EUbOPEN: Enabling and Unlocking biology in the OPEN (Joint with Goethe University Frankfurt, University of Oxford, Karolinska Institute and 9 others)

2025

A patent review of von Hippel-Lindau (VHL)-recruiting chemical matter: E3 Ligase Ligands for PROTACs and targeted protein degradation (2019-present)

Urbina Teixidor, A., Hallatt, A., Robertson, J. & Ciulli, A. (Lead / Corresponding author), 2025, In: Expert Opinion on Therapeutic Patents. 35, 3, p. 197-238 42 p.

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Rational Design of PROTAC Linkers Featuring Ferrocene as a Molecular Hinge to Enable Dynamic Conformational Changes

Salerno, A., Wieske, L. H. E., Diehl, C. J. & Ciulli, A. (Lead / Corresponding author), 23 Apr 2025, In: Journal of the American Chemical Society. 147, 16, p. 13328-13344 17 p.

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The efflux pump ABCC1/MRP1 constitutively restricts PROTAC sensitivity in cancer cells

Wolf, G., Craigon, C., Teoh, S. T., Essletzbichler, P., Onstein, S., Cassidy, D., Uijttewaal, E. C. H., Dvorak, V., Cao, Y., Bensimon, A., Elling, U., Ciulli, A. & Superti-Furga, G. (Lead / Corresponding author), 20 Feb 2025, In: Cell Chemical Biology. 32, 2, p. 291-306.e6 23 p.

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3 Citations (Scopus)

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2024

Design of a Cereblon construct for crystallographic and biophysical studies of protein degraders

Kroupova, A., Spiteri, V., Rutter, Z., Furihata, H., Darren, D., Ramachandran, S., Chakraborti, S., Haubrich, K., Pethe, J., Gonzales, D., Wijaya, A., Rodriguez-Rios, M., Sturbaut, M., Lynch, D., Farnaby, W., Nakasone, M., Zollman, D. (Lead / Corresponding author) & Ciulli, A. (Lead / Corresponding author), 15 Oct 2024, In: Nature Communications. 15, 14 p., 8885.

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3 Citations (Scopus)

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Imidazo[1,2-b]pyridazines as inhibitors of DYRK kinases

Henderson, S. H., Sorrell, F. J., Bennett, J. M., Fedorov, O., Hanley, M. T., Godoi, P. H., Ruela de Sousa, R., Robinson, S., Navratilova, I. H., Elkins, J. M. (Lead / Corresponding author) & Ward, S. E. (Lead / Corresponding author), 5 Apr 2024, In: European Journal of Medicinal Chemistry. 269, 14 p., 116292.

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2 Citations (Scopus)

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Leveraging Dual-Ligase Recruitment to Enhance Protein Degradation via a Heterotrivalent Proteolysis Targeting Chimera

Bond, A. G., Muñoz i Ordoño, M., Bisbach, C. M., Craigon, C., Makukhin, N., Caine, E. A., Nagala, M., Urh, M., Winter, G. E. (Lead / Corresponding author), Riching, K. M. (Lead / Corresponding author) & Ciulli, A. (Lead / Corresponding author), 28 Nov 2024, In: Journal of the American Chemical Society. 146, 49, p. 33675−33711 37 p.

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4 Citations (Scopus)

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Mechanism of degrader-targeted protein ubiquitinability

Crowe, C., Nakasone, M., Chandler, S., Craigon, C., Sathe, G., Tatham, M., Makukhin, N., Hay, R. & Ciulli, A. (Lead / Corresponding author), 11 Oct 2024, In: Science Advances. 10, 41, 21 p., eado6492.

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10 Citations (Scopus)

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Stereochemical inversion at a 1,4-cyclohexyl PROTAC linker fine-tunes conformation and binding affinity

Pierri, M., Liu, X., Kroupova, A., Rutter, Z., Hallatt, A. J. & Ciulli, A. (Lead / Corresponding author), 15 Sept 2024, In: Bioorganic & Medicinal Chemistry Letters. 110, 6 p., 129861.

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3 Citations (Scopus)

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Targeted protein degradation via intramolecular bivalent glues

Hsia, O., Hinterndorfer, M., Cowan, A. D., Iso, K., Ishida, T., Sundaramoorthy, R., Nakasone, M. A., Imrichova, H., Schätz, C., Rukavina, A., Husnjak, K., Wegner, M., Correa-Sáez, A., Craigon, C., Casement, R., Maniaci, C., Testa, A., Kaulich, M., Dikic, I. & Winter, G. E. (Lead / Corresponding author) & 1 others, Ciulli, A. (Lead / Corresponding author), 7 Mar 2024, In: Nature. 627, 8002, p. 204-211 8 p.

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71 Citations (Scopus)

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Ternary Complex-Templated Dynamic Combinatorial Chemistry for the Selection and Identification of Homo-PROTACs

Diehl, C. J., Salerno, A. & Ciulli, A. (Lead / Corresponding author), 17 Jun 2024, In: Angewandte Chemie International Edition. 63, 25, 9 p., e202319456.

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4 Citations (Scopus)

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The pro-drug C13 activates AMPK by two distinct mechanisms

Freemantle, J. B., Shah, D., Lynch, D. M., Ciulli, A., Hundal, H. S. & Hardie, D. G. (Lead / Corresponding author), Sept 2024, In: The Biochemical journal. 481, 18, p. 1203-1219 17 p.

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2 Citations (Scopus)

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2023

Expanding the Structural Diversity at the Phenylene Core of Ligands for the von Hippel-Lindau E3 Ubiquitin Ligase: Development of Highly Potent Hypoxia-Inducible Factor-1α Stabilizers

Vu, L. P., Diehl, C. J., Casement, R., Bond, A. G., Steinebach, C., Strašek, N., Bricelj, A., Perdih, A., Schnakenburg, G., Sosič, I., Ciulli, A. (Lead / Corresponding author) & Gütschow, M. (Lead / Corresponding author), 28 Sept 2023, In: Journal of Medicinal Chemistry. 66, 18, p. 12776-12811 36 p.

