Chaikuad, Apirat : rechercher sur Z-Library

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1

Furo[3,2- b ]pyridine: A Privileged Scaffold for Highly Selective Kinase Inhibitors and Effective Modulators of the Hedgehog Pathway

Němec, Václav, Hylsová, Michaela, Maier, Lukáš, Flegel, Jana, Sievers, Sonja, Ziegler, Slava, Schroeder, Martin, Berger, Benedict-Tilman, Chaikuad, Apirat, Valčíková, Barbora, Uldrijan, Stjepan, Drápe

Journal:

Angewandte Chemie

Année:

2018

Langue:

english

Fichier:

PDF, 1.41 MB

english, 2018

2

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

Chaikuad, Apirat, M C Tacconi, Eliana, Zimmer, Jutta, Liang, Yanke, Gray, Nathanael S, Tarsounas, Madalena, Knapp, Stefan

Journal:

Nature Chemical Biology

Année:

2014

Langue:

english

Fichier:

PDF, 4.50 MB

english, 2014

3

Structure-based approaches towards identification of fragments for the low-druggability ATAD2 bromodomain

Chaikuad, Apirat, Petros, Andrew M., Fedorov, Oleg, Xu, Jing, Knapp, Stefan

Journal:

Année:

2014

Langue:

english

Fichier:

PDF, 752 KB

english, 2014

4

The Cysteinome of Protein Kinases as a Target in Drug Development

Chaikuad, Apirat, Koch, Pierre, Laufer, Stefan A., Knapp, Stefan

Journal:

Angewandte Chemie International Edition

Année:

2018

Fichier:

PDF, 1.33 MB

2018

5

Discovery of first in vivo active inhibitors of soluble epoxide hydrolase (sEH) phosphatase domain

Kramer, Jan S, Woltersdorf, Stefano, Duflot, Thomas, Hiesinger, Kerstin, Lillich, Felix F, Knöll, Felix, Wittmann, Sandra K, Klingler, Franca M, Brunst, Steffen, Chaikuad, Apirat, Morisseau, Christoph

Journal:

Journal of Medicinal Chemistry

Année:

2019

Langue:

english

Fichier:

PDF, 1.42 MB

english, 2019

6

Hepatitis Delta Virus histone mimicry drives the recruitment of chromatin remodelers for viral RNA replication

Abeywickrama-Samarakoon, Natali, Cortay, Jean-Claude, Sureau, Camille, Müller, Susanne, Alfaiate, Dulce, Guerrieri, Francesca, Chaikuad, Apirat, Schröder, Martin, Merle, Philippe, Levrero, Massimo, Dé

Journal:

Nature Communications

Année:

2020

Langue:

english

Fichier:

PDF, 1.70 MB

english, 2020

7

Conservation of structure and activity inPlasmodiumpurine nucleoside phosphorylases

Apirat Chaikuad, R Leo Brady

Journal:

BMC Structural Biology

Année:

2009

Langue:

english

Fichier:

PDF, 3.10 MB

english, 2009

8

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

Chaikuad, Apirat, Pilka, Ewa S, De Riso, Antonio, von Delft, Frank, Kavanagh, Kathryn L, Vénien-Bryan, Catherine, Oppermann, Udo, Yue, Wyatt W

Journal:

BMC Structural Biology

Année:

2012

Langue:

english

Fichier:

PDF, 3.00 MB

english, 2012

9

Structure and kinetic characterization of human sperm-specific glyceraldehyde-3-phosphate dehydrogenase, GAPDS

Chaikuad, Apirat, Shafqat, Naeem, Al‑Mokhtar, Ruby, Cameron, Gus, Clarke, Anthony R., Brady, R. Leo, Oppermann, Udo, Frayne, Jan, Yue, Wyatt W.

