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Items: 1 to 20 of 47

1.

Development, Optimization, and Structure-Activity Relationships of Covalent-Reversible JAK3 Inhibitors Based on a Tricyclic Imidazo[5,4- d]pyrrolo[2,3- b]pyridine Scaffold.

Forster M, Chaikuad A, Dimitrov T, Döring E, Holstein J, Berger BT, Gehringer M, Ghoreschi K, Müller S, Knapp S, Laufer SA.

J Med Chem. 2018 Jun 13. doi: 10.1021/acs.jmedchem.8b00571. [Epub ahead of print]

PMID:
29852068
2.

Molecular structures of cdc2-like kinases in complex with a new inhibitor chemotype.

Walter A, Chaikuad A, Helmer R, Loaëc N, Preu L, Ott I, Knapp S, Meijer L, Kunick C.

PLoS One. 2018 May 3;13(5):e0196761. doi: 10.1371/journal.pone.0196761. eCollection 2018.

3.

Halogen-Aromatic π Interactions Modulate Inhibitor Residence Times.

Heroven C, Georgi V, Ganotra GK, Brennan P, Wolfreys F, Wade RC, Fernández-Montalván AE, Chaikuad A, Knapp S.

Angew Chem Int Ed Engl. 2018 Jun 11;57(24):7220-7224. doi: 10.1002/anie.201801666. Epub 2018 May 9.

PMID:
29601130
4.

Isoform-Selective ATAD2 Chemical Probe with Novel Chemical Structure and Unusual Mode of Action.

Fernández-Montalván AE, Berger M, Kuropka B, Koo SJ, Badock V, Weiske J, Puetter V, Holton SJ, Stöckigt D, Ter Laak A, Centrella PA, Clark MA, Dumelin CE, Sigel EA, Soutter HH, Troast DM, Zhang Y, Cuozzo JW, Keefe AD, Roche D, Rodeschini V, Chaikuad A, Díaz-Sáez L, Bennett JM, Fedorov O, Huber KVM, Hübner J, Weinmann H, Hartung IV, Gorjánácz M.

ACS Chem Biol. 2017 Nov 17;12(11):2730-2736. doi: 10.1021/acschembio.7b00708. Epub 2017 Oct 24.

PMID:
29043777
5.

The Cysteinome of Protein Kinases as a Target in Drug Development.

Chaikuad A, Koch P, Laufer SA, Knapp S.

Angew Chem Int Ed Engl. 2018 Apr 9;57(16):4372-4385. doi: 10.1002/anie.201707875. Epub 2018 Feb 2. Review.

PMID:
28994500
6.

Characterization of a highly selective inhibitor of the Aurora kinases.

Ferguson FM, Doctor ZM, Chaikuad A, Sim T, Kim ND, Knapp S, Gray NS.

Bioorg Med Chem Lett. 2017 Sep 15;27(18):4405-4408. doi: 10.1016/j.bmcl.2017.08.016. Epub 2017 Aug 10.

PMID:
28818446
7.

Structures of PGAM5 Provide Insight into Active Site Plasticity and Multimeric Assembly.

Chaikuad A, Filippakopoulos P, Marcsisin SR, Picaud S, Schröder M, Sekine S, Ichijo H, Engen JR, Takeda K, Knapp S.

Structure. 2017 Jul 5;25(7):1089-1099.e3. doi: 10.1016/j.str.2017.05.020. Epub 2017 Jun 22.

8.

A Specific and Covalent JNK-1 Ligand Selected from an Encoded Self-Assembling Chemical Library.

Zimmermann G, Rieder U, Bajic D, Vanetti S, Chaikuad A, Knapp S, Scheuermann J, Mattarella M, Neri D.

Chemistry. 2017 Jun 16;23(34):8152-8155. doi: 10.1002/chem.201701644. Epub 2017 May 30.

9.

Development of Potent, Selective SRPK1 Inhibitors as Potential Topical Therapeutics for Neovascular Eye Disease.

Batson J, Toop HD, Redondo C, Babaei-Jadidi R, Chaikuad A, Wearmouth SF, Gibbons B, Allen C, Tallant C, Zhang J, Du C, Hancox JC, Hawtrey T, Da Rocha J, Griffith R, Knapp S, Bates DO, Morris JC.

ACS Chem Biol. 2017 Mar 17;12(3):825-832. doi: 10.1021/acschembio.6b01048. Epub 2017 Feb 6.

10.

Identification of CLK1 Inhibitors by a Fragment-linking Based Virtual Screening.

Walter A, Chaikuad A, Loaëc N, Preu L, Knapp S, Meijer L, Kunick C, Koch O.

Mol Inform. 2017 Apr;36(4). doi: 10.1002/minf.201600123. Epub 2016 Dec 21.