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8 Citations (Scopus)

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Proximity-Based Modalities for Biology and Medicine

Liu, X. & Ciulli, A. (Lead / Corresponding author), 26 Jul 2023, In: ACS Central Science. 9, 7, p. 1269-1284 16 p.

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80 Citations (Scopus)

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Structure-based design of a phosphotyrosine-masked covalent ligand targeting the E3 ligase SOCS2

Ramachandran, S., Makukhin, N., Haubrich, K., Nagala, M., Forrester, B., Lynch, D. M., Casement, R., Testa, A., Bruno, E., Gitto, R. & Ciulli, A. (Lead / Corresponding author), 10 Oct 2023, In: Nature Communications. 14, 17 p., 6345.

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19 Citations (Scopus)

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2022

Discovery of XL01126: A Potent, Fast, Cooperative, Selective, Orally Bioavailable, and Blood-Brain Barrier Penetrant PROTAC Degrader of Leucine-Rich Repeat Kinase 2

Liu, X., Kalogeropulou, A. F., Domingos, S., Makukhin, N., Nirujogi, R., Singh, F., Shpiro, N., Saalfrank, A., Sammler, E., Ganley, I. G., Moreira, R., Alessi, D. R. (Lead / Corresponding author) & Ciulli, A. (Lead / Corresponding author), 21 Sept 2022, In: Journal of the American Chemical Society. 144, 37, p. 16930-16952 23 p.

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104 Citations (Scopus)

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Sequence and structural variations determining the recruitment of WNK kinases to the KLHL3 E3 ligase

Chen, Z., Zhang, J., Murillo-de-Ozores, A. R., Castañeda-Bueno, M., D'Amico, F., Heilig, R., Manning, C., Sorrell, F. J., D'Angiolella, V., Fischer, R., Mulder, M., Gamba, G., Alessi, D. R. & Bullock, A. N. (Lead / Corresponding author), 4 Mar 2022, In: Biochemical Journal. 479, 5, p. 661-675 15 p.

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4 Citations (Scopus)

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Target 2035-update on the quest for a probe for every protein

Mueller, S. (Lead / Corresponding author), Ackloo, S., Al Chawaf, A., Al-Lazikani, B., Antolin, A., Baell, J. B., Beck, H., Beedie, S., Betz, U. A. K., Bezerra, G. A., Brennan, P. E., Brown, D., Brown, P. J., Bullock, A. N., Carter, A. J., Chaikuad, A., Chaineau, M., Ciulli, A., Collins, I. & Dreher, J. & 43 others, Drewry, D., Edfeldt, K., Edwards, A. M., Egner, U., Frye, S. V., Fuchs, S. M., Hall, M. D., Hartung, I. V., Hillisch, A., Hitchcock, S. H., Homan, E., Kannan, N., Kiefer, J. R., Knapp, S., Kostic, M., Kubicek, S., Leach, A. R., Lindemann, S., Marsden, B. D., Matsui, H., Meier, J. L., Merk, D., Michel, M., Morgan, M. R., Mueller-Fahrnow, A., Owen, D. R., Perry, B. G., Rosenberg, S. H., Saikatendu, K. S., Schapira, M., Scholten, C., Sharma, S., Simeonov, A., Sundstrom, M., Superti-Furga, G., Todd, M. H., Tredup, C., Vedadi, M., von Delft, F., Willson, T. M., Winter, G. E., Workman, P. & Arrowsmith, C. H. (Lead / Corresponding author), 27 Jan 2022, In: RSC Medicinal Chemistry. 13, 1, p. 13-21 9 p.

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58 Citations (Scopus)

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2021

Amide-to-ester substitution as a strategy for optimizing PROTAC permeability and cellular activity

Klein, V. G., Bond, A. G., Craigon, C., Lokey, R. S. (Lead / Corresponding author) & Ciulli, A. (Lead / Corresponding author), 23 Dec 2021, In: Journal of Medicinal Chemistry. 64, 24, p. 18082-18101 20 p.

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89 Citations (Scopus)

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Automated Determination of Nuclear Magnetic Resonance Chemical Shift Perturbations in Ligand Screening Experiments: The PICASSO Web Server

Laveglia, V., Giachetti, A., Cerofolini, L., Haubrich, K., Fragai, M., Ciulli, A. & Rosato, A. (Lead / Corresponding author), 27 Dec 2021, In: Journal of Chemical Information and Modeling. 61, 12, p. 5726-5733 8 p.

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5 Citations (Scopus)

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Development of BromoTag: A “Bump-&-Hole”-PROTAC system to induce potent, rapid, and selective degradation of tagged target proteins

Bond, A. G., Craigon, C., Chan, K. H., Testa, A., Karapetsas, A., Fasimoye, R., Macartney, T., Blow, J. J., Alessi, D. R. & Ciulli, A. (Lead / Corresponding author), 28 Oct 2021, In: Journal of Medicinal Chemistry. 64, 20, p. 15477-15502 26 p.

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57 Citations (Scopus)

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E3 Ligase Ligands for PROTACs: How They Were Found and How to Discover New Ones

Ishida, T. & Ciulli, A. (Lead / Corresponding author), 1 Apr 2021, In: SLAS Discovery. 26, 4, p. 484-502 19 p.

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224 Citations (Scopus)

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EUbOPEN: Enabling and Unlocking biology in the OPEN (Joint with Goethe University Frankfurt, University of Oxford, Karolinska Institute and 9 others)

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