Journal:

Biochemical Journal

Année:

2011

Langue:

english

Fichier:

PDF, 1.52 MB

english, 2011

10

Structure of Lactate Dehydrogenase from Plasmodium vivax : Complexes with NADH and APADH †

Chaikuad, Apirat, Fairweather, Victoria, Conners, Rebecca, Joseph-Horne, Tim, Turgut-Balik, Dilek, Brady, R. Leo

Journal:

Année:

2005

Langue:

english

Fichier:

PDF, 370 KB

english, 2005

11

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

De Nicola, Gian Felice, Martin, Eva Denise, Chaikuad, Apirat, Bassi, Rekha, Clark, James, Martino, Luigi, Verma, Sharwari, Sicard, Pierre, Tata, Renée, Atkinson, R Andrew, Knapp, Stefan, Conte, Maria

Journal:

Nature Structural and Molecular Biology

Année:

2013

Langue:

english

Fichier:

PDF, 1.57 MB

english, 2013

12

Copper is required for oncogenic BRAF signalling and tumorigenesis

Brady, Donita C., Crowe, Matthew S., Turski, Michelle L., Hobbs, G. Aaron, Yao, Xiaojie, Chaikuad, Apirat, Knapp, Stefan, Xiao, Kunhong, Campbell, Sharon L., Thiele, Dennis J., Counter, Christopher M.

Journal:

Année:

2014

Langue:

english

Fichier:

PDF, 4.14 MB

english, 2014

13

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

Chaikuad, Apirat, Keates, Tracy, Vincke, Cécile, Kaufholz, Melanie, Zenn, Michael, Zimmermann, Bastian, Gutiérrez, Carlos, Zhang, Rong‑guang, Hatzos‑Skintges, Catherine, Joachimiak, Andrzej, Muylderma

Journal:

Biochemical Journal

Année:

2014

Langue:

english

Fichier:

PDF, 2.22 MB

english, 2014

14

Targeting Low-Druggability Bromodomains: Fragment Based Screening and Inhibitor Design against the BAZ2B Bromodomain

Ferguson, Fleur M., Fedorov, Oleg, Chaikuad, Apirat, Philpott, Martin, Muniz, Joao R. C., Felletar, Ildiko, von Delft, Frank, Heightman, Tom, Knapp, Stefan, Abell, Chris, Ciulli, Alessio

Journal:

Journal of Medicinal Chemistry

Année:

2013

Langue:

english

Fichier:

PDF, 1.43 MB

english, 2013

15

Bisubstrate Inhibitor Approach for Targeting Mitotic Kinase Haspin

Kestav, Katrin, Lavogina, Darja, Raidaru, Gerda, Chaikuad, Apirat, Knapp, Stefan, Uri, Asko

Journal:

Bioconjugate Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 363 KB

english, 2015

16

Structure and Mechanism of Human UDP-glucose 6-Dehydrogenase

Egger, Sigrid, Chaikuad, Apirat, Kavanagh, Kathryn L., Oppermann, Udo, Nidetzky, Bernd

Journal:

Journal of Biological Chemistry

Année:

2011

Langue:

english

Fichier:

PDF, 3.92 MB

english, 2011

17

Small Molecules Dorsomorphin and LDN-193189 Inhibit Myostatin/GDF8 Signaling and Promote Functional Myoblast Differentiation

Horbelt, Daniel, Boergermann, Jan H., Chaikuad, Apirat, Alfano, Ivan, Williams, Eleanor, Lukonin, Ilya, Timmel, Tobias, Bullock, Alex N., Knaus, Petra

Journal:

Journal of Biological Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 4.08 MB

english, 2015

18

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

Kerr, Georgina, Sheldon, Helen, Chaikuad, Apirat, Alfano, Ivan, von Delft, Frank, Bullock, Alex N., Harris, Adrian L.

Journal:

Année:

2015

Langue:

english

Fichier:

PDF, 1.81 MB

english, 2015

19

10-Iodo-11 H -indolo[3,2- c ]quinoline-6-carboxylic Acids Are Selective Inhibitors of DYRK1A

Falke, Hannes, Chaikuad, Apirat, Becker, Anja, Loaëc, Nadège, Lozach, Olivier, Abu Jhaisha, Samira, Becker, Walter, Jones, Peter G., Preu, Lutz, Baumann, Knut, Knapp, Stefan, Meijer, Laurent, Kunick,

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 4.01 MB

english, 2015

20

Structure Enabled Design of BAZ2-ICR, A Chemical Probe Targeting the Bromodomains of BAZ2A and BAZ2B

