{"id":27,"date":"2023-11-03T19:02:18","date_gmt":"2023-11-03T19:02:18","guid":{"rendered":"https:\/\/sites.dundee.ac.uk\/farnaby-group\/?page_id=27"},"modified":"2025-11-05T13:06:42","modified_gmt":"2025-11-05T13:06:42","slug":"publications","status":"publish","type":"page","link":"https:\/\/sites.dundee.ac.uk\/farnaby-group\/publications\/","title":{"rendered":"Publications"},"content":{"rendered":"\n
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23. Identification of a Highly Cooperative PROTAC Degrader Targeting GTP-Loaded KRAS(On) Alleles<\/strong><\/p>\n\n\n\n


Vesna Vetma, Ilaria Puoti, Natalia K. Karolak, Sohini Chakraborti, Emelyne Diers, Enrico Girardi, Shakil Khan, Giorgia Kidd, Katrin G. Kropatsch, Ross Mclennan, Suzanne O\u2019Connor, Matthias Samwer, Nicole Trainor, Claire Whitworth, Andre J. Wijaya, Jeff Y. F. Wong, David Zollman, William Farnaby, Johannes Popow, Alessio Ciulli*<\/strong>, Peter Ettmayer*<\/strong>, Kirsten McAulay*<\/strong><\/p>\n\n\n\n

J. Am. Chem. Soc.<\/em>\u00a0(2025)<\/p>\n\n\n\n

doi: 10.1021\/jacs.5c10354<\/a><\/p>\n<\/div>

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22. Frustration in the protein-protein interface plays a central role in the cooperativity of PROTAC ternary complexes<\/strong> <\/p>\n\n\n\n


Ning Ma, Supriyo Bhattacharya, Sanychen Muk, Zuzana Jandova, Philipp S. Schmalhorst, Soumadwip Ghosh, Keith Le, Emelyne Diers, Nicole Trainor, William Farnaby, Michael J. Roy, Christiane Kofink, Peter Greb, Harald Weinstabl, Alessio Ciulli, Gerd Bader, Kyra Sankar, Andreas Bergner & Nagarajan Vaidehi<\/p>\n\n\n\n

Nat Commun<\/em> 16<\/strong>, 8595 (2025)<\/p>\n\n\n\n

doi: 10.1038\/s41467-025-63713-7<\/a><\/p>\n<\/div>

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21. Stick it with VHL<\/strong><\/p>\n\n\n\n

William Farnaby<\/p>\n\n\n\n

Nature Chemical Biology News and Views<\/em>. <\/p>\n\n\n\n

Publication date: 24th June 2025<\/p>\n\n\n\n

doi: 10.1038\/s41589-025-01897-1<\/a><\/p>\n<\/div>

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20. Discovery of a CNS active GSK3 degrader using orthogonally reactive linker screening<\/strong><\/p>\n\n\n\n

Andreas Holmqvist*, Nur Mehpare Kocaturk*, Christina Duncan, Jennifer Riley, Steve Baginski, Graham Marsh, Joel Cressor-Brown, Hannah Maple, Kristiina Juvonen, Gajanan Sathe, Nicola Morrice, Calum Sutherland, Kevin Read, William Farnaby (corresponding author)<\/p>\n\n\n\n

Nat Commun<\/em>\u00a016<\/strong>, 8857 (2025)<\/p>\n\n\n\n

doi: 10.1038\/s41467-025-63928-8<\/a><\/p>\n\n\n\n

Pre-print first posted at ChemRxiv<\/em> on 10th March 2025; doi:: 10.26434\/chemrxiv-2025-nq14w<\/a><\/p>\n\n\n\n


*contributed equally as first author<\/p>\n<\/div>

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19. Use of Aldehyde\u2013Alkyne\u2013Amine Couplings to Generate Medicinal Chemistry-Relevant Linkers<\/strong><\/p>\n\n\n\n

