
10.

Structure-Based Design and Synthesis of 3-Amino-1,5-dihydro-4H-pyrazolopyridin-4-one Derivatives as Tyrosine Kinase 2 Inhibitors.

Yogo T, Nagamiya H, Seto M, Sasaki S, Shih-Chung H, Ohba Y, Tokunaga N, Lee GN, Rhim CY, Yoon CH, Cho SY, Skene R, Yamamoto S, Satou Y, Kuno M, Miyazaki T, Nakagawa H, Okabe A, Marui S, Aso K, Yoshida M.

J Med Chem. 2016 Jan 28;59(2):733-49. doi: 10.1021/acs.jmedchem.5b01857. Epub 2016 Jan 8.

PMID:
26701356
11.

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.

Bioorg Med Chem Lett. 2013 Jun 15;23(12):3662-6. doi: 10.1016/j.bmcl.2013.02.083. Epub 2013 Feb 27.

PMID:
23664874
12.

Structure-based discovery of cellular-active allosteric inhibitors of FAK.

Tomita N, Hayashi Y, Suzuki S, Oomori Y, Aramaki Y, Matsushita Y, Iwatani M, Iwata H, Okabe A, Awazu Y, Isono O, Skene RJ, Hosfield DJ, Miki H, Kawamoto T, Hori A, Baba A.

Bioorg Med Chem Lett. 2013 Mar 15;23(6):1779-85. doi: 10.1016/j.bmcl.2013.01.047. Epub 2013 Jan 26.

PMID:
23414845
13.

Structure-based design of pyridopyrimidinediones as dipeptidyl peptidase IV inhibitors.

Lam B, Zhang Z, Stafford JA, Skene RJ, Shi L, Gwaltney SL 2nd.

Bioorg Med Chem Lett. 2012 Nov 1;22(21):6628-31. doi: 10.1016/j.bmcl.2012.08.110. Epub 2012 Sep 7.

PMID:
23025999
14.

Discovery and characterization of novel allosteric FAK inhibitors.

Iwatani M, Iwata H, Okabe A, Skene RJ, Tomita N, Hayashi Y, Aramaki Y, Hosfield DJ, Hori A, Baba A, Miki H.

Eur J Med Chem. 2013 Mar;61:49-60. doi: 10.1016/j.ejmech.2012.06.035. Epub 2012 Jun 26.

PMID:
22819505
15.

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.

J Biol Chem. 2011 May 27;286(21):18756-65. doi: 10.1074/jbc.M110.206193. Epub 2011 Mar 30.

16.

Design and synthesis of pyrimidinone and pyrimidinedione inhibitors of dipeptidyl peptidase IV.

Zhang Z, Wallace MB, Feng J, Stafford JA, Skene RJ, Shi L, Lee B, Aertgeerts K, Jennings A, Xu R, Kassel DB, Kaldor SW, Navre M, Webb DR, Gwaltney SL.

J Med Chem. 2011 Jan 27;54(2):510-24. doi: 10.1021/jm101016w. Epub 2010 Dec 27.

PMID:
21186796
17.

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.

Bioorg Med Chem Lett. 2010 May 15;20(10):3142-5. doi: 10.1016/j.bmcl.2010.03.091. Epub 2010 Mar 30.

PMID:
20392638
18.

Benzimidazole and imidazole inhibitors of histone deacetylases: Synthesis and biological activity.

Bressi JC, de Jong R, Wu Y, Jennings AJ, Brown JW, O'Connell S, Tari LW, Skene RJ, Vu P, Navre M, Cao X, Gangloff AR.

Bioorg Med Chem Lett. 2010 May 15;20(10):3138-41. doi: 10.1016/j.bmcl.2010.03.092. Epub 2010 Mar 30.

PMID:
20392637
19.

X-ray structures of the LXRalpha LBD in its homodimeric form and implications for heterodimer signaling.

Fradera X, Vu D, Nimz O, Skene R, Hosfield D, Wynands R, Cooke AJ, Haunsø A, King A, Bennett DJ, McGuire R, Uitdehaag JC.

J Mol Biol. 2010 May 28;399(1):120-32. doi: 10.1016/j.jmb.2010.04.005. Epub 2010 Apr 9.

PMID:
20382159
20.

Structure-based design and synthesis of benzimidazole derivatives as dipeptidyl peptidase IV inhibitors.

Wallace MB, Feng J, Zhang Z, Skene RJ, Shi L, Caster CL, Kassel DB, Xu R, Gwaltney SL 2nd.

Bioorg Med Chem Lett. 2008 Apr 1;18(7):2362-7. doi: 10.1016/j.bmcl.2008.02.071. Epub 2008 Mar 4.

PMID:
18346892
21.

Functional and crystal structure analysis of active site adaptations of a potent anti-angiogenic human tRNA synthetase.