Drouin, Ludovic, McGrath, Sally, Vidler, Lewis R., Chaikuad, Apirat, Monteiro, Octovia, Tallant, Cynthia, Philpott, Martin, Rogers, Catherine, Fedorov, Oleg, Liu, Manjuan, Akhtar, Wasim, Hayes, Angela

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 385 KB

english, 2015

21

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

Kovackova, Sona, Chang, Lei, Bekerman, Elena, Neveu, Gregory, Barouch-Bentov, Rina, Chaikuad, Apirat, Heroven, Christina, Šála, Michal, De Jonghe, Steven, Knapp, Stefan, Einav, Shirit, Herdewijn, Piet

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 1.46 MB

english, 2015

22

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

Chen, Peiling, Chaikuad, Apirat, Bamborough, Paul, Bantscheff, Marcus, Bountra, Chas, Chung, Chun-wa, Fedorov, Oleg, Grandi, Paola, Jung, David, Lesniak, Robert, Lindon, Matthew, Müller, Susanne, Phil

Journal:

Journal of Medicinal Chemistry

Année:

2015

Langue:

english

Fichier:

PDF, 7.19 MB

english, 2015

23

UDP-glucose dehydrogenase: structure and function of a potential drug target

Egger, Sigrid, Chaikuad, Apirat, Kavanagh, Kathryn L., Oppermann, Udo, Nidetzky, Bernd

Journal:

Biochemical Society Transactions

Année:

2010

Langue:

english

Fichier:

PDF, 1.03 MB

english, 2010

24

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

Morozumi, Yuichi, Boussouar, Fayçal, Tan, Minjia, Chaikuad, Apirat, Jamshidikia, Mahya, Colak, Gozde, He, Huang, Nie, Litong, Petosa, Carlo, de Dieuleveult, Maud, Curtet, Sandrine, Vitte, Anne-Laure,

Journal:

Journal of Molecular Cell Biology

Année:

2015

Fichier:

PDF, 1.95 MB

2015

25

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

Morozumi, Yuichi, Boussouar, Fayçal, Tan, Minjia, Chaikuad, Apirat, Jamshidikia, Mahya, Colak, Gozde, He, Huang, Nie, Litong, Petosa, Carlo, de Dieuleveult, Maud, Curtet, Sandrine, Vitte, Anne-Laure,

Journal:

Journal of Molecular Cell Biology

Année:

2015

Langue:

english

Fichier:

PDF, 1.95 MB

english, 2015

26

The ins and outs of selective kinase inhibitor development

Müller, Susanne, Chaikuad, Apirat, Gray, Nathanael S, Knapp, Stefan

Journal:

Nature Chemical Biology

Année:

2015

Langue:

english

Fichier:

PDF, 940 KB

english, 2015

27

Structure-based identification of inhibitory fragments targeting the p300/CBP-associated factor bromodomain

Chaikuad, Apirat, Lang, Steffen, Brennan, Paul E, Temperini, Claudia, Fedorov, Oleg, Hollander, Johan, Nachane, Ruta, Abell, Chris, Müller, Susanne, Siegal, Gregg, Knapp, Stefan

Journal:

Journal of Medicinal Chemistry

Année:

2016

Langue:

english

Fichier:

PDF, 999 KB

english, 2016

28

Conformational plasticity of glycogenin and its maltosaccharide substrate during glycogen biogenesis

Apirat Chaikuad, D. Sean Froese, Georgina Berridge, Frank von Delft, Udo Oppermann and Wyatt W. Yue

Journal:

Proceedings of the National Academy of Sciences

Année:

2011

Langue:

english

Fichier:

PDF, 2.13 MB

english, 2011

29

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

Lavogina, Darja, Kestav, Katrin, Chaikuad, Apirat, Heroven, Christina, Knapp, Stefan, Uri, Asko

Journal:

Acta Crystallographica Section F Structural Biology Communications

Année:

2016

Langue:

english

Fichier:

PDF, 1.17 MB

english, 2016

30

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, Yannick J., Zeinyeh, Wael, Boibessot, Thibaut, Nauton, Lionel, Théry, Vincent, Knapp, Stefan, Chaikuad, Apirat, Loaëc, Nadège, Meijer, Laurent, Anizon, Fabrice, Giraud, Francis, Moreau, Pascale

Journal:

European Journal of Medicinal Chemistry

Année:

2016

Langue:

english

Fichier:

PDF, 607 KB

english, 2016

31

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

Chaikuad, Apirat, Bullock, Alex N.