Andrew McGown*<\/strong>, Vesna Vetma, Damien Crepin, Yan Lin, Claire Adcock, Conner Craigon, Jordan Nafie, Daniel von Emloh, L\u00e9a Sutton, Kiera Bailey, Lewis Edmunds, Manvendra Sharma, Jonathan D. Wilden, Simon J. Coles, Graham J. Tizzard, William Farnaby, Alessio Ciulli, George E. Kostakis, John Spencer*<\/strong><\/p>\n\n\n\n

ACS Med. Chem. Lett.<\/em> Publication date : January 25th, 2025<\/strong> <\/p>\n\n\n\n

doi: 10.1021\/acsmedchemlett.4c00531<\/a><\/p>\n\n\n\n


*co-corresponding authors<\/p>\n<\/div>

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18. Targeting cancer with small molecule pan-KRAS degraders<\/strong><\/p>\n\n\n\n

Johannes Popow*, William Farnaby*, Andreas Gollner*, Christiane Kofink*, Gerhard Fischer, Melanie Wurm, David Zollman, Andre Wijaya, Nikolai Mischerikow, Carina Hasenoehrl, Polina Prokofeva, Heribert Arnhof, Silvia Arce-Solano, Sammy Bell, Georg Boeck, Emelyne Diers, Aileen B Frost, Jake Goodwin-Tindall, Jale Karolyi-Oezguer, Shakil Khan, Theresa Klawatsch, Manfred Koegl, Roland Kousek, Barbara Kratochvil, Katrin Kropatsch, Arnel A Lauber, Ross McLennan, Sabine Olt, Daniel Peter, Oliver Petermann, Vanessa Roessler, Peggy Stolt-Bergner, Patrick Strack, Eva Strauss, Nicole Trainor, Vesna Vetma, Claire Whitworth, Siying Zhong, Jens Quant, Harald Weinstabl, Bernhard K\u00fcster, Peter Ettmayer (lead\/corresponding author), Alessio Ciulli (lead\/corresponding author)<\/p>\n\n\n\n

*contributed equally as first author<\/p>\n\n\n\n

Science. <\/em>Publication Date: September 19, 2024,<\/strong> doi: 10.1126\/science.adm8684<\/a><\/p>\n\n\n\n

Pre-print first posted at bioRxiv<\/em> on 26th October 2023; doi: 10.1101\/2023.10.24.563163<\/a><\/p>\n<\/div>

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17. Confounding factors in targeted degradation of short-lived proteins<\/strong><\/p>\n\n\n\n

Vesna Vetma, Laura Casares-Perez, J\u00e1n Elia\u0161, Andrea Stingu, Anju Kombara, Teresa Gmaschitz, Nina Braun, Tuncay Ciftci, Georg Dahmann, Emelyne Diers, Thomas Gerstberger, Peter Greb, Giorgia Kidd, Christiane Kofink, Ilaria Puoti, Valentina Spiteri, Nicole Trainor, Yvonne Westermaier, Claire Whitworth, Alessio Ciulli, William Farnaby, Kirsten McAulauy, Aileen B. Frost, Nicola Chessum, Manfred Koegl<\/p>\n\n\n\n

ACS Chem. Biol<\/em>. Publication Date: July 3, 2024<\/strong>, doi: 10.1021\/acschembio.4c00152<\/a><\/p>\n\n\n\n

Pre-print first posted at BioRxiv<\/em> on 22 February 2024<\/strong>; doi: 10.1101\/2024.02.19.581012<\/a><\/p>\n<\/div>

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16. Design of a Cereblon construct for crystallographic and biophysical studies of protein degraders<\/strong><\/p>\n\n\n\n

Alena Kroupova, Valentina A. Spiteri, Hirotake Furihata, Darren Darren, Sarath Ramachandran, Zoe J. Rutter, Sohini Chakraborti, Kevin Haubrich, Julie Pethe, Denzel Gonzales, Andre Wijaya, Maria Rodriguez-Rios, Dylan M. Lynch, William Farnaby, Mark A. Nakasone, *David Zollman, *Alessio Ciulli<\/p>\n\n\n\n

