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Items: 1 to 20 of 161

1.

Enabling structure-based drug design of Tyk2 through co-crystallization with a stabilizing aminoindazole inhibitor.

Argiriadi MA, Goedken ER, Banach D, Borhani DW, Burchat A, Dixon RW, Marcotte D, Overmeyer G, Pivorunas V, Sadhukhan R, Sousa S, Moore NS, Tomlinson M, Voss J, Wang L, Wishart N, Woller K, Talanian RV.

BMC Struct Biol. 2012 Sep 20;12:22. doi: 10.1186/1472-6807-12-22.

2.

Rational mutagenesis to support structure-based drug design: MAPKAP kinase 2 as a case study.

Argiriadi MA, Sousa S, Banach D, Marcotte D, Xiang T, Tomlinson MJ, Demers M, Harris C, Kwak S, Hardman J, Pietras M, Quinn L, DiMauro J, Ni B, Mankovich J, Borhani DW, Talanian RV, Sadhukhan R.

BMC Struct Biol. 2009 Mar 18;9:16. doi: 10.1186/1472-6807-9-16.

3.

Structural and Functional Characterization of the JH2 Pseudokinase Domain of JAK Family Tyrosine Kinase 2 (TYK2).

Min X, Ungureanu D, Maxwell S, Hammarén H, Thibault S, Hillert EK, Ayres M, Greenfield B, Eksterowicz J, Gabel C, Walker N, Silvennoinen O, Wang Z.

J Biol Chem. 2015 Nov 6;290(45):27261-70. doi: 10.1074/jbc.M115.672048. Epub 2015 Sep 10.

PMID:
26359499
4.

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
5.

Design of a peptide inhibitor of tyrosine kinase 2.

Works MG, Song B, Kibler P, Tanga MJ, Galande AK, D'Andrea A.

Protein Pept Lett. 2014 May;21(5):419-25.

PMID:
24304386
6.
7.

Lead identification of novel and selective TYK2 inhibitors.

Liang J, Tsui V, Van Abbema A, Bao L, Barrett K, Beresini M, Berezhkovskiy L, Blair WS, Chang C, Driscoll J, Eigenbrot C, Ghilardi N, Gibbons P, Halladay J, Johnson A, Kohli PB, Lai Y, Liimatta M, Mantik P, Menghrajani K, Murray J, Sambrone A, Xiao Y, Shia S, Shin Y, Smith J, Sohn S, Stanley M, Ultsch M, Zhang B, Wu LC, Magnuson S.

Eur J Med Chem. 2013 Sep;67:175-87. doi: 10.1016/j.ejmech.2013.03.070. Epub 2013 May 14.

PMID:
23867602
8.

Structure-driven HtL: design and synthesis of novel aminoindazole inhibitors of c-Jun N-terminal kinase activity.

Stocks MJ, Barber S, Ford R, Leroux F, St-Gallay S, Teague S, Xue Y.

Bioorg Med Chem Lett. 2005 Jul 15;15(14):3459-62.

PMID:
15950471
9.

Design and synthesis of 6-anilinoindazoles as selective inhibitors of c-Jun N-terminal kinase-3.

Swahn BM, Huerta F, Kallin E, Malmström J, Weigelt T, Viklund J, Womack P, Xue Y, Ohberg L.

Bioorg Med Chem Lett. 2005 Nov 15;15(22):5095-9.

PMID:
16140012
10.

Structural and thermodynamic characterization of the TYK2 and JAK3 kinase domains in complex with CP-690550 and CMP-6.

Chrencik JE, Patny A, Leung IK, Korniski B, Emmons TL, Hall T, Weinberg RA, Gormley JA, Williams JM, Day JE, Hirsch JL, Kiefer JR, Leone JW, Fischer HD, Sommers CD, Huang HC, Jacobsen EJ, Tenbrink RE, Tomasselli AG, Benson TE.

J Mol Biol. 2010 Jul 16;400(3):413-33. doi: 10.1016/j.jmb.2010.05.020. Epub 2010 May 15.

PMID:
20478313
11.

Discovery of Tyk2 inhibitors via the virtual site-directed fragment-based drug design.

