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Items: 1 to 50 of 92

1.

Structure-Based Design of a Macrocyclic PROTAC.

Testa A, Hughes SJ, Lucas X, Wright JE, Ciulli A.

Angew Chem Int Ed Engl. 2019 Nov 19. doi: 10.1002/anie.201914396. [Epub ahead of print] Review.

PMID:
31746102
2.

Design and Characterization of SGK3-PROTAC1, an Isoform Specific SGK3 Kinase PROTAC Degrader.

Tovell H, Testa A, Zhou H, Shpiro N, Crafter C, Ciulli A, Alessi DR.

ACS Chem Biol. 2019 Sep 20;14(9):2024-2034. doi: 10.1021/acschembio.9b00505. Epub 2019 Sep 5.

3.

Bifunctional chemical probes inducing protein-protein interactions.

Maniaci C, Ciulli A.

Curr Opin Chem Biol. 2019 Oct;52:145-156. doi: 10.1016/j.cbpa.2019.07.003. Epub 2019 Aug 13. Review.

PMID:
31419624
4.

Publisher Correction: BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design.

Farnaby W, Koegl M, Roy MJ, Whitworth C, Diers E, Trainor N, Zollman D, Steurer S, Karolyi-Oezguer J, Riedmueller C, Gmaschitz T, Wachter J, Dank C, Galant M, Sharps B, Rumpel K, Traxler E, Gerstberger T, Schnitzer R, Petermann O, Greb P, Weinstabl H, Bader G, Zoephel A, Weiss-Puxbaum A, Ehrenhöfer-Wölfer K, Wöhrle S, Boehmelt G, Rinnenthal J, Arnhof H, Wiechens N, Wu MY, Owen-Hughes T, Ettmayer P, Pearson M, McConnell DB, Ciulli A.

Nat Chem Biol. 2019 Aug;15(8):846. doi: 10.1038/s41589-019-0329-z.

PMID:
31267096
5.

Protein degradation for drug discovery.

Ciulli A, Farnaby W.

Drug Discov Today Technol. 2019 Apr;31:1-3. doi: 10.1016/j.ddtec.2019.04.002. No abstract available.

PMID:
31200853
6.

Structural insights into substrate recognition by the SOCS2 E3 ubiquitin ligase.

Kung WW, Ramachandran S, Makukhin N, Bruno E, Ciulli A.

Nat Commun. 2019 Jun 10;10(1):2534. doi: 10.1038/s41467-019-10190-4.

7.

BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design.

Farnaby W, Koegl M, Roy MJ, Whitworth C, Diers E, Trainor N, Zollman D, Steurer S, Karolyi-Oezguer J, Riedmueller C, Gmaschitz T, Wachter J, Dank C, Galant M, Sharps B, Rumpel K, Traxler E, Gerstberger T, Schnitzer R, Petermann O, Greb P, Weinstabl H, Bader G, Zoephel A, Weiss-Puxbaum A, Ehrenhöfer-Wölfer K, Wöhrle S, Boehmelt G, Rinnenthal J, Arnhof H, Wiechens N, Wu MY, Owen-Hughes T, Ettmayer P, Pearson M, McConnell DB, Ciulli A.

Nat Chem Biol. 2019 Jul;15(7):672-680. doi: 10.1038/s41589-019-0294-6. Epub 2019 Jun 10. Erratum in: Nat Chem Biol. 2019 Jul 2;:.

8.

Correction to "3-Fluoro-4-hydroxyprolines: Synthesis, Conformational Analysis, and Stereoselective Recognition by the VHL E3 Ubiquitin Ligase for Targeted Protein Degradation".

Testa A, Lucas X, Castro GV, Chan KH, Wright JE, Runcie AC, Gadd MS, Harrison WTA, Ko EJ, Fletcher D, Ciulli A.

J Am Chem Soc. 2019 May 8;141(18):7644. doi: 10.1021/jacs.9b03833. Epub 2019 Apr 24. No abstract available.

PMID:
31017404
9.

Rapid and Reversible Knockdown of Endogenously Tagged Endosomal Proteins via an Optimized HaloPROTAC Degrader.

Tovell H, Testa A, Maniaci C, Zhou H, Prescott AR, Macartney T, Ciulli A, Alessi DR.

ACS Chem Biol. 2019 May 17;14(5):882-892. doi: 10.1021/acschembio.8b01016. Epub 2019 Apr 22.

10.

Cereblon versus VHL: Hijacking E3 ligases against each other using PROTACs.

Girardini M, Maniaci C, Hughes SJ, Testa A, Ciulli A.

Bioorg Med Chem. 2019 Jun 15;27(12):2466-2479. doi: 10.1016/j.bmc.2019.02.048. Epub 2019 Feb 22.

11.

RNA-seq analysis of PHD and VHL inhibitors reveals differences and similarities to the hypoxia response.

