Our recent publications from 2022 to 2025
PubMed Link
Google Scholar Link
Previous Publications
* A.C. Corresponding Author
- Dylan E. Ramage, Lianne H.E. Wieske, Charlotte Crowe, Jens B. Christensen, Theo A. von Wilmowski, Drew W. Grant, Zoe Bannister, Mark A. Nakasone, Kevin Haubrich, Mark Dorward, Iva A. Tchasovnikarova, Michael P. Weekes, N. Sumru Bayin, Alessio Ciulli, Richard T. Timms. LRRC58 defines an E3 ubiquitin ligase complex sensitive to cysteine abundance. bioRxiv 2025.09.23.678073; doi: https://doi.org/10.1101/2025.09.23.678073
- Valentina A. Spiteri, Dmitri Segal, Alejandro Correa-Sáez, Kentaro Iso, Ryan Casement, Miquel Muñoz i Ordoño, Mark A. Nakasone, Gajanan Sathe, Caroline Schätz, Hannah E. Peters, Mark Doward, Lisa Kainacher, Angus D. Cowan, Alessio Ciulli*, Georg E. Winter.* Dual E3 ligase recruitment by monovalent degraders enables redundant and tuneable degradation of SMARCA2/4. bioRxiv 2025.08.04.668513; doi: https://doi.org/10.1101/2025.08.04.668513
- Vesna Vetma, Ilaria Puoti, Natalia Karolak, Sohini Chakraborti, Emelyne Diers, Enrico Girardi, Shakil Khan, Giorgia Kidd, Ross McLennan, Suzanne O’Connor, Nicole Trainor, Claire Whitworth, Andre Wijaya, Jeff Wong, David Zollman, William Farnaby, Johannes Popow, Alessio Ciulli*, Peter Ettmayer*, Kirsten McAulay*. Identification of a Highly Cooperative PROTAC Degrader Targeting GTP-loaded KRAS(on) Alleles. ChemRxiv. 2025; doi: 10.26434/chemrxiv-2025-706mw. This content is a preprint and has not been peer-reviewed.
- Maria Rodriguez-Rios, Conner Craigon, Mark A. Nakasone, Adam G. Bond, Mark Dorward, Anthony K. Edmonds, Mark C. Norley, Robert E. Arnold, Paul M. Wood, Stephen J. Reynolds, Joel O. Cresser-Brown, Graham P. Marsh, Hannah J. Maple, Alessio Ciulli*. BromoCatch: a self-labelling tag platform for protein analysis and live cell imaging. bioRxiv 2025.04.07.647551; doi: https://doi.org/10.1101/2025.04.07.647551
- Lan, H., Hsia, O., Nakasone, M., Wijaya, A., Ciulli, A.*, Butts, C.*, Aggarwal, V.* Computation, Synthesis and NMR Investigations of PROTAC Linker Conformation, Chamaleonicity and their Impacts on the Mode of Action. ChemRxiv. 2024; doi: 10.26434/chemrxiv-2024-5dbnb. This content is a preprint and has not been peer-reviewed.
- James B. Shaum, Erica A. Steen, Miquel Muñoz i Ordoño, Daniela V. Wenge, Hakyung Cheong, Moritz Hunkeler, Eric M. Bilotta, Zoe Rutter, Paige A. Barta, Natalia Milosevich, Lauren M. Hargis, Jordan Janowski, Timothy R. Bishop, Trever R. Carter, Bryce da Camara, Matthias Hinterndorfer, Lucas Dada, Wen-Ji He, Fabian Offensperger, Hirotake Furihata, Sydney R. Schweber, Charlie Hatton, Yanhe Wen, Benjamin F. Cravatt, Keary M. Engle, Bruno Melillo, Seiya Kitamura, Alessio Ciulli, Scott A. Armstrong, Eric S. Fischer, Georg E. Winter, Michael A. Erb. High-throughput diversification of protein-ligand surfaces to discover chemical inducers of proximity. bioRxiv 2024.09.30.615685; doi: https://doi.org/10.1101/2024.09.30.615685.
- Ponzo, I., Solda, A., Crowe, C., Dahl, G., Geschwindner, S.*, Ciulli, A.*, Rant, U.* Proximity Biosensor Assay for PROTAC Ternary Complex Analysis. ChemRxiv. 2024; doi: 10.26434/chemrxiv-2024-8w4zb. This content is a preprint and has not been peer-reviewed.