Yang XL, Guo M, Kapoor M, Ewalt KL, Otero FJ, Skene RJ, McRee DE, Schimmel P.

Structure. 2007 Jul;15(7):793-805.

22.

Discovery of alogliptin: a potent, selective, bioavailable, and efficacious inhibitor of dipeptidyl peptidase IV.

Feng J, Zhang Z, Wallace MB, Stafford JA, Kaldor SW, Kassel DB, Navre M, Shi L, Skene RJ, Asakawa T, Takeuchi K, Xu R, Webb DR, Gwaltney SL 2nd.

J Med Chem. 2007 May 17;50(10):2297-300. Epub 2007 Apr 19. Erratum in: J Med Chem. 2008 Jul 24;51(14):4357.

PMID:
17441705
23.

Two conformations of a crystalline human tRNA synthetase-tRNA complex: implications for protein synthesis.

Yang XL, Otero FJ, Ewalt KL, Liu J, Swairjo MA, Köhrer C, RajBhandary UL, Skene RJ, McRee DE, Schimmel P.

EMBO J. 2006 Jun 21;25(12):2919-29. Epub 2006 May 25.

24.

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.

J Biol Chem. 2005 Feb 11;280(6):4639-48. Epub 2004 Oct 28.

25.

Structural snapshots of human HDAC8 provide insights into the class I histone deacetylases.

Somoza JR, Skene RJ, Katz BA, Mol C, Ho JD, Jennings AJ, Luong C, Arvai A, Buggy JJ, Chi E, Tang J, Sang BC, Verner E, Wynands R, Leahy EM, Dougan DR, Snell G, Navre M, Knuth MW, Swanson RV, McRee DE, Tari LW.

Structure. 2004 Jul;12(7):1325-34.

26.

Structural basis for iron binding and release by a novel class of periplasmic iron-binding proteins found in gram-negative pathogens.

Shouldice SR, Skene RJ, Dougan DR, Snell G, McRee DE, Schryvers AB, Tari LW.

J Bacteriol. 2004 Jun;186(12):3903-10.

27.

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.

J Biol Chem. 2004 Jul 23;279(30):31655-63. Epub 2004 Apr 29.

28.

Alanyl-tRNA synthetase crystal structure and design for acceptor-stem recognition.

Swairjo MA, Otero FJ, Yang XL, Lovato MA, Skene RJ, McRee DE, Ribas de Pouplana L, Schimmel P.

Mol Cell. 2004 Mar 26;13(6):829-41.

29.

Crystal structure of human dipeptidyl peptidase IV in complex with a decapeptide reveals details on substrate specificity and tetrahedral intermediate formation.

Aertgeerts K, Ye S, Tennant MG, Kraus ML, Rogers J, Sang BC, Skene RJ, Webb DR, Prasad GS.

Protein Sci. 2004 Feb;13(2):412-21. Epub 2004 Jan 10.

30.

Crystal structures that suggest late development of genetic code components for differentiating aromatic side chains.

Yang XL, Otero FJ, Skene RJ, McRee DE, Schimmel P, Ribas de Pouplana L.

Proc Natl Acad Sci U S A. 2003 Dec 23;100(26):15376-80. Epub 2003 Dec 11.

31.

Presence of ferric hydroxide clusters in mutants of Haemophilus influenzae ferric ion-binding protein A.

Shouldice SR, Skene RJ, Dougan DR, McRee DE, Tari LW, Schryvers AB.

Biochemistry. 2003 Oct 21;42(41):11908-14.

PMID:
14556621
32.

Crystal structure of Pasteurella haemolytica ferric ion-binding protein A reveals a novel class of bacterial iron-binding proteins.

Shouldice SR, Dougan DR, Williams PA, Skene RJ, Snell G, Scheibe D, Kirby S, Hosfield DJ, McRee DE, Schryvers AB, Tari LW.

J Biol Chem. 2003 Oct 17;278(42):41093-8. Epub 2003 Jul 25.

33.

High resolution structure of an alternate form of the ferric ion binding protein from Haemophilus influenzae.

Shouldice SR, Dougan DR, Skene RJ, Tari LW, McRee DE, Yu RH, Schryvers AB.

J Biol Chem. 2003 Mar 28;278(13):11513-9. Epub 2003 Jan 17.

34.

Crystal structure of a human aminoacyl-tRNA synthetase cytokine.

Yang XL, Skene RJ, McRee DE, Schimmel P.

Proc Natl Acad Sci U S A. 2002 Nov 26;99(24):15369-74. Epub 2002 Nov 11.

35.

Construct shift in the treatment of a case of homosexuality.

Skene RA.

Br J Med Psychol. 1973 Sep;46(3):287-92. No abstract available.

PMID:
4749735

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