Fragments 2019

7th RSC-BMCS Fragment-based Drug Discovery meeting

Sunday to Tuesday, 24th to 26th March 2019

at Churchill College, Cambridge, UK

 

Click image to the top left for flier download.

 

Registration is closed

 

Twitter hashtag - #Fragments19

 

Downloads and Links

Second announcement

First announcement

 

Delegate bookings - please check and notify Maggi Churchouse if your requirements have changed

 

FragNet delegates requiring extra nights of accommodation - please use this form

Alternative college accommodation (Churchill is fully booked) - University Rooms website
Hotel and bed and breakfast accommodation - Visit Cambridge website

 

Travel information and directions to Churchill College

RSC website

Synopsis

The aim of the 7th RSC-BMCS Fragment-based Drug Discovery meeting was 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 the theme, having over three-quarters of the presentations focused on case studies. The conference included successful examples from all types of fragment-based approaches, including high concentration, NMR, SPR and X-ray screening.

Who should attend

This conference was suitable for scientists including all chemists as well as other important disciplines including biophysics, structural biology, etc. This international meeting attracted delegates from the UK, several mainland European countries, as well as from the USA, Japan, China and South Korea.

Pre-conference Workshop
We were pleased to announce that we completely changed the pre-conference workshop for this event. It contained new materials provided by new speakers compared with previous years.   The pre-conference workshop was intended for those new to the area of FALG/FBLG an introduction into the fundamental principles governing fragment-based drug discovery approaches.

 

A series of four short presentations with opportunities for discussions took place. The pre-conference workshop was offered free-of-charge to conference attendees.

Call for Posters
Selected student speakers were invited to present at the flash presentation session prior to the poster session, and the flash poster programme may be found here.  The closing date for abstract submission was 1st February.

Programme

Where presentation titles are highlighted in blue, you may download a .pdf of the presentation.

Sunday, 24th March

14.00

Refreshments

14.15Registration opens
18.40Registration closes
 

Training Course

Session chairJohn Barker, Evotec, UK

15.00

Introduction to FBDD

Roderick Hubbard, University of York and Vernalis, UK

15.40

X-ray crystallography: an essential tool in Fragment Discovery but how to know its limitations

John Barker, Evotec, UK

16.15

Refreshments

16.45

Which fragment hits do we follow up?  Backing the right horsec

Alison Woolford, Astex Pharmaceuticals, UK

17.20

Fragments: the best training ground for our next generation of medicinal chemists

Darryl McConnell, Boehringer Ingelheim, Austria

18.00

Close

19.00

Buffet supper in College (closes at 20.00)

 

Monday, 25th March

09.15

Registration, refreshments, exhibition and posters

 
Session chairSamantha Hughes, AstraZeneca, UK

10.20

Opening remarks

Samantha Hughes, AstraZeneca, UK

10.30

Enabling FBDD for GPCRs with protein engineering and biophysics

Rob Cooke, Sosei Heptares, UK

11.15

Enabling drug discovery against the Bcl-2 family of proteins - from fragments to clinical candidates
Roderick Hubbard, University of York and Vernalis, UK, and
András Kotschy, Servier Research Institute of Medicinal Chemistry, Hungary

Session chairDarryl McConnell, Boehringer Ingelheim, Austria

12.00

Flash poster presentations

 

Fragment-based approach to discover compounds targeting the ATP-binding domain of bacterial histidine kinases
Marco Albanese, Oxford Drug Design Ltd / University of Buckingham, UK (P01)
 

Fragment-based approaches to targeting Mycobacterium abscessus PurC (SAICAR synthetase)
Sitthivut Charoensutthivarakul, University of Cambridge, UK (P09)
 

Towards the discovery of inhibitors targeting Zika and Dengue virus: methyltransferase using fragment-based screening
Shymaa Damfo, University College London, UK (P11)

 

Capillary electrophoresis and microscale thermophoresis in fragment-based drug discovery : development of screening bioassays towards FXIIa
Clara Davoine, University of Namur, Belgium (P13)


Combining in silico analysis and fragment screening to identify novel, druggable secondary ligand binding sites in cancer targets
People's Poster Prize Winner

Catherine Fletcher, Institute of Cancer Research / University of London, UK (P17)
 

Fragment screening with STD-NMR to identify new inhibitors of the anti-infective target DXS
Sandra Johannsen, Helmholtz Institute for Pharmaceutical Research Saarland, Germany (P21)
 