Refereed Papers In Primary Journals
* A.C. Corresponding Author
2025
155. Hughes, S.J., Stec, W.J., Davies, C.T.R., McGarry, D., Williams, A., Carrara, M., Del Barco Barrantes, I., Harris, R., Tasegian, A., Owens, D.D.G., Fawcett, A., Hellicar, J., Azevedo, A., Meier, G.P., Runcie, A.C., Greger, L., O’Rourke, M., Churcher, I., Pass, M., Brown, G.A., Ciulli, A., Modis, L.K., Testa, A.
Mode of action of a DCAF16-recruiting targeted glue that can selectively degrade BRD9.
Nat. Commun. 2025 Oct 27; 16(1):8516.
- PMID: 41145412.
- Pre-print first posted at BioRxiv on 31 December 2024; doi: 10.1101/2024.12.31.630899
154. Ma, N., Bhattacharya, S., Muk, S., Jandova, Z., Schmalhorst, P.S., Ghosh, S., Le, K., Diers, E., Trainor, N., Farnaby, W., Roy, M.J., Kofink, C., Greb, P., Weinstabl, H., Ciulli, A., Bader, G., Sankar, K., Bergner, A., Vaidehi, N.
Frustration in the protein-protein interface plays a central role in the cooperativity of PROTAC ternary complexes.
Nat. Commun. 2025 Sep 29; 16(1):8595.
- PMID: 41022846.
153. Dikic, I., Mayor-Ruiz, C., Winter, G.E., Koch, K., Ciulli, A.*, Thomä, N.H.
Opportunities in proximity modulation: Bridging academia and industry.
Mol. Cell. 2025 Aug 21; 85(16):3012-3022.
- PMID: 40845803.
152. Lloyd, H.C., Li, Y., Payne, N.C., Zhao, Z., Xu, W., Kroupova, A., Zollman, D., Long, T., Kabir, F., Chen, M., Freeman, R., Feng, E.Y., Xi, S.Y., Hsu, Y.C., Ciulli, A., Mazitschek, R., Woo, C.M.
A method for the detection and enrichment of endogenous cereblon substrates.
Cell Chem. Biol. 2025 Aug 21; 32(8):1028-1041.e13.
- PMID: 40782806.
- Pre-print first posted at BioRxiv on 26 March 2025; doi: 10.1101/2025.03.24.645063
151. Hinterndorfer, M., Spiteri, V.A., Ciulli, A.*, Winter, G.E.*
Targeted protein degradation for cancer therapy.
Nat. Rev. Cancer. 2025 Jul; 25(7):493-516.
- PMID: 40281114.
150. Vetma, V., O’Connor, S., Ciulli, A.*
Development of PROTAC degrader drugs for cancer
Annu. Rev. Cancer Biol. 2025 Apr; 9:119-140.
- Review in Advance, 30 Oct 2024
149. Salerno, A., Wieske, L.H.E., Diehl, C.J., Ciulli, A.*
Rational Design of PROTAC Linkers Featuring Ferrocene as a Molecular Hinge to Enable Dynamic Conformational Changes.
J Am Chem Soc. 2025 Apr 23;147(16):13328-13344.
- PMID: 40208910 PMCID: PMC12022980.
- Pre-print first posted at ChemRxiv on 21 December 2025; doi: 10.26434/chemrxiv-2024-1lm1h
148. Usart, M., Kimmerlin, Q., Stetka, J., Stoll, C., Rai, S., Almeida Fonseca, T., Karjalainen, R., Hao-Shen, H., Roux, J., El Taher, A., Lynch, D., Makukhin, N., Ciulli, A., Skoda, R.C.
Loss of Socs2 improves molecular responses to IFNα in a mouse model of myeloproliferative neoplasms driven by JAK2-V617F.
Leukemia. 2025 Apr;39(4):876-887.
- PMID: 40069287
147. Newton, L.S., Gathmann, C., Ridewood, S., Smith, R.J., Wijaya, A.J., Hornsby, T.W., Morling, K.L., Annett, D., Chiozzi, R.Z., Reuschl, A.K., Govasli, M.L., Tan, Y.Y., Thorne, L.G., Jolly, C., Thalassinos, K., Ciulli, A., Towers, G.J., Selwood, D.L.