Frost J, Ciulli A, Rocha S.

Wellcome Open Res. 2019 Jan 29;4:17. doi: 10.12688/wellcomeopenres.15044.1. eCollection 2019.

12.

Highly Selective PTK2 Proteolysis Targeting Chimeras to Probe Focal Adhesion Kinase Scaffolding Functions.

Popow J, Arnhof H, Bader G, Berger H, Ciulli A, Covini D, Dank C, Gmaschitz T, Greb P, Karolyi-Özguer J, Koegl M, McConnell DB, Pearson M, Rieger M, Rinnenthal J, Roessler V, Schrenk A, Spina M, Steurer S, Trainor N, Traxler E, Wieshofer C, Zoephel A, Ettmayer P.

J Med Chem. 2019 Mar 14;62(5):2508-2520. doi: 10.1021/acs.jmedchem.8b01826. Epub 2019 Feb 22.

PMID:
30739444
13.

SPR-Measured Dissociation Kinetics of PROTAC Ternary Complexes Influence Target Degradation Rate.

Roy MJ, Winkler S, Hughes SJ, Whitworth C, Galant M, Farnaby W, Rumpel K, Ciulli A.

ACS Chem Biol. 2019 Mar 15;14(3):361-368. doi: 10.1021/acschembio.9b00092. Epub 2019 Feb 22.

14.

Spy vs. spy: selecting the best reporter for 19F NMR competition experiments.

de Castro GV, Ciulli A.

Chem Commun (Camb). 2019 Jan 29;55(10):1482-1485. doi: 10.1039/c8cc09790a.

15.

New molecular and therapeutic insights into canine diffuse large B-cell lymphoma elucidates the role of the dog as a model for human disease.

Aresu L, Ferraresso S, Marconato L, Cascione L, Napoli S, Gaudio E, Kwee I, Tarantelli C, Testa A, Maniaci C, Ciulli A, Hillmann P, Bohnacker T, Wymann MP, Comazzi S, Milan M, Riondato F, Rovere GD, Giantin M, Giannuzzi D, Bertoni F.

Haematologica. 2019 Jun;104(6):e256-e259. doi: 10.3324/haematol.2018.207027. Epub 2018 Dec 13. No abstract available.

16.

Iterative Design and Optimization of Initially Inactive Proteolysis Targeting Chimeras (PROTACs) Identify VZ185 as a Potent, Fast, and Selective von Hippel-Lindau (VHL) Based Dual Degrader Probe of BRD9 and BRD7.

Zoppi V, Hughes SJ, Maniaci C, Testa A, Gmaschitz T, Wieshofer C, Koegl M, Riching KM, Daniels DL, Spallarossa A, Ciulli A.

J Med Chem. 2019 Jan 24;62(2):699-726. doi: 10.1021/acs.jmedchem.8b01413. Epub 2018 Dec 28.

17.

Surface Probing by Fragment-Based Screening and Computational Methods Identifies Ligandable Pockets on the von Hippel-Lindau (VHL) E3 Ubiquitin Ligase.

Lucas X, Van Molle I, Ciulli A.

J Med Chem. 2018 Aug 23;61(16):7387-7393. doi: 10.1021/acs.jmedchem.8b00842. Epub 2018 Aug 8.

18.

3-Fluoro-4-hydroxyprolines: Synthesis, Conformational Analysis, and Stereoselective Recognition by the VHL E3 Ubiquitin Ligase for Targeted Protein Degradation.

Testa A, Lucas X, Castro GV, Chan KH, Wright JE, Runcie AC, Gadd MS, Harrison WTA, Ko EJ, Fletcher D, Ciulli A.

J Am Chem Soc. 2018 Jul 25;140(29):9299-9313. doi: 10.1021/jacs.8b05807. Epub 2018 Jul 12. Erratum in: J Am Chem Soc. 2019 May 8;141(18):7644.

19.

Optimization of a "bump-and-hole" approach to allele-selective BET bromodomain inhibition.

Runcie AC, Zengerle M, Chan KH, Testa A, van Beurden L, Baud MGJ, Epemolu O, Ellis LCJ, Read KD, Coulthard V, Brien A, Ciulli A.

Chem Sci. 2018 Jan 24;9(9):2452-2468. doi: 10.1039/c7sc02536j. eCollection 2018 Mar 7.

20.

Thioamide substitution to probe the hydroxyproline recognition of VHL ligands.

Soares P, Lucas X, Ciulli A.

Bioorg Med Chem. 2018 Jul 15;26(11):2992-2995. doi: 10.1016/j.bmc.2018.03.034. Epub 2018 Mar 23.

21.

Targeting Ligandable Pockets on Plant Homeodomain (PHD) Zinc Finger Domains by a Fragment-Based Approach.