*co-corresponding authors<\/p>\n\n\n\n

Nat Commun<\/em>. <\/strong>Publication date 15th October 2024<\/strong>; <\/p>\n\n\n\n

doi: 10.1038\/s41467-024-52871-9<\/a><\/p>\n\n\n\n

Pre-print first posted at BioRxiv<\/em> on 20 January 2024<\/strong> <\/p>\n\n\n\n

doi: 10.1101\/2024.01.17.575503<\/a><\/p>\n<\/div>

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15. Breaking free from the crystal lattice: Structural biology in solution to study protein degraders.<\/strong><\/p>\n\n\n\n

Kevin Haubrich, Valentina Spiteri, William Farnaby<\/strong>, Frank Sobott, Alessio Ciulli<\/p>\n\n\n\n

Curr Opin Struct Biol <\/em>2023, <\/strong>79, 10234.<\/p>\n\n\n\n

doi: 10.1016\/j.sbi.2023.102534<\/a><\/p>\n<\/div>

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14. Crystallization of VHL-based PROTAC-induced ternary complexe<\/strong>s<\/p>\n\n\n\n

Andre J. Wijaya, William Farnaby<\/strong>, Alessio Ciulli<\/p>\n\n\n\n

Methods Enzymol<\/em> 2023<\/strong>, <\/em>681, 242-261.<\/p>\n\n\n\n

doi: 10.1016\/bs.mie.2022.10.005<\/a><\/p>\n<\/div>

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13. A selective and orally bioavailable VHL-recruiting PROTAC achieves SMARCA2 degradation in vivo<\/strong><\/p>\n

Christiane Kofink,\u00a0Nicole Trainor,\u00a0Barbara Mair,\u00a0Simon W\u00f6hrle,\u00a0Melanie Wurm,\u00a0Nikolai Mischerikow,\u00a0Michael J. Roy,\u00a0Gerd Bader,\u00a0Peter Greb,\u00a0G\u00e9raldine Garavel,\u00a0Emelyne Diers,\u00a0Ross McLennan,\u00a0Claire Whitworth,\u00a0Vesna Vetma,\u00a0Klaus Rumpel,\u00a0Maximilian Scharnweber,\u00a0Julian E. Fuchs,\u00a0Thomas Gerstberger,\u00a0Yunhai Cui,\u00a0Gabriela Gremel,\u00a0Paolo Chetta,\u00a0Stefan Hopf,\u00a0Nicole Budano,\u00a0Joerg Rinnenthal,\u00a0Gerhard Gmaschitz,\u00a0Moriz Mayer,\u00a0Manfred Koegl,\u00a0Alessio Ciulli,\u00a0Harald Weinstabl\u00a0&\u00a0William Farnaby<\/p>\n\n\n\n

Nat. Commun. <\/em>2022<\/strong>, 13 (1), 5969. <\/p>\n\n\n\n

doi: 10.1038\/s41467-022-33430-6<\/a><\/p>\n<\/div>

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12. Discovery of Soticlestat, a Potent and Selective Inhibitor for Cholesterol 24-Hydroxylase (CH24H)<\/strong><\/p>\n\n\n\n

Tatsuki Koike, Masato Yoshikawa, Haruhi Kamisaki Ando, William Farnaby<\/strong>, Toshiya Nishi, Etsorou Watanabe, Jason Yano, Maki Miyamoto, Shigeru Kondo, Tsuyoshi Ishi, Takanobu Kuroita<\/p>\n\n\n\n

J Med Chem <\/em>2021 <\/strong>64(16):12228-12244. <\/p>\n\n\n\n

doi: 10.1021\/acs.jmedchem.1c00864<\/a><\/p>\n<\/div>

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11. Transforming targeted cancer therapy with PROTACs: A forward-looking perspective<\/strong><\/p>\n\n\n\n

William Farnaby<\/strong>, Manfred Koegl, Darryl B. McConnell, Alessio Ciulli<\/p>\n\n\n\n