Macrocycle-based PROTACs selectively degrade cyclophilin A and inhibit HIV-1 and HCV
Nat. Commun. 2025 Feb 10;16(1):1484.
- PMID: 39929804 PMCID: PMC11811207
- Pre-print first posted at Research Square on 15 March 2023; DOI: 10.21203/rs.3.rs-2639894/v1
146. McGown, A., Vetma, V., Crepin, D., Lin, Y., Adcock, C., Craigon, C., Nafie, J., von Emloh, D., Sutton, L., Bailey, K., Edmunds, L., Sharma, M., Wilden, J.D., Coles, S.J., Tizzard, G.J., Farnaby, W., Ciulli, A., Kostakis, G.E., Spencer, J.
Use of Aldehyde–Alkyne–Amine Couplings to Generate Medicinal Chemistry-Relevant Linkers
ACS Med. Chem. Lett. 2025 Jan 25;16(2):278-284.
- PMID: 39967623 PMCID: PMC11831382
145. Urbina, A., Hallatt, A.J., Robertson, J., Ciulli, A.*
A patent review of von Hippel-Lindau (vhl)-recruiting chemical matter: E3 ligase ligands for PROTACs and targeted protein degradation (2019-present)
Expert Opin. Ther. Pat. 2025 Feb 6:1-42.
- PMID: 39834300
- Listed as 1st Most Read Article in the journal (Feb 2025)
144. 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.
The efflux pump ABCC1/MRP1 constitutively restricts PROTAC sensitivity in cancer cells
Cell Chem. Biol. 2025 Feb 20;32(2):291-306.e6.
- PMID: 39755121
143. Alkhalaf, L.M., Arrowsmith, C., Balskus, E.P., Bergamini, G., Bhandari, R., Chang, C.J., Chen, P., Chen, X., Ciulli, A., Cricco, J.A., Davis, B.G., Delbianco, M., Dudareva, N., Dueber, E., Ferguson, F., de Giuseppe, P.O., Hamachi, I., Hammond, M.C., Hatzios, S.K., Do Heo, W., Janet, J.P., Kamat, S.S., Knapp, S., Krishnan, Y., Lang, K., Laraia, L., Leveson-Gower, R.B., Li, X.D., Liu, D.R., Liu, M.F., London, N., Mahanta, N., Mayor-Ruiz, C., Muir, T., Murakami, M.T., Rhee, H.W., Robers, M., Satz, A., Schulman, B.A., Shen, B., Shoichet, B., Strauss, E., Suzuki, T., Tiwary, P., Waldmann, H., Ward, T.R., Weeks, A., Weerapana, E., Winter, G.
Thoughts for the future
Nat. Chem. Biol. 2025 Jan;21(1):6-15.
- PMID: 39719500
2024
142. Lynch, D.M., Forrester, B., Webb, T., Ciulli, A.*
Unravelling the druggability and immunological roles of the SOCS-family proteins
Front. Immunol. 2024 Nov 29;15:1449397.
- PMID: 39676878 PMCID: PMC11638205
141. Tredup, C.; Ackloo, S.; Beck, H.; Brown, P.; Bullock, A.; Ciulli, A.; Dikic, I.; Edfeldt, K.; Edwards, A.; Elkins, J.; Farin, H.; Fon, E.A.; Gstaiger, M.; Günther, J.; Gustavsson, A.-L.; Häberle, S.; Isigkeit, L.; Huber, K.; Kotschy, A.; Krämer, O.; Leach, A.R. ; Marsden, B.; Matsui, H.; Merk, D.; Montel, F.; Mulder, M.; Müller, S.; Owen, D.; Proschak, E.; Röhm, S.; Stolz, A.; Sundström, M.; von Delft, F.; Willson, T.; Arrowsmith, C.H.; Knapp, S.
Toward Target 2035: EUbOPEN – a public-private partnership to enable & unlock biology in the open
RSC Med. Chem. 2024 Nov 29;16(2):457-464.