Journal:

Cold Spring Harbor Perspectives in Biology

Année:

2016

Langue:

english

Fichier:

PDF, 1.13 MB

english, 2016

32

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, Apirat, Diharce, Julien, Schröder, Martin, Foucourt, Alicia, Leblond, Bertrand, Casagrande, Anne-Sophie, Desire, Laurent, Bonnet, Pascal, Knapp, Stefan, Besson, Thierry

Journal:

Journal of Medicinal Chemistry

Année:

2016

Langue:

english

Fichier:

PDF, 884 KB

english, 2016

33

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

Forster, Michael, Chaikuad, Apirat, Bauer, Silke M., Holstein, Julia, Robers, Matthew B., Corona, Cesear R., Gehringer, Matthias, Pfaffenrot, Ellen, Ghoreschi, Kamran, Knapp, Stefan, Laufer, Stefan A.

Journal:

Cell Chemical Biology

Année:

2016

Langue:

english

Fichier:

PDF, 2.10 MB

english, 2016

34

Discovery of a PCAF Bromodomain Chemical Probe

Moustakim, Moses, Clark, Peter G. K., Trulli, Laura, Fuentes de Arriba, Angel L., Ehebauer, Matthias T., Chaikuad, Apirat, Murphy, Emma J., Mendez-Johnson, Jacqui, Daniels, Danette, Hou, Chun-Feng D.,

Journal:

Angewandte Chemie International Edition

Année:

2017

Langue:

english

Fichier:

PDF, 1.02 MB

english, 2017

35

Back Cover: Discovery of a PCAF Bromodomain Chemical Probe (Angew. Chem. Int. Ed. 3/2017)

Moustakim, Moses, Clark, Peter G. K., Trulli, Laura, Fuentes de Arriba, Angel L., Ehebauer, Matthias T., Chaikuad, Apirat, Murphy, Emma J., Mendez-Johnson, Jacqui, Daniels, Danette, Hou, Chun-Feng D.,

Journal:

Angewandte Chemie International Edition

Année:

2017

Fichier:

PDF, 1.38 MB

2017

36

Discovery of a PCAF Bromodomain Chemical Probe

Moustakim, Moses, Clark, Peter G. K., Trulli, Laura, Fuentes de Arriba, Angel L., Ehebauer, Matthias T., Chaikuad, Apirat, Murphy, Emma J., Mendez-Johnson, Jacqui, Daniels, Danette, Hou, Chun-Feng D.,

Journal:

Angewandte Chemie

Année:

2017

Langue:

english

Fichier:

PDF, 970 KB

english, 2017

37

NIH Public Access

Chaikuad, Apirat, Knapp, Stefan, Xiao, Kunhong, Campbell, Sharon L, Thiele, Dennis J

Année:

2014

Langue:

english

Fichier:

PDF, 1.64 MB

english, 2014

38

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

Walter, Anne, Chaikuad, Apirat, Loaëc, Nadège, Preu, Lutz, Knapp, Stefan, Meijer, Laurent, Kunick, Conrad, Koch, Oliver

Journal:

Molecular Informatics

Année:

2017

Langue:

english

Fichier:

PDF, 1.85 MB

english, 2017

39

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

Batson, Jennifer, Toop, Hamish D., Redondo, Clara, Babaei-Jadidi, Roya, Chaikuad, Apirat, Wearmouth, Stephen F., Gibbons, Brian, Allen, Claire, Tallant, Cynthia, Zhang, Jingxue, Du, Chunyun, Hancox, J

Journal:

ACS Chemical Biology

Année:

2017

Langue:

english

Fichier:

PDF, 1.35 MB

english, 2017

40

Rücktitelbild: Discovery of a PCAF Bromodomain Chemical Probe (Angew. Chem. 3/2017)