PMID:
28000414
11.

Discovery of New Bromodomain Scaffolds by Biosensor Fragment Screening.

Navratilova I, Aristotelous T, Picaud S, Chaikuad A, Knapp S, Filappakopoulos P, Hopkins AL.

ACS Med Chem Lett. 2016 Sep 20;7(12):1213-1218. eCollection 2016 Dec 8.

12.

Discovery of a PCAF Bromodomain Chemical Probe.

Moustakim M, Clark PG, Trulli L, Fuentes de Arriba AL, Ehebauer MT, Chaikuad A, Murphy EJ, Mendez-Johnson J, Daniels D, Hou CD, Lin YH, Walker JR, Hui R, Yang H, Dorrell L, Rogers CM, Monteiro OP, Fedorov O, Huber KV, Knapp S, Heer J, Dixon DJ, Brennan PE.

Angew Chem Int Ed Engl. 2017 Jan 16;56(3):827-831. doi: 10.1002/anie.201610816. Epub 2016 Dec 14.

13.

Selective JAK3 Inhibitors with a Covalent Reversible Binding Mode Targeting a New Induced Fit Binding Pocket.

Forster M, Chaikuad A, Bauer SM, Holstein J, Robers MB, Corona CR, Gehringer M, Pfaffenrot E, Ghoreschi K, Knapp S, Laufer SA.

Cell Chem Biol. 2016 Nov 17;23(11):1335-1340. doi: 10.1016/j.chembiol.2016.10.008. Epub 2016 Nov 10.

14.

Structural Basis of Intracellular TGF-β Signaling: Receptors and Smads.

Chaikuad A, Bullock AN.

Cold Spring Harb Perspect Biol. 2016 Nov 1;8(11). pii: a022111. doi: 10.1101/cshperspect.a022111. Review.

PMID:
27549117
15.

An Unusual Binding Model of the Methyl 9-Anilinothiazolo[5,4-f] quinazoline-2-carbimidates (EHT 1610 and EHT 5372) Confers High Selectivity for Dual-Specificity Tyrosine Phosphorylation-Regulated Kinases.

Chaikuad A, Diharce J, Schröder M, Foucourt A, Leblond B, Casagrande AS, Désiré L, Bonnet P, Knapp S, Besson T.

J Med Chem. 2016 Nov 23;59(22):10315-10321. Epub 2016 Nov 2.

PMID:
27766861
16.

Co-crystal structures of the protein kinase haspin with bisubstrate inhibitors.

Lavogina D, Kestav K, Chaikuad A, Heroven C, Knapp S, Uri A.

Acta Crystallogr F Struct Biol Commun. 2016 May;72(Pt 5):339-45. doi: 10.1107/S2053230X16004611. Epub 2016 Apr 22.

17.

Discovery of pyrido[3,4-g]quinazoline derivatives as CMGC family protein kinase inhibitors: Design, synthesis, inhibitory potency and X-ray co-crystal structure.

Esvan YJ, Zeinyeh W, Boibessot T, Nauton L, Théry V, Knapp S, Chaikuad A, Loaëc N, Meijer L, Anizon F, Giraud F, Moreau P.

Eur J Med Chem. 2016 Aug 8;118:170-7. doi: 10.1016/j.ejmech.2016.04.004. Epub 2016 Apr 5.

PMID:
27128181
18.

Structure-Based Identification of Inhibitory Fragments Targeting the p300/CBP-Associated Factor Bromodomain.

Chaikuad A, Lang S, Brennan PE, Temperini C, Fedorov O, Hollander J, Nachane R, Abell C, Müller S, Siegal G, Knapp S.

J Med Chem. 2016 Feb 25;59(4):1648-53. doi: 10.1021/acs.jmedchem.5b01719. Epub 2016 Jan 13.

19.

The ins and outs of selective kinase inhibitor development.

Müller S, Chaikuad A, Gray NS, Knapp S.

Nat Chem Biol. 2015 Nov;11(11):818-21. doi: 10.1038/nchembio.1938. No abstract available.

PMID:
26485069
20.

Atad2 is a generalist facilitator of chromatin dynamics in embryonic stem cells.

Morozumi Y, Boussouar F, Tan M, Chaikuad A, Jamshidikia M, Colak G, He H, Nie L, Petosa C, de Dieuleveult M, Curtet S, Vitte AL, Rabatel C, Debernardi A, Cosset FL, Verhoeyen E, Emadali A, Schweifer N, Gianni D, Gut M, Guardiola P, Rousseaux S, Gérard M, Knapp S, Zhao Y, Khochbin S.

J Mol Cell Biol. 2016 Aug;8(4):349-62. doi: 10.1093/jmcb/mjv060. Epub 2015 Oct 12.

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