- PMID: 39618964 PMCID: PMC11605244
140. Bond, A. G.; Muñoz i Ordoño, M.; Bisbach, C. M.; Craigon, C.; Makukhin, N.; Caine, E. A.; Nagala, M.; Urh, M.; Winter, G. E.;* Riching, K. M.;* Ciulli, A.*
Leveraging Dual-Ligase Recruitment to Enhance Protein Degradation via a Heterotrivalent Proteolysis Targeting Chimera
J. Am. Chem. Soc. 2024 Dec 11;146(49):33675-33711.
- PMID: 39606859 PMCID: PMC11638965
- Pre-print first posted at ChemRxiv on 21 August 2024; DOI: 26434/chemrxiv-2024-lvvhf
139. Kroupova, A., Spiteri, V.A., Rutter, Z.J., Furihata, H., Darren, D., Ramachandran, S., Chakraborti, S., Haubrich, K., Pethe, J., Gonzales, D., Wijaya, A.J., Rodriguez-Rios, M., Sturbaut, M., Lynch, D.M., Farnaby, W., Nakasone, M.A., Zollman, D.*, Ciulli, A.*
Design of a Cereblon construct for crystallographic and biophysical studies of protein degraders
Nat Commun. 2024 Oct 15;15(1):8885.
- PMID: 39406745 PMCID: PMC11480361
- Pre-print first posted at BioRxiv on 17 January 2024; 2024.01.17.575503; doi: 1101/2024.01.17.575503
- Featured in the UoD Stories website
- His6-TEV-CRBN-midi (Plasmid #215330) is now available on Addgene.
- X-ray crystallography data generated in this study have been deposited in the Protein Data Bank (PDB) under accession codes: 8RQ1 (apo CRBNmidi), 8RQ8 (CRBNmidi:mezigdomide), 8RQ9 (CRBNmidi:CFT-1297:BRD4BD2), 8RQA (CRBNmidi:lenalidomide), 8RQC (CRBNmidi:mezigdomide:IKZF1ZF2), 9GAO (CRBNmidi:compound 1).
138. Crowe, C., Nakasone, M.A., Chandler, S., Craigon,C., Sathe, G., Tatham, M.H., Makukhin, N., Hay, R.T., Ciulli, A.*
Mechanism of degrader-targeted protein ubiquitinability
- PMID: 39392888 PMCID: PMC11468923
- Pre-print first posted at BioRxiv on 5 February 2024; 2024.02.05.578957; doi: 1101/2024.02.05.578957
- Featured in the UoD Stories website
- Covered in Ian Churcher’s blog
- Electron microscopy reconstructions have been deposited to the Electron Microscopy Databank (EMDB) under accession codes EMD-19569 and EMD-19567. Atomic models have been deposited to the PDB under IDs 8RWZ (Open non-crosslinked structure Brd4BD2-MZ1-(NEDD8)-CRL2VHL) and 8RX0 (Closed crosslinked structure of (NEDD8)-CRL2VHL-MZ1-Brd4BD2-Ub(G76S, K48C)-UBE2R1(C93K, S138C, C191S, C223S)-Ub).
137. Popow, J., Farnaby, W., Gollner, A., Kofink, C., Fischer, G., Wurm, M., Zollman, D., Wijaya, A., Mischerikow, N., Hasenoehrl, C., Prokofeva, P., Arnhof, H., Arce-Solano, S., Bell, S., Boeck, G., Diers, E., Frost, A.B., Goodwin-Tindall, J., Karolyi-Oezguer, J., Khan, S., Klawatsch, T., Koegl, M., Kousek, R., Kratochvil, B., Kropatsch, K., Lauber, A.A., McLennan, R., Olt, S., Peter, D., Petermann, O., Roessler, V., Stolt-Bergner, P., Strack, P., Strauss, E., Trainor, N., Vetma, V., Whitworth, C., Zhong, S., Quant, J., Weinstabl, H., Kuster, B., Ettmayer, P.*, Ciulli, A.*
Targeting cancer with small-molecule pan-KRAS degraders
Science 2024 Sep 20;385(6715):1338-1347.