Amato A, Lucas X, Bortoluzzi A, Wright D, Ciulli A.

ACS Chem Biol. 2018 Apr 20;13(4):915-921. doi: 10.1021/acschembio.7b01093. Epub 2018 Mar 20.

22.

Molecular recognition of ternary complexes: a new dimension in the structure-guided design of chemical degraders.

Hughes SJ, Ciulli A.

Essays Biochem. 2017 Nov 8;61(5):505-516. doi: 10.1042/EBC20170041. Print 2017 Nov 8. Review.

23.

Homo-PROTACs: bivalent small-molecule dimerizers of the VHL E3 ubiquitin ligase to induce self-degradation.

Maniaci C, Hughes SJ, Testa A, Chen W, Lamont DJ, Rocha S, Alessi DR, Romeo R, Ciulli A.

Nat Commun. 2017 Oct 10;8(1):830. doi: 10.1038/s41467-017-00954-1.

24.

Mind the Metal: A Fragment Library-Derived Zinc Impurity Binds the E2 Ubiquitin-Conjugating Enzyme Ube2T and Induces Structural Rearrangements.

Morreale FE, Testa A, Chaugule VK, Bortoluzzi A, Ciulli A, Walden H.

J Med Chem. 2017 Oct 12;60(19):8183-8191. doi: 10.1021/acs.jmedchem.7b01071. Epub 2017 Oct 3.

26.

Gram-Scale Laboratory Synthesis of TC AC 28, a High-Affinity BET Bromodomain Ligand.

Khan R, Marsh G, Felix R, Kemmitt PD, Baud MGJ, Ciulli A, Spencer J.

ACS Omega. 2017 Aug 8;2(8):4328-4332. doi: 10.1021/acsomega.7b00780. eCollection 2017 Aug 31.

27.
29.

Crystal Structure of the Cul2-Rbx1-EloBC-VHL Ubiquitin Ligase Complex.

Cardote TAF, Gadd MS, Ciulli A.

Structure. 2017 Jun 6;25(6):901-911.e3. doi: 10.1016/j.str.2017.04.009.

30.

Brd4-Brd2 isoform switching coordinates pluripotent exit and Smad2-dependent lineage specification.

Fernandez-Alonso R, Davidson L, Hukelmann J, Zengerle M, Prescott AR, Lamond A, Ciulli A, Sapkota GP, Findlay GM.

EMBO Rep. 2017 Jul;18(7):1108-1122. doi: 10.15252/embr.201643534. Epub 2017 Jun 6.

31.

Allosteric Targeting of the Fanconi Anemia Ubiquitin-Conjugating Enzyme Ube2T by Fragment Screening.

Morreale FE, Bortoluzzi A, Chaugule VK, Arkinson C, Walden H, Ciulli A.

J Med Chem. 2017 May 11;60(9):4093-4098. doi: 10.1021/acs.jmedchem.7b00147. Epub 2017 May 2.

32.

Investigation of the mycobacterial enzyme HsaD as a potential novel target for anti-tubercular agents using a fragment-based drug design approach.

Ryan A, Polycarpou E, Lack NA, Evangelopoulos D, Sieg C, Halman A, Bhakta S, Eleftheriadou O, McHugh TD, Keany S, Lowe ED, Ballet R, Abuhammad A, Jacobs WR Jr, Ciulli A, Sim E.

Br J Pharmacol. 2017 Jul;174(14):2209-2224. doi: 10.1111/bph.13810. Epub 2017 May 9.

33.

The biochemical properties of the two Arabidopsis thaliana isochorismate synthases.

Macaulay KM, Heath GA, Ciulli A, Murphy AM, Abell C, Carr JP, Smith AG.

Biochem J. 2017 Apr 28;474(10):1579-1590. doi: 10.1042/BCJ20161069.

34.

Structural basis of molecular recognition of helical histone H3 tail by PHD finger domains.

Bortoluzzi A, Amato A, Lucas X, Blank M, Ciulli A.

Biochem J. 2017 May 4;474(10):1633-1651. doi: 10.1042/BCJ20161053.

35.

Structural basis of PROTAC cooperative recognition for selective protein degradation.

Gadd MS, Testa A, Lucas X, Chan KH, Chen W, Lamont DJ, Zengerle M, Ciulli A.

Nat Chem Biol. 2017 May;13(5):514-521. doi: 10.1038/nchembio.2329. Epub 2017 Mar 13.

36.

Targeting Bacillosamine Biosynthesis in Bacterial Pathogens: Development of Inhibitors to a Bacterial Amino-Sugar Acetyltransferase from Campylobacter jejuni.

De Schutter JW, Morrison JP, Morrison MJ, Ciulli A, Imperiali B.

J Med Chem. 2017 Mar 9;60(5):2099-2118. doi: 10.1021/acs.jmedchem.6b01869. Epub 2017 Feb 22.

