Book chapters and patents

Book Chapters

10. Ramachandran, S., Szewczyk, M., Barghout, S.H., Ciulli, A., Barsyte-Lovejoy, D., Vu, V.

HiBiT Cellular Thermal Shift Assay (HiBiT CETSA).

Methods Mol. Biol. 2023, vol. 2706, pp. 149-165

 

9. Ciulli, A.,* Hsia, O.

PROTAC Degraders: Mechanism, Recent Advances, and Future Challenges, In: ‘Protein Homeostasis in Drug Discovery: A Chemical Biology Perspective’

M. Kostic and L. H. Jones, Ed., John Wiley & Sons. 2023, pp. 317-356. ISBN: 978-1-119-77418-1

DOI: 10.1002/9781119774198.ch9

 

8. Bartoschik, T., Zoephel, A., Rumpel, K., Ciulli, A., Heffern, C.

MST and TRIC Technology to Reliably Study PROTAC Binary and Ternary Binding in Drug Development, In: ‘Targeted Protein Degradation’. Methods in Molecular Biology, vol 2365.

Cacace A.M., Hickey C.M., Békés M. (eds) Humana, New York, NY, 2021. ISBN: 978-1-0716-1664-2

Methods Mol Biol. 2021, vol. 2365, pp. 115-133

  • See Figures here

7. Casement R., Bond A., Craigon C., Ciulli A.*

Mechanistic and Structural Features of PROTAC Ternary Complexes, In: ‘Targeted Protein Degradation’. Methods in Molecular Biology, vol 2365.

Cacace A.M., Hickey C.M., Békés M. (eds) Humana, New York, NY, 2021. ISBN: 978-1-0716-1664-2

Methods Mol Biol. 2021, vol. 2365, pp. 79-113

  • See Figures here

6. Zollman, D., Ciulli, A.*

Structural and Biophysical Principles of Degrader Ternary Complexes, in: ‘Protein Degradation with New Chemical Modalities: Successful Strategies in Drug Discovery and Chemical Biology’.

H. Weinmann and C. Crews, Ed., Royal Society of Chemistry, Cambridge, UK, 2020, pp. 14–54. ISBN: 978-1-78801-686-5

DOI: 10.1039/9781839160691-00014

 

5. Bortoluzzi, A., Ciulli, A.*

Protein-Based NMR Methods Applied to Drug Discovery, in: ‘Applied Biophysics in Drug Discovery’.

D. Huddler and E. R. Zartler, Ed., John Wiley & Sons. 2017, pp. 153-173. ISBN: 978-1-119-09948-2

DOI: 10.1002/9781119099512.ch9

 

4. Ciulli, A.*

Biophysical Screening for the Discovery of Small-Molecule Ligands, in: ‘Protein-Ligand Interactions – Methods and Applications, 2nd Ed.’.

T. Daviter and M. Williams, Ed., Springer Protocols, Humana Press, 2013. ISBN: 978-1-62703-397-8

Methods Mol Biol. 2013, vol. 1008, pp. 357-388

3. Śledź, P., Abell, C., Ciulli, A.*

Ligand‐Observed NMR in Fragment‐Based Approaches, in: ‘NMR of Biomolecules: Towards Mechanistic Systems Biology’.

I. Bertini, K. McGreevy and G. Parigi, Ed., Wiley, 2012, pp. 265–280. ISBN: 978-3-527-32850-5

DOI: 10.1002/9783527644506.ch15

 

2. Heikkila, T.J., Surade, S., Silvestre, H.L., Dias, M.V., Ciulli, A., Bromfield, K.M., Scott, D.E., Howard, N.I, Wen, S., Wei, A.H., Osborne, D.M., Abell, C., Blundell, T.L.

Fragment-based drug discovery in academia: Experiences from a tuberculosis programme, in: Proceedings of the NATO International School of Crystallography, 40th Course ‘From Molecules to Medicine: Structure of Biological Macromolecules and Its Relevance in Combating New Diseases and Bioterrorism’.

J. L. Sussman and P. Spadon, Ed., Springer, 2009, pp. 21–36. ISBN: 978-9-048-12338-4

DOI: 10.1007/978-90-481-2339-1_3

 

1. Ciulli, A., Blundell, T.L., Abell, C.

Discovery and extrapolation of fragment structures towards drug design, in: ‘Computational and Structural Approaches to Drug Discovery – Ligand-Protein Interactions’.