- PMID: 39298590
- Pre-print first posted at BioRxiv on 26 October 2023; doi: 1101/2023.10.24.563163
- Covered in UoD Stories website
- Featured in the same issue of Science as Perspective “KRAS takes the road to destruction”
- Featured in Chemical & Engineering News
- Highlighted in Cancer Discovery Research Watch
- Highlighted in Nature Biotechnology
- X-ray crystallography data generated in this study have been deposited in the Protein Data Bank (PDB) under accession codes: 8QUG (KRAS-G12C in Complex with Compound 1), 8QW6 (compound 3 in complex with VCB (pVHL:ElonginC:ElonginB) and KRAS G12V C118S GDP), 8QW7 (compound 4 in complex with KRAS G12V C118S GDP and VCB), 8QVU (ACBI3 in complex with KRAS G12D C118S GDP and VCB).
- Cryo-EM density maps have been deposited in the Electron Microscopy Databank (EMDB) under accession code EMD-18657. The atomic model is deposited to the PDB under ID 8QU8 (PROTAC-mediated complex of KRAS with VHL/Elongin-B/Elongin-C/Cullin-2/Rbx1).
- Our pan-KRAS VHL-based PROTAC degrader ACBI3 (together with its negative control cis-ACBI3) are available from Boehringer Ingelheim’s OpnMe Portal: order for free, no strings attached!
136. Freemantle, J.B., Shah, D., Lynch, D.M., Ciulli, A., Hundal, H.S., Hardie, D.G.
The pro-drug C13 activates AMPK by two distinct mechanisms
Biochem. J. 2024, Sep 18;481(18):1203-1219.
- PMID: 39222030 PMCID: PMC11555695
135. Hatoyama, Y., Islam, M., Bond, A.G., Hayashi, K.-I., Ciulli, A., Kanemaki, M.T.
Combination of AID2 and BromoTag expands the utility of degron-based protein knockdowns
EMBO Rep., 2024 Sep;25(9):4062-4077.
- PMID: 39179892 PMCID: PMC11387839
- Pre-print first posted at BioRxiv on 22 March 2024; doi: 10.1101/2024.03.20.586026
134. Cavalli, A.,* Ciulli, A.*
Editorial overview: New concept in drug discovery
Curr. Opin. Struct. Biol. 2024, 88, 102911
- PMID: 39168047
133. Vetma, V., Casarez-Perez, L., Eliaš, J., Stingu, A., Kombara, A., Gmaschitz, T., Braun, N., Ciftci, T., Dahmann, G., Diers, E., Gerstberger, T., Greb, P., Kidd, G., Kofink, C., Puoti, I, Spiteri, V., Trainor, N., Westermaier, Y., Whitworth, C., Ciulli, A., Farnaby, W., McAulay, K., Frost, A.B., Chessum, N., Koegl, M.
Confounding Factors in Targeted Degradation of Short-Lived Proteins
ACS Chem. Biol. 2024 Jul 19;19(7):1484-1494.
- PMID: 38958654
- Pre-print first posted at BioRxiv on 22 February 2024; doi: 10.1101/2024.02.19.581012
- Listed as 2nd Most Read Article in the journal (1-month timeframe, Aug 2024)
- Highlighted in Derek Lowe’s blog In the Pipeline
132. Pierri, M., Liu, X., Kroupova, A., Rutter, Z., Hallatt, A.J., Ciulli, A.*
Stereochemical inversion at a 1,4-cyclohexyl PROTAC linker fine-tunes conformation and binding affinity
Bioorg. Med. Chem. Lett. 2024 Sep 15;110:129861.
- PMID: 38942127
- 2nd Most Downloaded Article in the journal (Dec 2024)
- X-ray crystallographic atomic coordinates and structure factors are available at the Protein Data Bank (PDB) under accession codes 9EQM (pVHL:ElonginC:ElonginB complex (VCB) in complex with compound MP-1-21) and 9EQJ (VCB in complex with compound MP-1-39).
131. Diehl, C. J., Salerno, A., Ciulli, A.*
Ternary Complex-Templated Dynamic Combinatorial Chemistry for the Selection and Identification of Homo-PROTACs.
Angew. Chem. Int. Ed. Engl. 2024 Jun 17;63(25):e202319456.
- PMID: 38626385
- Pre-print first posted at ChemRxiv on 16 December 2023; doi: 10.26434/chemrxiv-2023-tz70z
130. 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.,* Ciulli, A.*
Targeted protein degradation via intramolecular bivalent glues
Nature 2024 Mar;627(8002):204-211.