Moustakim, Moses, Clark, Peter G. K., Trulli, Laura, Fuentes de Arriba, Angel L., Ehebauer, Matthias T., Chaikuad, Apirat, Murphy, Emma J., Mendez-Johnson, Jacqui, Daniels, Danette, Hou, Chun-Feng D.,

Journal:

Angewandte Chemie

Année:

2017

Fichier:

PDF, 3.53 MB

2017

41

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

Chaikuad, Apirat, Knapp, Stefan, von Delft, Frank

Journal:

Acta Crystallographica Section D Biological Crystallography

Année:

2015

Langue:

english

Fichier:

PDF, 2.18 MB

english, 2015

42

A specific and covalent JNK-1 ligand selected from an encoded self-assembling chemical library

Zimmermann, Gunther, Rieder, Ulrike, Bajic, Davor, Vanetti, Sara, Chaikuad, Apirat, Knapp, Stefan, Scheuermann, Jörg, Mattarella, Martin, Neri, Dario

Journal:

Chemistry - A European Journal

Année:

2017

Langue:

english

Fichier:

PDF, 2.07 MB

english, 2017

43

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

Chaikuad, Apirat, Filippakopoulos, Panagis, Marcsisin, Sean R., Picaud, Sarah, Schröder, Martin, Sekine, Shiori, Ichijo, Hidenori, Engen, John R., Takeda, Kohsuke, Knapp, Stefan

Journal:

Année:

2017

Langue:

english

Fichier:

PDF, 4.96 MB

english, 2017

44

Characterization of a highly selective inhibitor of the Aurora kinases

Ferguson, Fleur M., Doctor, Zainab M., Chaikuad, Apirat, Sim, Taebo, Kim, Nam Doo, Knapp, Stefan, Gray, Nathanael S.

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2017

Langue:

english

Fichier:

PDF, 1.35 MB

english, 2017

45

Targeting the Protein Kinases Cysteinome

Chaikuad, Apirat, Koch, Pierre, Laufer, Stefan, Knapp, Stefan

Journal:

Angewandte Chemie International Edition

Année:

2017

Langue:

english

Fichier:

PDF, 2.78 MB

english, 2017

46

Targeting the Protein Kinases Cysteinome

Chaikuad, Apirat, Koch, Pierre, Laufer, Stefan, Knapp, Stefan

Journal:

Angewandte Chemie

Année:

2017

Langue:

english

Fichier:

PDF, 2.78 MB

english, 2017

47

Halogen-aromatic π-interactions modulate inhibitor residence time

Heroven, Christina, Georgi, Victoria, Ganotra, Gaurav K., Brennan, Paul E, Wolfreys, Finn, Wade, Rebecca C., Fernández-Montalván, Amaury E., Chaikuad, Apirat, Knapp, Stefan

Journal:

Angewandte Chemie International Edition

Année:

2018

Langue:

english

Fichier:

PDF, 2.67 MB

english, 2018

48

Halogen-aromatic π-interactions modulate inhibitor residence time

Heroven, Christina, Georgi, Victoria, Ganotra, Gaurav K., Brennan, Paul E, Wolfreys, Finn, Wade, Rebecca C., Fernández-Montalván, Amaury E., Chaikuad, Apirat, Knapp, Stefan

Journal:

Angewandte Chemie

Année:

2018

Langue:

english

Fichier:

PDF, 2.67 MB

english, 2018

49

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, Michael, Chaikuad, Apirat, Dimitrov, Teodor, Döring, Eva, Holstein, Julia, Berger, Benedict-Tilman, Gehringer, Matthias, Ghoreschi, Kamran, Müller, Susanne, Knapp, Stefan, Laufer, Stefan A.

Journal:

Journal of Medicinal Chemistry

Année:

2018

Langue:

english

Fichier:

PDF, 2.02 MB

english, 2018

50

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

Walter, Anne, Chaikuad, Apirat, Helmer, Renate, Loaëc, Nadège, Preu, Lutz, Ott, Ingo, Knapp, Stefan, Meijer, Laurent, Kunick, Conrad, Lodola, Alessio

Journal:

Année:

2018

Langue:

english

Fichier:

PDF, 9.85 MB

english, 2018