Curr. Opin. Pharmacol.<\/em> 2021<\/strong>, 57<\/em>, 175-183<\/p>\n\n\n\n

doi: 10.1016\/j.coph.2021.02.009<\/a><\/p>\n<\/div>

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10. Soticlestat, a novel cholesterol 24-hydroxylase inhibitor shows a therapeutic potential for neural hyperexcitation in mice<\/strong><\/p>\n\n\n\n

Toshiya Nishi, Shinichi Kondo, Maki Miyamoto, Sayuri Watanabe, Shigeo Hasegawa, Shigeru Kondo, Jason Yano, Etsurou Watanabe, Tsuyoshi Ishi, Masato Yoshikawa, Haruhi Kamisaki Ando, William Farnaby<\/strong>, Shinji Fujimoto, Eiji Sunahara, Momoko Ohori, Matthew J. During, Takanobu Kuroita & Tatsuki Koike<\/p>\n\n\n\n

Scientific Reports<\/em> 2020<\/strong>, <\/strong>10, 17081<\/p>\n\n\n\n

doi: 10.1038\/s41598-020-74036-6<\/a><\/p>\n<\/div>

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9. Protein degradation for drug discovery. <\/strong>[Editorial]<\/p>\n\n\n\n

Alessio Ciulli & William Farnaby<\/strong><\/p>\n\n\n\n

Drug Discov. Today Technol.<\/em> 2019<\/strong> Apr 31: 1-3<\/p>\n\n\n\n

doi: 10.1016\/j.ddtec.2019.04.002<\/a><\/p>\n<\/div>

<\/figure><\/div>\n\n\n\n
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8. BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design<\/strong><\/p>\n\n\n\n

William Farnaby<\/strong>*, Manfred Koegl*, Michael J. Roy, Claire Whitworth, Emelyne Diers, Nicole Trainor, David Zollman, Steffen Steurer, Jale Karolyi-Oezguer, Carina Riedmueller, Teresa Gmaschitz, Johannes Wachter, Christian Dank, Michael Galant, Bernadette Sharps, Klaus Rumpel, Elisabeth Traxler, Thomas Gerstberger, Renate Schnitzer, Oliver Petermann, Peter Greb, Harald Weinstabl, Gerd Bader, Andreas Zoephel, Alexander Weiss-Puxbaum, Katharina Ehrenh\u00f6fer-W\u00f6lfer, Simon W\u00f6hrle, Guido Boehmelt, Joerg Rinnenthal, Heribert Arnhof, Nicola Wiechens, Meng-Ying Wu, Tom Owen-Hughes, Peter Ettmayer, Mark Pearson, Darryl B. McConnell & Alessio Ciulli<\/p>\n\n\n\n

*contributed equally<\/p>\n\n\n\n

Nat Chem Biol <\/em>2019,<\/strong> 15 (7), 672\u2013680. <\/p>\n\n\n\n

doi: 10.1038\/s41589-019-0294-6<\/a><\/p>\n<\/div>

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7. SPR-measured dissociation kinetics of PROTAC ternary complexes influence target degradation rate<\/strong><\/p>\n\n\n\n

Michael J. Roy, Sandra Winkler, Scott J. Hughes, Claire Whitworth, Michael Galant, William Farnaby<\/strong>, Klaus Rumpel, Alessio Ciulli<\/p>\n<\/div>

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6. Identification of compounds acting as negative allosteric modulators of the LPA1<\/sub> receptor<\/strong><\/p>\n\n\n\n

Jonathan Ellery, Louise Dickson, Toni Cheung, Loredana Ciuclan, Peter Bunyard, Stephen Mack, William J Buffham, William Farnaby<\/strong>, Philip Mitchell, Daniel Brown, Richard Isaacs, Matt Barnes<\/p>\n\n\n\n