- PMID: 38383787 PMCID: PMC10917667
- Preprint first posted at BioRxiv on 14 February 2023 version 1: DOI: 10.1101/2023.02.14.528511v1
- Preprint version 2 DOI: 10.1101/2023.02.14.528511v2
- Covered in UoD News website
- Covered in CeMM News website
- Highlighted in Nature Reviews Drug Discovery
- Highlighted in Cancer Discovery Research Watch
- Highlighted in Nature Chemical Biology
- Cryo-EM density maps are deposited in the EMDB with the accession code EMD-17172. The atomic model is deposited under Protein Data Bank ID 8OV6 (Ternary structure of intramolecular bivalent glue degrader IBG1 bound to BRD4 and DCAF16:DDB1deltaBPB)
- Our dual Brd2/4 intramolecular bivalent glue degrader IBG3 is available from Tocris and MedChemExpress
2023
129. Ciulli, A.*, O’Connor, S.*, Chung, C.-W., Hartung, I. V., Testa, A., Daniels, D. L., Heitman, L. H.*
The 17th EFMC Short Course on Medicinal Chemistry on Small Molecule Protein Degraders
128. Ramachandran, S., Makukhin, N., Haubrich, K., Nagala, M., Forrester, B., Lynch, D.M., Casement, R., Testa, A., Bruno, E., Gitto, R., Ciulli, A. *
Structure-based design of a phosphotyrosine-masked covalent ligand targeting the E3 ligase SOCS2
- PMID: 37816714 PMCID: PMC10564737
- Preprint version 1 DOI: 10.26434/chemrxiv-2022-bvj80
- Preprint version 2 DOI: 10.26434/chemrxiv-2022-bvj80-v2
- See Figures here
- Covered in UoD Stories and SLS News websites
- Highlighted in Nature Chemical Biology; doi: 10.1038/s41589-024-01557-w
- X-ray crystallographic atomic coordinates and structure factors are available at the PDB under accession codes 7ZLP (compound 9 soaked to SOCS2:ElonginC:ElonginB complex (SBC2)), 7ZLN (compound 11 soaked to SBC2), 7ZLO (compound 12 soaked to SBC2), 7ZLR (compound 13 soaked to SBC2), 7ZLS (compound 13 co-crystallized in complex with SBC2), 7ZLM (compound MN551 co-crystallized in complex with SBC2)
- Our SOCS2 covalent inhibitor is available from MedChemExpress: unprotected MN551 for biophysical/structural studies or work ex-vivo / in cell lysates; and POM-protected cell-penetrant prodrug version MN714 for cellular studies
- MN714 / MN551 is qualified within EUbOpen as a Chemical Probe for SOCS2, more info in the ProbeSheet
127. 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.*, Gütschow, M*
Expanding the Structural Diversity at the Phenylene Core of Ligands for the von Hippel-Lindau (VHL) E3 Ubiquitin Ligase: Development of Highly Potent Hypoxia-Inducible Factor-1alpha (HIF-1alpha) Stabilizers
J. Med. Chem. 2023, 66 (18), 12776-12811
- PMID: 37708384 PMCID: PMC10544018
- Pre-print first posted at ChemRxiv on 07 March 2023; DOI: 10.26434/chemrxiv-2023-5gbb6
- Newer version 2 available from August 1st, 2023 at 10.26434/chemrxiv-2023-5gbb6-v2
- See Figures here
- The coordinates and structure factors of the associated co-crystal structure of the binary complexes between VHL and inhibitors 30, 33, and 37 are available in the PDB with accession codes 8CQK, 8CQL, and 8CQE, respectively.