Jang WD, Kim JT, Son HY, Park SY, Cho YS, Koo TS, Lee H, Kang NS.

Bioorg Med Chem Lett. 2015 Sep 15;25(18):3947-52. doi: 10.1016/j.bmcl.2015.07.037. Epub 2015 Jul 21.

PMID:
26231159
12.

Kinase crystal identification and ATP-competitive inhibitor screening using the fluorescent ligand SKF86002.

Parker LJ, Taruya S, Tsuganezawa K, Ogawa N, Mikuni J, Honda K, Tomabechi Y, Handa N, Shirouzu M, Yokoyama S, Tanaka A.

Acta Crystallogr D Biol Crystallogr. 2014 Feb;70(Pt 2):392-404. doi: 10.1107/S1399004713028654. Epub 2014 Jan 29.

PMID:
24531473
13.

A new regulatory switch in a JAK protein kinase.

Tsui V, Gibbons P, Ultsch M, Mortara K, Chang C, Blair W, Pulk R, Stanley M, Starovasnik M, Williams D, Lamers M, Leonard P, Magnuson S, Liang J, Eigenbrot C.

Proteins. 2011 Feb;79(2):393-401. doi: 10.1002/prot.22889.

PMID:
21117080
14.

Crystal structures of IL-2-inducible T cell kinase complexed with inhibitors: insights into rational drug design and activity regulation.

Kutach AK, Villaseñor AG, Lam D, Belunis C, Janson C, Lok S, Hong LN, Liu CM, Deval J, Novak TJ, Barnett JW, Chu W, Shaw D, Kuglstatter A.

Chem Biol Drug Des. 2010 Aug;76(2):154-63. doi: 10.1111/j.1747-0285.2010.00993.x. Epub 2010 Jun 9.

PMID:
20545945
15.

Selective JAK1 inhibitor and selective Tyk2 inhibitor patents.

Norman P.

Expert Opin Ther Pat. 2012 Oct;22(10):1233-49. Epub 2012 Sep 13. Review.

PMID:
22971156
16.

Crystallography for protein kinase drug design: PKA and SRC case studies.

Breitenlechner CB, Bossemeyer D, Engh RA.

Biochim Biophys Acta. 2005 Dec 30;1754(1-2):38-49. Epub 2005 Oct 21. Review.

PMID:
16269279
17.

Crystallization to obtain protein-ligand complexes for structure-aided drug design.

Danley DE.

Acta Crystallogr D Biol Crystallogr. 2006 Jun;62(Pt 6):569-75. Epub 2006 May 12.

PMID:
16699182
18.

Development of a fluorescent-tagged kinase assay system for the detection and characterization of allosteric kinase inhibitors.

Simard JR, Getlik M, Grütter C, Pawar V, Wulfert S, Rabiller M, Rauh D.

J Am Chem Soc. 2009 Sep 23;131(37):13286-96. doi: 10.1021/ja902010p.

PMID:
19572644
19.

Lead optimization of a 4-aminopyridine benzamide scaffold to identify potent, selective, and orally bioavailable TYK2 inhibitors.

Liang J, van Abbema A, Balazs M, Barrett K, Berezhkovsky L, Blair W, Chang C, Delarosa D, DeVoss J, Driscoll J, Eigenbrot C, Ghilardi N, Gibbons P, Halladay J, Johnson A, Kohli PB, Lai Y, Liu Y, Lyssikatos J, Mantik P, Menghrajani K, Murray J, Peng I, Sambrone A, Shia S, Shin Y, Smith J, Sohn S, Tsui V, Ultsch M, Wu LC, Xiao Y, Yang W, Young J, Zhang B, Zhu BY, Magnuson S.

J Med Chem. 2013 Jun 13;56(11):4521-36. doi: 10.1021/jm400266t. Epub 2013 May 29.

PMID:
23668484
20.

Engineering of an isolated p110α subunit of PI3Kα permits crystallization and provides a platform for structure-based drug design.

Chen P, Deng YL, Bergqvist S, Falk MD, Liu W, Timofeevski S, Brooun A.

Protein Sci. 2014 Oct;23(10):1332-40. doi: 10.1002/pro.2517. Epub 2014 Aug 7.

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