Eur J Pharmacol<\/em> 2018<\/strong> 833, 8-15. <\/p>\n\n\n\n

doi: 10.1016\/j.ejphar.2018.05.040<\/a><\/p>\n<\/div>

<\/figure><\/div>\n\n\n\n
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5. Modular synthesis of thirty lead-like scaffolds suitable for CNS drug discovery<\/strong><\/p>\n\n\n\n

Joan Mayol-Llinas, William Farnaby<\/strong>, Adam Nelson<\/p>\n\n\n\n

Chem. Commun.<\/em> 2017<\/strong>, 53, 12345-12348<\/p>\n\n\n\n

doi: 10.1039\/C7CC06078E<\/a><\/p>\n<\/div>

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4. Assessment of the Target Engagement and D-Serine Biomarker Profiles of the D-Amino Acid Oxidase Inhibitors Sodium Benzoate and PGM030756<\/strong><\/p>\n\n\n\n

Eimear Howley, Michael Bestwick, Rosa Fradley, Helen Harrison, Mathew Leveridge, Kengo Okada, Charlotte Fieldhouse, Will Farnaby<\/strong>, Hannah Canning, Andy P Sykes, Kevin Merchant, Katherine Hazel, Catrina Kerr, Natasha Kinsella, Louise Walsh, David G Livermore, Isaac Hoffman, Jonathan Ellery, Phillip Mitchell, Toshal Patel, Mark Carlton, Matt Barnes, David J Miller<\/p>\n\n\n\n

Neurochem Res<\/em> 2017<\/strong>, 42, 3279-3288. <\/p>\n\n\n\n

doi: 10.1007\/s11064-017-2367-9<\/a><\/p>\n<\/div>

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3. Assessing molecular scaffolds for CNS drug discovery<\/strong><\/p>\n\n\n\n

Joan Mayol-Llinas, Adam Nelson, William Farnaby<\/strong>, Andrew Ayscough<\/p>\n\n\n\n

Drug Discov Today <\/em>2017<\/strong>, 22, 965-969. <\/p>\n\n\n\n

doi: 10.1016\/j.drudis.2017.01.008<\/a><\/p>\n<\/div>

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2. Synthesis of (\u2212)-(S<\/em>,S<\/em>)-clemastine by Invertive N \u2192 C Aryl Migration in a Lithiated Carbamate<\/strong><\/p>\n\n\n\n

Anne M. Fournier,  Robert A. Brown, William Farnaby<\/strong>, Hideki Miyatake-Ondozabal and  Jonathan Clayden<\/p>\n\n\n\n

Org. Lett.<\/em> 2010<\/strong>, 12, 10, 2222\u20132225<\/p>\n\n\n\n

doi: 10.1021\/ol100627c<\/a><\/p>\n<\/div>

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1. N to C Aryl Migration in Lithiated Carbamates: \u03b1-Arylation of Benzylic Alcohols<\/strong><\/p>\n\n\n\n

Jonathan Clayden, William Farnaby<\/strong>, Damian M. Grainger, Ulrich Hennecke, Michele Mancinelli ,Daniel J. Tetlow, Ian H. Hillier and Mark A. Vincent<\/p>\n\n\n\n

J Am Chem Soc <\/em>2009<\/strong>, 131, 3410-3411. <\/p>\n\n\n\n

doi: 10.1021\/ja808959e<\/a><\/p>\n<\/div>

\"\"<\/figure><\/div>\n\n\n\n

Patents<\/h2>\n\n\n\n

(Several have been granted in varying territories; for simplicity initial applications are shown only)<\/em><\/p>\n\n\n\n

1. <\/strong>KRAS Degrading compounds comprising annulated 2-amino-3-cyano thiophenes WO2023099620<\/strong> (2023) <\/p>\n\n\n\n

2. <\/strong>Proteolysis targeting chimera (Protacs) as degraders of SMARCA2 and\/or SMARCA4. WO2020078933 <\/strong>(2020) <\/p>\n\n\n\n

3.<\/strong> 3-Substituted 2-aminoazaindole derivatives as GPR43 agonists and positive allosteric modulators and their preparation. WO2015198045<\/strong> (2015). <\/p>\n\n\n\n