R. M. Stroud and J. Finer-Moore, Ed., Royal Society of Chemistry, London, UK, 2008, pp. 293–318. ISBN: 978-1-84755-796-4

DOI: 10.1039/9781847557964-00291

 

 

Patents

13. KRAS degrading compounds comprising annulated 2-amino-3-cyano thiophenes

Broeker, Joachim; Ciulli, Alessio; Diers, Emelyne; Gollner, Andreas; Goodwin-Tindall, Jake; Farnaby, William; Kofink, Christiane; Mantoulidis, Andreas; McLennan, Ross; Popow, Johannes; Schmiedel, Martin; Smethurst, Christian Alan Paul; Trainor, Nicole; Weinstabl, Harald; Zhong, Siying, Zollman, David; Abbott, Jason; Cui, Jianwen; Fesik, Stephen W.; Little, Andrew; Sarkar, Dhruba; Waterson, Alex

PCT Int. Appl. (PCT/EP2022/083950, 30/11/2022), WO 2023/099620

 

12. Protein degrader

Ciulli, Alessio; Bond, Adam George; Craigon, Connor George; Chan, Kwok-Ho; Testa, Andrea; Alessi, Dario

PCT Int. Appl. (23/09/2022), WO 2023/047121

 

11. Improved small molecules

Ciulli, Alessio; Testa, Andrea; Maniaci, Chiara; Makukhin, Nikolai; Imaide, Satomi; Daniels, Danette; Riching, Kristin

PCT Int. Appl. (19/10/2021), WO 2022/101603

 

10. Proteolysis targeting chimera (Protacs) as degraders of SMARCA2 and/or SMARCA4

Ciulli, Alessio; Dank, Christian; Diers, Emelyne; Farnaby, William; Roy, Michael; Steurer, Steffen; Trainor, Nicole

PCT Int. Appl. (23/04/2020), WO 2020/078933

 

9. Bifunctional molecules for targeting USP14

Testa, Andrea; Hughes, Scott J.; Butcher, Steven P.; Ciulli, Alessio

PCT Int. Appl. (19/12/2019), WO 2019/238886

 

8. Bifunctional molecules for targeting RPN11

Ciulli, Alessio; Testa, Andrea; Hughes, Scott J.; Butcher, Steven P.

PCT Int. Appl. (19/12/2019), WO 2019/238817

 

7. Bifunctional molecules for targeting UCHL5

Ciulli, Alessio; Testa, Andrea; Hughes, Scott J.; Butcher, Steven P.

PCT Int. Appl. (19/12/2019), WO 2019/238816

 

6. Small molecules

Ciulli, Alessio; Maniaci, Chiara; Hughes, Scott J.; Testa, Andrea

PCT Int. Appl. (18/10/2018), WO 2018/189554

 

5. Fluorohydroxyproline derivatives useful in the preparation of proteolysis targeting chimeras

Ciulli, Alessio; Testa, Andrea

PCT Int. Appl. (22/03/2018), WO 2018/051107

 

4. Derivatives of 1-[(cyclopentyl or 2-pyrrolidinyl)carbonylaminomethyl]-4-(1,3-thiazol-5-yl) benzene which are useful for the treatment of proliferative, autoimmune or inflammatory diseases

Ciulli, Alessio; Zengerle, Michael; Chan, Kwok-Ho

PCT Int. Appl. (22/09/2016), WO 2016/146985

 

3. Enzyme Functional Probes

Shiao, Enrique, L.; Baud, Matthias, G. J.; Ciulli, Alessio; Chan, Kwok-Ho; Zengerle, Michael

PCT Int. Appl. (04/06/2015), WO 2015/079259

 

2. Compounds and Methods for the Inhibition of VCB E3 Ubiquitin Ligase.

Crews, Craig, M.; Buckley, Dennis; Ciulli, Alessio; Jorgensen, William; Gareiss, Peter, C.; Van Molle, Inge; Gustafson, Jeffrey; Tae, Hyun-Seop; Michel, Julien; Hoyer, Dentin, W.; Roth, Anke, G.; Harling, John, D.; Smith, Ian Edward, D.; Miah, Afjal, H.; Campos, Sebastien, A.; Le, Joelle

PCT Int. Appl. (18/07/2013), WO 2013/106646

 

1. Compounds & Methods for the Enhanced Degradation of Targeted Proteins & Other Polypeptides by an E3 Ubiquitin Ligase.

Crews, Craig, M.; Buckley, Dennis; Ciulli, Alessio; Jorgensen, William; Gareiss, Peter, C.; Van Molle, Inge; Gustafson, Jeffrey; Tae, Hyun-Seop; Michel, Julien; Hoyer, Dentin, W.; Roth, Anke, G.; Harling, John, D.; Smith, Ian Edward, D.; Miah, Afjal, H.; Campos, Sebastien, A.; Le, Joelle

PCT Int. Appl. (18/07/2013), WO 2013/106643