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Results: 1 to 20 of 27

1.

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 Jul 23. [Epub ahead of print]

2.

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 1;71(Pt 8):1627-39. doi: 10.1107/S1399004715007968. Epub 2015 Jul 28.

3.

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.

PMID:
25822739
4.

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. 2015 Apr 6. [Epub ahead of print]

PMID:
25799074
5.

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.

6.

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.

7.

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
8.

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.

9.

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.

10.

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.

PMID:
25195011
11.

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.

12.

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.

13.

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.

14.

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.

15.

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.

16.

A new class of small molecule inhibitor of BMP signaling.

Sanvitale CE, Kerr G, Chaikuad A, Ramel MC, Mohedas AH, Reichert S, Wang Y, Triffitt JT, Cuny GD, Yu PB, Hill CS, Bullock AN.

PLoS One. 2013 Apr 30;8(4):e62721. doi: 10.1371/journal.pone.0062721. Print 2013.

17.

Structural basis for Cul3 protein assembly with the BTB-Kelch family of E3 ubiquitin ligases.

Canning P, Cooper CD, Krojer T, Murray JW, Pike AC, Chaikuad A, Keates T, Thangaratnarajah C, Hojzan V, Ayinampudi V, Marsden BD, Gileadi O, Knapp S, von Delft F, Bullock AN.

J Biol Chem. 2013 Mar 15;288(11):7803-14. doi: 10.1074/jbc.M112.437996. Epub 2013 Jan 24. Erratum in: J Biol Chem. 2013 Sep 27;388(39):28304. Ayinampudi, Vikram [added].

18.

Structure of the bone morphogenetic protein receptor ALK2 and implications for fibrodysplasia ossificans progressiva.

Chaikuad A, Alfano I, Kerr G, Sanvitale CE, Boergermann JH, Triffitt JT, von Delft F, Knapp S, Knaus P, Bullock AN.

J Biol Chem. 2012 Oct 26;287(44):36990-8. doi: 10.1074/jbc.M112.365932. Epub 2012 Sep 12.

19.

Structure of human aspartyl aminopeptidase complexed with substrate analogue: insight into catalytic mechanism, substrate specificity and M18 peptidase family.

Chaikuad A, Pilka ES, De Riso A, von Delft F, Kavanagh KL, Vénien-Bryan C, Oppermann U, Yue WW.

BMC Struct Biol. 2012 Jun 21;12:14. doi: 10.1186/1472-6807-12-14.

20.

Conformational plasticity of glycogenin and its maltosaccharide substrate during glycogen biogenesis.

Chaikuad A, Froese DS, Berridge G, von Delft F, Oppermann U, Yue WW.

Proc Natl Acad Sci U S A. 2011 Dec 27;108(52):21028-33. doi: 10.1073/pnas.1113921108. Epub 2011 Dec 12.

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