8th Fragment-based Drug Discovery Meeting
Event
8th RSC-BMCS Fragment-based Drug Discovery Meeting
Dates
Sunday – Tuesday, 27th-29th March 2022
Place
Churchill College, Cambridge plus Virtual
Churchill College
Churchill College
Important links and downloads
Twitter hashtag – #Fragments22
To view Covid-19 RSC policy, click here
Synopsis
The aim of the 8th RSC-BMCS Fragment-based Drug Discovery meeting will be to continue the focus on case studies in Fragment-based Drug Discovery that have delivered compounds to late stage medicinal chemistry, preclinical or clinical programmes. The Fragment series was started in 2007 and continues with this theme in having over three-quarters of the presentations focused on case studies. This will be complemented by technology progress in high concentration, NMR, SPR and X-ray screening.
Who should attend
This conference is suitable for scientists including chemists, biophysicists, structural biologists, etc., with either existing experience of fragments or wanting to learn about this exciting approach to drug discovery. This international meeting attracts delegates from the UK, several mainland European counties, as well as from the USA, Japan, China and South Korea.
Call for Posters / Abstracts
Abstract submission is now closed.
Programme
Sunday, 27th March
| 16.00- | 18.00 Delegate Registration |
| 19.00 | Buffet supper in Churchill College |
Monday, 28th March
| 07.30 | Registration and refreshments |
| 10.20 | Opening remarks Gordon Saxty, Fidelta |
| 10.30 | Session 1: Case Histories Session chair: Mike Hann, GSK S01: FBLD-Enabled Discovery of cGAS Inhibitors Fabio Casagrande and Katrin Groebke Zbinden |
| 11.00 | S02: The Discovery and optimisation of small molecule Inhibitors of TNF - Using Fragments to Inhibit a Protein: Protein Interaction James O’Connell, UCB |
| 11.30 | Session 2: Flash poster presentations Chair: Samantha Hughes, AstraZeneca FO01: Reactivity Profiling of Sulfur(VI) Fluorides as ‘Beyond Cysteine’ Reactive Electrophiles Katherine Gilbert, GSK |
| 11.32 | FO02: Development of Chemical Tools Targeting the Non-Catalytic Functions of Tankyrase Iona Black, The Institute of Cancer Research |
| 11.34 | FO03: Exploring the bromodomain of SMARCA4 (BRG1) by Weak Affinity Chromatography (WAC™) People's Poster Prize Winner Kirill Popov, Red Glead Discovery |
| 11.36 | FO04: Successful Fragment library screening by Grating Coupling Interferometry (GCI) against E3 Ligase Target Nick Martin, Domainex |
| 11.38 | FO05: Identification of fragments for the development of protein-protein-interaction inhibitors targeting the N-domain of p97 Student Poster Prize Winner Sebastian Bothe, Julius-Maximilians-University Wuerzburg |
| 11.40 | FO06: Synthesis and biological evaluation of small fragment inhibitors of Tumor Necrosis Factor Receptor 1 (TNFR1) Sara Pannilunghi, University of Geneva |
| 11.42 | FO07: The synergy of fragment-based drug discovery and high throughput approaches – application to the discovery of inhibitors of the KEAP1:NRF2 protein-protein interaction Charlotte Griffiths-Jones, Astex Pharmaceuticals |
| 11.44 | FO08: Title Fragment-based discovery of a novel, brain penetrant, orally active HDAC2 inhibitor Yuji Ochi, Astex Pharmaceuticals |
| 11.46 | FO09: 4-pi-photocyclisation as an enabling tool for the synthesis of highly functionalised small-ring carbocyclic and heterocyclic fragments Susannah Coote, Lancaster University |
| 11.48 | FO10: Using fragment-based drug discovery to synthesise novel inhibitors of Mycobacterium tuberculosis dihydrofolate reductase Tim Kirkman, University of Warwick |
| 11.50 | FO11: Inhibitor or degrader? A drug discovery campaign against B-Cell lymphoma 6 protein Roxanne Smith, Institute of Cancer Research |
| 11.52 | FO12: Fragment based design of mycobacterial thioredoxin reductase inhibitors: from a fragment screening to novel inhibitors Friederike Theresa Fusser, Westfälische Wilhelms-Universität |
| 11.54 | FO13: Specific inhibition of CK2α from an anchor outside the active site Paul Brear, University of Cambridge |
| 11.56 | FO15: Harnessing the Biophysical Fragment Screening Sweet Spot to Discover New Chemotypes for BRPF1 Inhibition Industry Poster Prize Winner Thomas Pesnot, Concept Life Sciences |