Fragment-based covalent ligand screening enables rapid discovery of inhibitors for the RBR E3 ubiquitin ligase HOIP
Academic Poster Prize Winner

Henrik Johansson, The Francis Crick Institute, UK (P23)

 

Design, synthesis and biochemical evaluation of bacterial collagenase inhibitors
Cansu Kaya, Helmholtz Institute for Pharmaceutical Research Saarland, Germany (P25)
 

Exploration of fragment-derived modulators of glycoside hydrolases
Eleni Makraki, University of York, UK (P27)
 

Fragment-based discovery of novel active and allosteric site binders of T. brucei farnesyl pyrophosphate synthase
Lena Muenzker, Novartis Basel, Switzerland / Philipps-Universität Marburg, Germany (P29)


Structurally-enabled progression of novel fragment hits for the epigenetic target BRD3
Silvia Paoletta, Sygnature Discovery, UK (P31)
 

Design and synthesis of allosteric inhibitors of cell cycle proteins as potential cancer therapeutics
Alexia Papaioannou, Newcastle University, UK (P33)
 

Rapid covalent-probe discovery by electrophile fragment screening
Efrat Resnick, The Weizmann Institute of Science, Israel (P35)
 

Use of paramagnetic NMR with lanthanide binding tags to locate fragment binding sites
Charlotte Softley, Helmholtz Zentrum Münich, Germany (P37)
 

Developing fragment screening methods for intrinsically disordered proteins: Tau as a test case
Darius Vagrys, University of York / Vernalis Rnd Ltd, UK (P39)
 

Discovery of a high affinity inhibitor of cGAS through NMR based FBDD
Hong Wang, Pfizer Worldwide R&D, USA (P41)
 

12.30

Lunch, poster session (odd-numbers), exhibition

Poster abstract from Lorena Zara (did not not print correctly in the handbook)

Poster abstract from Ailsa Powell (Industry Poster Prize Winner)

 

Session chairThorsten Nowak, C4X Discovery, UK

13.30

Learnings from fragment based lead generation for RORg

Yafeng Xue, AstraZeneca, Sweden

14.15

FBLD at Merck: strategy and biophysical screening platforms

Please send a message to request a copy of this presentation
Payal Sheth, Merck Sharp and Dohme, USA

15.00Refreshments, exhibition and posters
15.30

Fragment-based discovery of JAK1 inhibitors with excellent subtype selectivity

Andreas Ritzén, LEO Pharma, Denmark

16.15

Twenty years of thinking small
Harren Jhoti, Astex Pharmaceuticals, UK

17.00

Close

 

18.35

Walk to conference dinner

19.00Reception and conference dinner at Gonville and Caius College

 

Tuesday, 26th March

Session chairMike Hann, GlaxoSmithKline, UK

09.00

Fragment-based approaches to covalent inhibitors
György M Keserű, Hungarian Academy of Sciences, Hungary

09.45

Fragment-based stabilization of 14-3-3 Protein-Protein Interactions
Christian Ottmann, Eindhoven University of Technology, The Netherlands

10.30

Refreshments, exhibition and posters

11.00

Fragment-based discovery of chemical probes for new targets
Paul Brennan, Structural Genomics Consortium, University of Oxford, UK

11.45

Activity-based proteomics – protein and ligand discovery on a global scale
Ben Cravatt, The Scripps Research Institute, USA

12.30Lunch, poster session (even numbers), exhibition

 

Session chairAlison Woolford, Astex Pharmaceuticals, UK

13.30Kinetic fragment discovery, fragment recombination, and a cure for the common cold?
Ed Tate, Imperial College London, UK
14.15

The Lundbeck approach to FBDD in the CNS drug space: from weak fragments to the PDE1 inhibitor development candidate

Mauro Marigo, Lundbeck, Denmark

15.00

Refreshments, exhibition and posters

15.30Tractability assessment and hit ID using photoreactive fragments (PhABits)
Jacob Bush, GlaxoSmithKline, UK

16.15

Nanomolar KRAS inhibitors using fragments, NMR and Xray
Dirk Kessler, Boehringer-Ingelheim, Austria

17.00

Closing remarks

Alison Woolford, Astex Pharmaceuticals, UK

Close and depart

   

Bursaries and Sponsorship
Bursaries were available based on sponsorship of the event.

Bursary applications were invited, and the closing date was 1st February.

 

If you wished to sponsor students to expand their knowledge in this area, you were asked to contact the secretariat for further information.

We are grateful to our sponsors for their support of this event.