4.<\/strong> Preparation of 1,3-substituted 2-aminoindole derivatives and analogues useful in the treatment or prevention of diabetes mellitus, obesity and inflammatory bowel disease. WO2015198046 <\/strong>(2015). <\/p>\n\n\n\n

5. <\/strong>Preparation of amide derivatives as lysophosphatidic acid receptor antagonists. WO2015025164 <\/strong>(2015). <\/p>\n\n\n\n

6.<\/strong> Preparation of pyridine and pyrimidine derivatives as cholesterol 24 hydroxylase inhibitors. WO2014163161 <\/strong>(2014). <\/p>\n\n\n\n

7. <\/strong>Pyridazinones as DAAO enzyme inhibitors. WO2014096757<\/strong> (2014)<\/p>\n\n\n\n

8. <\/strong>Pyridazinone compounds and their use as DAAO inhibitors. WO2013027000<\/strong> (2013). <\/p>\n\n\n\n

9.<\/strong> Preparation of substituted hydroxypiperidines as cholesterol 24-hydroxylase inhibitors. US20130090341 <\/strong>(2013). <\/p>\n\n\n\n

10. <\/strong>5- or 6- substituted 3-hydroxy-2-(1H)-pyridinones as d-amino acid oxidase (DAAO) inhibitors in therapy of diseases such as schizophrenia, cognitive disorder and pain. WO2013004996<\/strong> (2013). <\/p>\n\n\n\n

11. <\/strong>Pyrimidinone compounds and their use. WO2013004995 <\/strong>(2013).<\/p>\n","protected":false},"excerpt":{"rendered":"

23. Identification of a Highly Cooperative PROTAC Degrader Targeting GTP-Loaded KRAS(On) Alleles Vesna Vetma, Ilaria Puoti, Natalia K. Karolak, Sohini Chakraborti, Emelyne Diers, Enrico Girardi, Shakil Khan, Giorgia Kidd, Katrin G. Kropatsch, Ross Mclennan, Suzanne O\u2019Connor, Matthias Samwer, Nicole Trainor, Claire Whitworth, Andre J. Wijaya, Jeff Y. F. Wong, David Zollman, William Farnaby, Johannes Popow, … <\/p>\n

Read more “Publications”<\/span><\/a><\/p>\n","protected":false},"author":764,"featured_media":0,"parent":0,"menu_order":0,"comment_status":"closed","ping_status":"closed","template":"","meta":{"_acf_changed":false,"inspiro_hide_title":false,"footnotes":""},"class_list":["post-27","page","type-page","status-publish","hentry"],"acf":[],"_links":{"self":[{"href":"https:\/\/sites.dundee.ac.uk\/farnaby-group\/wp-json\/wp\/v2\/pages\/27","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/sites.dundee.ac.uk\/farnaby-group\/wp-json\/wp\/v2\/pages"}],"about":[{"href":"https:\/\/sites.dundee.ac.uk\/farnaby-group\/wp-json\/wp\/v2\/types\/page"}],"author":[{"embeddable":true,"href":"https:\/\/sites.dundee.ac.uk\/farnaby-group\/wp-json\/wp\/v2\/users\/764"}],"replies":[{"embeddable":true,"href":"https:\/\/sites.dundee.ac.uk\/farnaby-group\/wp-json\/wp\/v2\/comments?post=27"}],"version-history":[{"count":52,"href":"https:\/\/sites.dundee.ac.uk\/farnaby-group\/wp-json\/wp\/v2\/pages\/27\/revisions"}],"predecessor-version":[{"id":432,"href":"https:\/\/sites.dundee.ac.uk\/farnaby-group\/wp-json\/wp\/v2\/pages\/27\/revisions\/432"}],"wp:attachment":[{"href":"https:\/\/sites.dundee.ac.uk\/farnaby-group\/wp-json\/wp\/v2\/media?parent=27"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}