X-ray crystal structure of lovastatin bound to the CD11a I-domain of beta 2 integrin, LFA-1. PDB ID: 1CQP, Kallen et al., J. Mol. Biol. 1999, 292, 1–9

Integrin Targeted Drug Discovery

 

Thursday, 28th March 2019

 

Royal Society of Chemistry at Burlington House, London, UK

 

 

Registration is closed

  

Twitter hashtag - #Integrins19

 

Downloads and Links
S
econd announcement and call for posters

First announcement and call for abstracts

Directions to the venue
RSC website

 

Synopsis
Integrins are heterodimeric, transmembrane receptors that function in cell adhesion and signalling. They are central to many disease states, including cancer, thrombosis, multiple sclerosis and Crohn’s disease. Integrin targeted therapeutics have been under investigation for some time, but few compounds have made it to / remained on the market due to side effects or lack of efficacy. Given the more recent structural insights, better understanding of downstream pathways, and potential application to a range of therapeutic areas, there has been a resurgence of interest in integrin inhibitors. This symposium brought together researchers in this area who provided both a historical overview of the area and recent progress in designing the next generation of integrin inhibitors.

 

Who should attend
Scientists from industry and academia, including medicinal and computational chemists.

 

Features of the Meeting
Therapeutic targets for integrins
Targeting different RGD recognising integrins
Drug discovery, medicinal chemistry and structure-based design
Plenary speakers, poster session and trade exhibition
 

Call for Poster Abstracts
Applications for poster presentations were welcomed. Posters were displayed throughout the day, and the closing date for submissions was  7th February 2019.    The call for oral abstract submission closed on 14th September 2018.

 

Accepted presenters should note that we regret that we did not offer the opportunity to deliver a flash oral presentation, as there was insufficient time in the programme - sorry!

 

Programme

Where presentation titles are highlighted in blue, the presentation file may be downloaded.

 

09.15

Registration and refreshments

09.55

Welcome and opening remarks

Douglas Williamson, Vernalis Research, UK

 

 

Session chair:  Richard Hatley, GlaxoSmithKline, UK

10.00

Integrins as therapeutic targets: a superficial, but non-trivial family

Simon Goodman, Freelance Consultant, formerly of Merck Serono

10.50

Discovery of novel integrin inhibitors

Thomas McInally, University of Nottingham, UK

11.25

Succinimide-based conjugates improve isoDGR cyclopeptide affinity to αvβ3 without promoting integrin allosteric activation

Giovanna Musco, San Raffaele Hospital Milan, Italy

12.00

New beta-lactam derivatives modulate cell adhesion and signaling mediated by RGD-binding and leukocyte integrins

Daria Giacomini, Chemistry, University of Bologna, Italy

12.30

Lunch, posters and exhibition

 

 

Session chair:  Blaise Lippa, Morphic Therapeutic, USA

13.30

Challenges in integrin antagonist discovery - lessons learnt from GPIIb/IIIa antagonists

Dermot Cox, Molecular and Cellular Therapeutics, Royal College of Surgeons in Ireland, Ireland

14.05

Integrin αvβ6-specific peptide-drug conjugates provide a novel and effective therapy for pancreatic cancer
Kate Moore, Barts Cancer Institute
, UK

14.40

New strategies to improve the efficacy of small molecule integrin antagonists

Helen Sheldrake, Cancer Therapeutics, University of Bradford, UK

15.15

Refreshments, exhibition and posters

 

 

Session chair:  Douglas Williamson, Vernalis Research, UK

15.45

Design of highly potent selective ligands for RGD recognizing integrin subtypes and their application in medicine

Horst Kessler, Chemistry, Technical University of Münich, Germany

16.20

Metadynamics-inspired discovery of cyclic pentapeptides as selective αvβ6 integrin ligands

Luciana Marinelli, University of Naples, Italy

16.55

Closing remarks

Richard Hatley, GlaxoSmithKline, UK

17.00

Drinks reception

18.00

Meeting closes

 

Registration and Bursaries
Registration for payments received by 24th February:
£120 RSC member
£150 Non-member
  £60 RSC student* member

Late rates for payments received from 25th February onwards:
£30 Late payment fee to be added to 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.

Some student bursaries were available (to assist with registration fee, travel and accommodation).  The closing date was 7th February.
 

Exhibition
A relevant trade exhibition added value to the symposium.   The exhibition were held in the same room as the catering (refreshments and lunch) and posters, and the exhibition package cost £530 and included:
- chair and table
- electrical access and wi-fi access

- one full delegate attendance.
 

A delegate pack insert could be booked at £175 - no more than two pages of A4 fixed together.

 

Venue and Travel
The symposium was held in the Science and Fish Rooms, Royal Society of Chemistry at Burlington House, Piccadilly, London, W1J 0BA, UK. Directions to venue.

Situated in central London, the RSC is easily accessible by public transport, and close to Green Park tube station.

 

Sponsors
Sponsors were encouraged to support this event, which will help us to offer inexpensive registration fees to young chemists.

 

We are grateful to our conference sponsor

 

 

 

We are grateful to our media partner

We are grateful to EFMC for supporting this event

Organising Committee
Richard Hatley, GlaxoSmithKline
Douglas Williamson, Vernalis Research (chairman)
Alison Woolford, Astex Pharmaceuticals
 

Secretariat Contact
Maggi Churchouse, 3 East Barn, Market Weston Road, Thelnetham, Diss IP22 1JJ, UK
Telephone: +44 (0)1359 221004
E-mail:  maggi@maggichurchouseevents.co.uk

 

To register an interest in future Integrins symposia, please e-mail the Secretariat.

 

Registration is open

 


 

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