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Items: 1 to 20 of 32

1.

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 1;72(Pt 5):339-45. doi: 10.1107/S2053230X16004611. Epub 2016 Apr 22.

PMID:
27139824
2.

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 Apr 5;118:170-177. doi: 10.1016/j.ejmech.2016.04.004. [Epub ahead of print]

PMID:
27128181
3.

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.

4.

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
5.

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. 2015 Oct 12. pii: mjv060. [Epub ahead of print]

6.

A core of kinase-regulated interactomes defines the neoplastic MDSC lineage.

Gato-Cañas M, Martinez de Morentin X, Blanco-Luquin I, Fernandez-Irigoyen J, Zudaire I, Liechtenstein T, Arasanz H, Lozano T, Casares N, Chaikuad A, Knapp S, Guerrero-Setas D, Escors D, Kochan G, Santamaría E.

Oncotarget. 2015 Sep 29;6(29):27160-75. doi: 10.18632/oncotarget.4746.

7.

Defined PEG smears as an alternative approach to enhance the search for crystallization conditions and crystal-quality improvement in reduced screens.

Chaikuad A, Knapp S, von Delft F.

Acta Crystallogr D Biol Crystallogr. 2015 Aug;71(Pt 8):1627-39. doi: 10.1107/S1399004715007968. Epub 2015 Jul 28.

8.

Selective Inhibitors of Cyclin G Associated Kinase (GAK) as Anti-Hepatitis C Agents.

Kovackova S, Chang L, Bekerman E, Neveu G, Barouch-Bentov R, Chaikuad A, Heroven C, Šála M, De Jonghe S, Knapp S, Einav S, Herdewijn P.

J Med Chem. 2015 Apr 23;58(8):3393-410. doi: 10.1021/jm501759m. Epub 2015 Apr 9.

9.

Discovery and Characterization of GSK2801, a Selective Chemical Probe for the Bromodomains BAZ2A and BAZ2B.

Chen P, Chaikuad A, Bamborough P, Bantscheff M, Bountra C, Chung CW, Fedorov O, Grandi P, Jung D, Lesniak R, Lindon M, Müller S, Philpott M, Prinjha R, Rogers C, Selenski C, Tallant C, Werner T, Willson TM, Knapp S, Drewry DH.

J Med Chem. 2016 Feb 25;59(4):1410-24. doi: 10.1021/acs.jmedchem.5b00209. Epub 2015 Apr 6.

10.

10-iodo-11H-indolo[3,2-c]quinoline-6-carboxylic acids are selective inhibitors of DYRK1A.

Falke H, Chaikuad A, Becker A, Loaëc N, Lozach O, Abu Jhaisha S, Becker W, Jones PG, Preu L, Baumann K, Knapp S, Meijer L, Kunick C.

J Med Chem. 2015 Apr 9;58(7):3131-43. doi: 10.1021/jm501994d. Epub 2015 Mar 23.

11.

Structure enabled design of BAZ2-ICR, a chemical probe targeting the bromodomains of BAZ2A and BAZ2B.

Drouin L, McGrath S, Vidler LR, Chaikuad A, Monteiro O, Tallant C, Philpott M, Rogers C, Fedorov O, Liu M, Akhtar W, Hayes A, Raynaud F, Müller S, Knapp S, Hoelder S.

J Med Chem. 2015 Mar 12;58(5):2553-9. doi: 10.1021/jm501963e. Epub 2015 Feb 26.

12.

Bisubstrate inhibitor approach for targeting mitotic kinase Haspin.

Kestav K, Lavogina D, Raidaru G, Chaikuad A, Knapp S, Uri A.

Bioconjug Chem. 2015 Feb 18;26(2):225-34. doi: 10.1021/bc500464r. Epub 2015 Jan 29.

PMID:
25595038
13.

A small molecule targeting ALK1 prevents Notch cooperativity and inhibits functional angiogenesis.

Kerr G, Sheldon H, Chaikuad A, Alfano I, von Delft F, Bullock AN, Harris AL.

Angiogenesis. 2015 Apr;18(2):209-17. doi: 10.1007/s10456-014-9457-y. Epub 2015 Jan 4.

14.

Small molecules dorsomorphin and LDN-193189 inhibit myostatin/GDF8 signaling and promote functional myoblast differentiation.

Horbelt D, Boergermann JH, Chaikuad A, Alfano I, Williams E, Lukonin I, Timmel T, Bullock AN, Knaus P.

J Biol Chem. 2015 Feb 6;290(6):3390-404. doi: 10.1074/jbc.M114.604397. Epub 2014 Nov 3.

15.

A unique inhibitor binding site in ERK1/2 is associated with slow binding kinetics.

Chaikuad A, Tacconi EM, Zimmer J, Liang Y, Gray NS, Tarsounas M, Knapp S.

Nat Chem Biol. 2014 Oct;10(10):853-60. doi: 10.1038/nchembio.1629. Epub 2014 Sep 7.

16.

Modulation of the chromatin phosphoproteome by the Haspin protein kinase.

Maiolica A, de Medina-Redondo M, Schoof EM, Chaikuad A, Villa F, Gatti M, Jeganathan S, Lou HJ, Novy K, Hauri S, Toprak UH, Herzog F, Meraldi P, Penengo L, Turk BE, Knapp S, Linding R, Aebersold R.

Mol Cell Proteomics. 2014 Jul;13(7):1724-40. doi: 10.1074/mcp.M113.034819. Epub 2014 Apr 14.

17.

Copper is required for oncogenic BRAF signalling and tumorigenesis.

Brady DC, Crowe MS, Turski ML, Hobbs GA, Yao X, Chaikuad A, Knapp S, Xiao K, Campbell SL, Thiele DJ, Counter CM.

Nature. 2014 May 22;509(7501):492-6. doi: 10.1038/nature13180. Epub 2014 Apr 9.

18.

Structure of cyclin G-associated kinase (GAK) trapped in different conformations using nanobodies.

Chaikuad A, Keates T, Vincke C, Kaufholz M, Zenn M, Zimmermann B, Gutiérrez C, Zhang RG, Hatzos-Skintges C, Joachimiak A, Muyldermans S, Herberg FW, Knapp S, Müller S.

Biochem J. 2014 Apr 1;459(1):59-69. doi: 10.1042/BJ20131399.

19.

Targeting low-druggability bromodomains: fragment based screening and inhibitor design against the BAZ2B bromodomain.

Ferguson FM, Fedorov O, Chaikuad A, Philpott M, Muniz JR, Felletar I, von Delft F, Heightman T, Knapp S, Abell C, Ciulli A.

J Med Chem. 2013 Dec 27;56(24):10183-7. doi: 10.1021/jm401582c. Epub 2013 Dec 13.

20.

Mechanism and consequence of the autoactivation of p38α mitogen-activated protein kinase promoted by TAB1.

De Nicola GF, Martin ED, Chaikuad A, Bassi R, Clark J, Martino L, Verma S, Sicard P, Tata R, Atkinson RA, Knapp S, Conte MR, Marber MS.

Nat Struct Mol Biol. 2013 Oct;20(10):1182-90. doi: 10.1038/nsmb.2668. Epub 2013 Sep 15.

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