| 12.00 | Lunch |
| 12.30 | Exhibition, poster session (odd numbers) and networking |
| 13.30 | Session 3: Session chair: Samantha Hughes, AstraZeneca S03 Electrophile Fragment Screening as an Efficient Tool for Covalent Inhibitor Discovery Nir London, Weizmann Institute of Science |
| 14.00 | S04 Reactive fragment profiling against the DUBome by MS-proteomics Rosa Cookson, GSK |
| 14.30 | S05 Reimagining Druggability using Chemoproteomic Platforms Daniel Nomura, University of California |
| 15.00 | Refreshments, exhibition, networking |
| 15:30 | Session 4: Panel discussion Session chair: Mary Wheldon, University of Dundee S06Thoughts on the future for FBDD Gianni Chessari, Astex Pharmaceuticals S06: Fragments: Impact, Lessons and What's Next? Roderick Hubbard, Vernalis |
| 16:30 | Refreshments, exhibition and networking |
| 17:30 | Close |
| 18.20 | Walk to conference dinner |
| 19.00 | Reception and conference dinner at St Johns College |
Tuesday, 29th March
| 9.30 | Session 5: Session chair: Alison Woolford, Astex Pharmaceuticals S07: SpotXplorer fragments for maximal coverage of pharmacophore space György M Keserű, Research Centre for Natural Sciences (RCNS) |
| 10.00 | S08: Enabling CryoEM for SBDD and FBDD Pamela Williams, Astex Pharmaceuticals |
| 10.30 | Refreshments, exhibition, networking |
| 11.00 | S09: Rapid optimisation of fragments and hits to lead compounds from screening of crude reaction mixtures Lisa Baker, Vernalis |
| 11.30 | S10: GPCR Fragment-Based Drug Discovery Ijen Chen, Sosei Heptares Chris de Graaf, Sosei Heptares |
| 12.00 | Lunch |
| 12.30 | Exhibition, poster session (even numbers) and networking |
| 13.30 | Session 6: Session chair: Gordon Saxty, Fidelta S11: Crystallographic fragment screening identifies sixty diverse inhibitors of carboxylesterase Notum. An example of hit selection, validation and optimisation to ARUK3001185. Paul Fish, ARUK UCL Drug Discovery Institute |
| 14.00 | S12: Late Breaking Talk CAM833 - a small-molecule inhibitor of the BRCA2-RAD51 protein-protein interaction Marko Hyvonen, Department of Biochemistry, Cambridge |
| 14.15 | Refreshments, exhibition and networking |
| 15.00 | S13: Fragment-based design of methionine adenosyl transferase (MAT2a) inhibitors with anti-tumour effect Marianne Schimpl and Ulf Börjesson, AstraZeneca |
| 15.30 | S14: Discovery of the first VHL-recruiting, orally bioavailable PROTAC preferentially degrading SMARCA2 over SMARCA4 Christiane Kofink, Boehringer-Ingelheim RCV GmbH & Co KG, Vienna |
| 16.00 | S15: Fragment based discovery of MRTX1719, a selective inhibitor of the PRMT5.MTA complex for the treatment of MTAP deleted tumours Christopher Smith, Mirati Therapeutics |
| 16.30 | Closing remarks Mike Hann, GSK Close and depart |
Conference dinner
The conference dinner will take place on Monday 28th March at St John’s College and is included within the delegate registration fee. The Hall at St John’s College is viewed by some as the most magnificent Hall within the Colleges of Cambridge, this splendid room is housed in a 16th century building with an impressive hammerbeam roof and fine old linen fold panelling. It is a semi-formal evening and is a great time to come together to enjoy a three-course meal.
St Johns College
St Johns College Dining Room
Want to become a member?
To join the RSC in order to qualify for discounted registration fees at all RSC, please follow this RSC link.
Student Bursaries
The RSC BMCS are offering some student bursaries to attend this meeting in person. Applications are open to PhD and post-doctoral applicants studying at academic institutions. Preference will be given to members of the RSC, a National Adhering Organisation of the EFMC, and any co-sponsoring organisation.
Bursary application is now closed.
Sponsors
We are grateful to our confirmed sponsors for their valued support.
Exhibitors
We are grateful to our confirmed exhibitors for their valued support.
Organising Committee
Mike Hann, GSK
Samantha Hughes, AstraZeneca
Darryl McConnell, Boehringer Ingelheim
Gordon Saxty, Fidelta d.o.o. (Chair)
Mary Wheldon, University of Dundee (Treasurer)
Alison Woolford, Astex Pharmaceuticals
Secretariat Contact
Hg3 Conferences Ltd
+44 (0)1423 529333
E-mail