This meeting was sponsored by

 

 

 

  

 

      

We are grateful to EFMC for supporting this event

Exhibition Opportunities
Those companies wishing to have a trade stand were encouraged to apply early to avoid disappointment as these were limited.

 

The exhibition space for this event is now fully booked - sorry

 

Exhibition charges were:

£750  exhibition stand space only (excludes attendees)

£146  trade stand staff rate (no access to the technical sessions, conference dinner excluded)

£72    conference dinner for trade stand staff

Full delegate rates as detailed below

 

Delegate pack inserts could be booked at £275.

 

The exhibition stand package included:

We provided a stand space measuring 3 m wide x 1.6 m deep (including display and table).
- A six foot trestle table and chair(s)
- A blue baize table cloth
- Access to electricity and wi-fi

- Logo inclusion in delegate handbook and rolling slides

- Exhibitor's promotional page in the printed delegate handbook.

Registration Fees
Sorry, registration is closed - fully booked

 

Registration fees include the Sunday afternoon workshop and Monday evening conference dinner (opt in required for both).

 

Early rates for payments received by 21st January
£300 RSC member
£380 non-member

£155 RSC student* member

£195 student* non-member

Standard rates for payments received between 22nd January and 22nd February
£360 RSC member
£450 non-member

£185 RSC student* member

£230 student* non-member

Late rate for payments received from 23rd February onwards
£55   late payment fee to be added to all the above standard rates
 

* Student is undergraduate or post-graduate, not post-doc, and does not apply to students in paid employment.
Member is paid-up member of the RSC

 

£78   one night's B&B accommodation in an en suite room at Churchill College (Sunday and Monday available)

 

Cancellation Policy
In the event of cancellation before 9th March 2019, 80% of the fee paid will be refunded. Cancellations must be received in writing.  Refunds will not be possible after that date although substitutions are possible at any time.

Accommodation fees will only be refunded (in line with the policy above) if the room can be resold.

In the unlikely event of cancellation of the meeting, fees paid will be refunded in full.  Registration acknowledgements will be sent within two weeks.
Accommodation
No rooms remaining at Churchill College - sorry. 

B&B accommodation at Churchill College in an en-suite bedroom was available to book at the time of registration for both Sunday and Monday, charged at £78 per night.

Alternative Accommodation
College accommodation - University Rooms website
Hotel and bed and breakfast accommodation - Visit Cambridge website

Breakfasts
For those resident in College, breakfast was served from 7.30 to 9.30 am in the Dining Hall. For non-resident locals who wished to join a networking light buffet breakfast, this was served in the Buttery from 9 am on Monday and from 8 am on Tuesday.

 

Conference Dinner
The conference dinner on Monday was held in the Old Courts Main Hall at Gonville and Caius College, and attendance was included in the registration fee - opt in was required.

 

Dress code: smart, casual - or you may wish to wear your dinner jacket, tuxedo, or special gown.

 

Travel to/from Conference Dinner
It was expected that the majority will walk, setting off on foot from the Porters’ Lodge at 6.35 pm.

Because the walk to the conference dinner was 1.2 miles (25 minutes’ walk along pavements), we booked three people movers with 8 seats per vehicle (provided by CamCab) - two trips per vehicle. These were intended for those who might struggle with the walk. The timings of the trips (outward and return) were displayed on the Registration Desk, where those who needed to use the transport could sign up for the trips (48 seats each way in total).

Venue and Travel
Address:  Churchill College, Storey's Way, Cambridge CB3 0DS.

Travel Overview:  Churchill College is a 15-minute walk from the centre of Cambridge. Travel to Cambridge is convenient by rail as well as by road. 

 

Rail and Air: The College is 2.7 miles from Cambridge railway station (CBG), and 32 miles from Stansted airport (40 minutes). There are plenty of public transport options – see Churchill's website, including the U-bus from/to the railway station which costs  £2.20, journey time 30 minutes.

 

Car: There is ample free parking on site along Churchill Road (the College's private road) in the main car park at the end of that road, and in the staff car park (if available). A clearly-sign posted grassed area may also be available. Visitor parking permits are not required.

 

Directions: Please follow this link, and here is a site plan of Churchill College

Organising Committee

John Barker Evotec
Mike Hann GlaxoSmithKline
Samantha Hughes AstraZeneca
Darryl McConnell Boehringer Ingelheim
Thorsten Nowak C4X Discovery
Gordon Saxty (chair) Fidelta
Alison Woolford Astex Pharmaceuticals

Registration is closed