(126. Ramachandran et al. book chapter)
125. Liu, X. Ciulli, A.*
Proximity-Based Modalities for Biology and Medicine
ACS Cent. Sci. 2023, 9 (7), 1269–1284
- PMID: 37521793 PMCID: PMC10375889
- See Figures here
- Listed as 1st Most Read Article in the journal (1-month timeframe, Aug 2023)
124. Haubrich, K., Spiteri, V.A., Farnaby, W., Sobott, F., Ciulli, A.*
Breaking free from the crystal lattice: Structural biology in solution to study protein degraders
Curr. Opin. Struct. Biol., 2023, 79, 102534
- PMID: 36804675
- Ranked amongst Most Downloaded Articles in the journal (August 2023)
123. Wijaya, A.J., Farnaby, W., Ciulli, A.*
Crystallization of VHL-based PROTAC-induced ternary complexes
Methods in Enzymology 2023, 681, 241–263
- PMID: 36764760
122. Hanzl, A., Casement, R., Imrichova, H., Hughes, S.J., Barone, E., Testa, A., Bauer, S., Wright, J., Brand, M., Ciulli, A.*, Winter, G.E.*
Functional E3 ligase hotspots and resistance mechanisms to small-molecule degraders
Nat. Chem. Biol. 2023, 19 (3), 323-333
- PMID: 36329119 PMCID: PMC7614256
- Pre-print posted at BioRxiv on 14 April 2022; DOI: https://doi.org/10.1101/2022.04.14.488316
- Covered in UoD News website
- Covered in CeMM News website
- Highlighted in Nature Reviews Drug Discovery
- Featured in a Spotlight article by Nico Thoma and colleagues in Trends in Pharmacological Sciences
- Atomic coordinates and structure factors for the ternary complex crystal structure VHL:AT7:Brd4-BD2 are available at the PDB under accession code 7ZNT.
(121. Hsia & Ciulli book chapter)
2022
120. Kofink, C., Trainor, N., Mair, B., Wöhrle, S., Wurm, M., Mischerikow, N., Roy, M., Bader, G., Greb, P., Garavel, G., Diers, E., McLennan, R., Whitworth, C., Vetma, V., Rumpel, K., Scharnweber, M., Fuchs, J.E., Gerstberger, T., Cui, Y., Gremel, G., Chetta, P., Hopf, S., Budano, N., Rinnenthal, J., Gmaschitz, G., Mayer, M., Koegl, M., Ciulli, A., Weinstabl, H., Farnaby, W.
A selective and orally bioavailable VHL-recruiting PROTAC achieves SMARCA2 degradation in vivo
- PMID: 36216795 PMCID: PMC9551036
- Pre-print posted at ChemRxiv on 1 February 2022; DOI: 10.26434/chemrxiv-2022-q63s3
- Covered in UoD and SLS News website
- Featured in a Comment article by John Harling and Chris Tinworth in Nature Communication
- X-ray co-crystal structures data have been deposited to the PDB under accession codes 7Z78 (compound 4 in complex with SMARCA2-BD), 7Z6L (VCB (pVHL:ElonginC:ElonginB complex): compound 5: SMARCA2-BD ternary complex), 7Z77 (VCB: compound 6: SMARCA2-BD ternary complex), and 7Z76 (VCB: compound 10: SMARCA2-BD ternary complex).
- Our SMARCA2 VHL-based PROTAC degrader ACBI2 (together with its negative control cis-ACBI2) are available from Boehringer Ingelheim’s OpnMe Portal: order for free, no strings attached!
- Find out more about ACBI2 in the Chemical Probes Portal
119. Cipriano, A., Milite, C., Feoli, A., Viviano, M., Pepe, G., Campiglia, P., Sarno, G., Picaud, S., Imaide, S., Makukhin, N., Filippakopoulos, P., Ciulli, A., Castellano, S., Sbardella, G.
Discovery of benzo[d]imidazole-6-sulfonamides as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the First Bromodomain
ChemMedChem 2022, 17 (20), e202200343
- PMID: 36040095 PMCID: PMC9826262
- See front cover here
118. Liu, X., Kalogeropulou, A., Domingos, S., Makukhin, N., Nirujogi, R., Singh, F., Shpiro, N., Saalfrank, A., Sammler, E., Ganley, I., Moreira, R., Alessi, D.*, Ciulli, A.*
Discovery of XL01126: A Potent, Fast, Cooperative, Selective, Oral bioavailable and Blood Brain Barrier Penetrant PROTAC Degrader of Leucine Rich Repeat Kinase 2 (LRRK2)
J. Am. Chem. Soc. 2022, 144 (37), 16930–16952
- PMID: 36007011 PMCID: PMC9501899
- Pre-print posted at ChemRxiv on 23 May 2022; DOI: 10.26434/chemrxiv-2022-4gzm0
- Covered in UoD and SLS Stories websites
- Listed as 3rd Most Read Article in the journal (1-month timeframe, Sept 2022)
- Listed as one of the Most Read Articles in the journal within the 12-month timeframe (July 2023)
- Our LRRK2 PROTAC degrader XL01126 is available from MedChemExpress
- Find out more about XL01126 in the Chemical Probes Portal
117. Diehl, C.J., Ciulli, A.*
Discovery of small molecule ligands for the von Hippel-Lindau (VHL) E3 ligase and their use as inhibitors and PROTAC degraders.