37.

Recognition of substrate degrons by E3 ubiquitin ligases and modulation by small-molecule mimicry strategies.

Lucas X, Ciulli A.

Curr Opin Struct Biol. 2017 Jun;44:101-110. doi: 10.1016/j.sbi.2016.12.015. Epub 2017 Jan 25. Review.

PMID:
28130986
38.

Potent and selective chemical probe of hypoxic signalling downstream of HIF-α hydroxylation via VHL inhibition.

Frost J, Galdeano C, Soares P, Gadd MS, Grzes KM, Ellis L, Epemolu O, Shimamura S, Bantscheff M, Grandi P, Read KD, Cantrell DA, Rocha S, Ciulli A.

Nat Commun. 2016 Nov 4;7:13312. doi: 10.1038/ncomms13312.

39.

Target validation: Switching domains.

Ciulli A.

Nat Chem Biol. 2016 Aug 18;12(9):659-60. doi: 10.1038/nchembio.2154. No abstract available.

PMID:
27538023
40.

Chemical genetics approaches for selective intervention in epigenetics.

Runcie AC, Chan KH, Zengerle M, Ciulli A.

Curr Opin Chem Biol. 2016 Aug;33:186-94. doi: 10.1016/j.cbpa.2016.06.031. Epub 2016 Jul 14. Review.

41.

Selectivity on-target of bromodomain chemical probes by structure-guided medicinal chemistry and chemical biology.

Galdeano C, Ciulli A.

Future Med Chem. 2016 Sep;8(13):1655-80. doi: 10.4155/fmc-2016-0059. Epub 2016 May 19. Review.

42.

Biophysical characterization of laforin-carbohydrate interaction.

Dias DM, Furtado J, Wasielewski E, Cruz R, Costello B, Cole L, Faria TQ, Baaske P, Brito RM, Ciulli A, Simões I, Macedo-Ribeiro S, Faro C, Geraldes CF, Castanheira P.

Biochem J. 2016 Feb 1;473(3):335-45. doi: 10.1042/BJ20141555. Epub 2015 Nov 17.

PMID:
26578817
43.

Cyclic and Macrocyclic Peptides as Chemical Tools To Recognise Protein Surfaces and Probe Protein-Protein Interactions.

Cardote TA, Ciulli A.

ChemMedChem. 2016 Apr 19;11(8):787-94. doi: 10.1002/cmdc.201500450. Epub 2015 Nov 13. Review.

44.

Optimization of Inhibitors of Mycobacterium tuberculosis Pantothenate Synthetase Based on Group Efficiency Analysis.

Hung AW, Silvestre HL, Wen S, George GP, Boland J, Blundell TL, Ciulli A, Abell C.

ChemMedChem. 2016 Jan 5;11(1):38-42. doi: 10.1002/cmdc.201500414. Epub 2015 Oct 21.

45.

New Synthetic Routes to Triazolo-benzodiazepine Analogues: Expanding the Scope of the Bump-and-Hole Approach for Selective Bromo and Extra-Terminal (BET) Bromodomain Inhibition.

Baud MG, Lin-Shiao E, Zengerle M, Tallant C, Ciulli A.

J Med Chem. 2016 Feb 25;59(4):1492-500. doi: 10.1021/acs.jmedchem.5b01135. Epub 2015 Oct 1.

47.

Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4.

Zengerle M, Chan KH, Ciulli A.

ACS Chem Biol. 2015 Aug 21;10(8):1770-7. doi: 10.1021/acschembio.5b00216. Epub 2015 Jun 16.

48.

Targeting Cullin-RING E3 ubiquitin ligases for drug discovery: structure, assembly and small-molecule modulation.

Bulatov E, Ciulli A.

Biochem J. 2015 May 1;467(3):365-86. doi: 10.1042/BJ20141450. Review.

49.

Molecular basis of histone tail recognition by human TIP5 PHD finger and bromodomain of the chromatin remodeling complex NoRC.

Tallant C, Valentini E, Fedorov O, Overvoorde L, Ferguson FM, Filippakopoulos P, Svergun DI, Knapp S, Ciulli A.

Structure. 2015 Jan 6;23(1):80-92. doi: 10.1016/j.str.2014.10.017. Epub 2014 Dec 18.

50.

Biophysical studies on interactions and assembly of full-size E3 ubiquitin ligase: suppressor of cytokine signaling 2 (SOCS2)-elongin BC-cullin 5-ring box protein 2 (RBX2).

Bulatov E, Martin EM, Chatterjee S, Knebel A, Shimamura S, Konijnenberg A, Johnson C, Zinn N, Grandi P, Sobott F, Ciulli A.

J Biol Chem. 2015 Feb 13;290(7):4178-91. doi: 10.1074/jbc.M114.616664. Epub 2014 Dec 11.

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