Chem. Soc. Rev. 2022, 51, 8216-8257
- PMID: 35983982 PMCID: PMC9528729
- See front cover here
116. Rasmussen, S.V.,Jin, J.X., Bickford, L.R., Woods, A.D., Sahm, F., Crawford, K.A., Nagamori, K., Goto, H., Torres, K.E., Sidoni, A., Rudzinski, E.R., Thway, K., Jones, R.L., Ciulli, A., Wright, H., Lathara, M., Srinivasa, G., Kannan, K., Huang, P.H., Grünewald, T.G.P., Berlow, N.E., Keller, C.
Functional genomic analysis of epithelioid sarcoma reveals distinct proximal and distal subtype biology
Clin. Transl. Med. 2022, 12 (7), e961
- PMID: 35839307 PMCID: PMC9286527
115. Gollner, A., Köster, M., Nicklin, P., Trieselmann, T., Klein, E., Vlach, J., Heine, C., Grundl, M., Ramharter, J., Wyatt, D., Chaturvedi, M., Ciulli, A., Carter, K.C., Müller, S., Bischoff, D., Ettmayer, P., Haaksma, E., Mack, J., McConnell, D., Stenkamp, D., Weinstabl, H., Zentgraf, M., Wood, C.R., Montel, F.
OpnMe.com: a digital initiative for sharing tools with the biomedical research community
Nat. Rev. Drug Discov. 2022, 21, 475-476
- PMID: 35459938
114. Grohmann, C., Magtoto, C.M., Walker, J.R., Chua, N.K., Gabrielyan, A., Hall, M., Cobbold, S.A., Mieruszynski, S., Brzozowski, M., Simpson, D.S., Dong, H., Dorizzi, B., Jacobsen, A.V., Morrish, E., Silke, N., Murphy, J.M., Heath, J.K., Testa, A., Maniaci, C., Ciulli, A., Lessene, G., Silke, J., Feltham, R.
Development of NanoLuc-targeting protein degraders and a universal reporter system to benchmark tag-targeted degradation platforms
- PMID: 35440107 PMCID: PMC9019100
113. Cowan, A.D., Ciulli, A.*
Driving E3 Ligase Substrate Specificity for Targeted Protein Degradation: Lessons from Nature and the Laboratory
Annu. Rev. Biochem., 2022, 91, 295-319
112. Webb, T., Craigon, C., Ciulli, A.*
Targeting Epigenetic Modulators Using PROTAC Degraders: Current Status and Future Perspective
Bioorg. Med. Chem. Lett. 2022, 63, 128653
- PMID: 35257896
- See Figures here
- Read the article open access before April 29, 2022 via the personalized Share Link
- Listed amongst the top Most Downloaded Articles in the Journal of the last 90 days (Sept 2022)
111. Liu, X., Ciulli, A.*
Targeted protein stabilization: DUB be good to me
Nat. Chem. Biol. 2022, 18 (4), 358-359
- PMID: 37039823
- News & Views article on Henning et al. Nat. Chem. Biol. 2022
- Read the article Open Access as SharedIt version here
- See Figure and links here
110. Bharathy, N., Cleary, M.M., Kim, J-A., Nagamori, K., Crawford, K.A., Wang, E., Saha, D., Settelmeyer, T.P., Purohit, R., Skopelitis, D., Chang, K., Doran, J.A., Kirschbaum, C.W., Bharathy, S., Crews, D.W., Randolph, M.E., Karnezis, A.N., Hudson-Price, L., Dhawan, J., Michalek, J.E., Ciulli, A.,* Vakoc, C.R. & Keller, C.*
SMARCA4 biology in alveolar rhabdomyosarcoma