7th RSC / SCI symposium on GPCRs

in Medicinal Chemistry

 

Monday-Wednesday, 10th-12th September 2018

 

Aptuit, Verona, Italy

 

 

 

 

 

 

 

Registration is open

 

Twitter hashtag - #GPCRsVerona

 

Downloads and Links

Online registration - for payment by card

Registration form - for payment by bank transfer or cheque

 

Third announcement

Second announcement

Poster abstract template - closing date is 11th July

Bursary application form - closing date is 30th July

 

Accommodation booking agency

Directions to Aptuit

Public bus-stop near Aptuit

Coach pick-up point in Verona

 

RSC webpage

SCI webpage

 

Synopsis

The key role of G protein-coupled receptors (GPCRs) in human disease underpins their importance to modern medicine. We are pleased to announce that Aptuit, Italy will support the seventh meeting in this series on GPCR drug discovery, which will combine cutting edge medicinal chemistry with innovative structural biology and novel drug design approaches.

 

The meeting will consist of:

Clinical candidates
Case studies in GPCR drug discovery and development
New structural biology and drug design
Allosteric modulation


Also:   poster session - trade exhibition opportunities - two evening dinners and vineyard visit - accommodation agency booking service

 

Call for Abstracts

Applications for poster presentations are welcome. Posters will be displayed throughout the meeting and applicants should indicate whether they wish to be considered for a flash oral presentation when submitting an abstract (two minutes, single slide).  Download an abstract template here and return to the secretariat.  The closing date is 11th July.  

 

The closing date for oral abstracts has passed (2nd January), and no further oral abstracts will be considered.

 

Programme - provisional

 

Monday, 10th September

08.30

Registration and refreshments

 

Session chair:  Fabrizio Micheli, Aptuit

09.20

Opening remarks

Simone Braggio, VP Drug Design and Discovery, Aptuit, and

David Miller, Co-chairman of the GPCRs Organising Committee

09:30

KeynoteGPCR Consortium: four years of progress in structural biology
Michael Hanson, GPCR Consortium, USA

10.20

The discovery of novel dopamine D1 positive allosteric modulators for the treatment of neurodegenerative disorders

Erik Hembre, Lilly

10.50

Refreshments, exhibition and posters

11.20

Ligand and sidechain mutations by FEP simulations: two sides of the same coin to determine binding modes on GPCRs
Hugo Gutiérrez de Terán, Uppsala University, Sweden

11.50

Discovery of selective Orexin-1 receptor antagonists: optimization of selectivity, pharmacokinetics and brain penetration

Brock Shireman, Janssen, USA

12.20

Lunch, exhibition and posters

 

 

Session chair:  Sarah Skerratt, Vertex Pharmaceuticals

13.30

Mining structural GPCR-ligand interaction maps to navigate medicinal chemistry space

Chris de Graaf, Heptares Therapeutics, UK and Vrije Universiteit Amsterdam, The Netherlands

14.00

Discovery of potent spiroazetidine-indolinones as M1 positive allosteric modulators
Carolina Martinez Lamenca, Janssen, Belgium

14.20

Refreshments, exhibition and posters

14.50

KeynoteStructure and mechanism of human CNS GPCRs

Daniel Rosenbaum, University of Texas Southwestern Medical Center, USA

15.40

Flash oral poster presentations (two-minute slots)

16.20

Poster session and drinks reception

18.30

Coaches depart for evening dinner restaurant

19.00

Dinner at San Matteo Church Ristorante, Verona city centre,

followed by free time

 

 

Tuesday, 11th September

 

Session chair:  David Miller, Inflazome

09.30

KeynoteApplication of structure-based drug design to peptidergic GPCRs

Miles Congreve, Heptares Therapeutics, UK

10.20

Trisubstituted cyclohexanes as dual antagonists of CCR2 and CCR5

Robert Cherney, BMS, USA

10.50

Refreshments, exhibition and posters

11.20

Disclosure of the clinical candidate BAY-840, a potent and selective hBradykinin B1 receptor antagonist for the treatment of chronic inflammatory diseases, generated within the Bayer-Evotec strategic alliance

Adam Davenport, Evotec

11.50

Novel and potent spirocyclic compounds as ghrelin receptor agonists
Cristina Gardelli, AstraZeneca, Sweden

12.20

Lunch, exhibition and posters

 

 

Session chair:  Caroline Low, Consultant

13.30

Keynote:  Allosteric modulators of GPCRs: theoretical and practical considerations

Arthur Christopoulos, Monash University, Australia

14.20

Hits and misses in the application of FEP to different classes of GPCRs

Herman van Vlijmen, Janssen, Pharmaceutical Companies of Johnson & Johnson, USA

14.50

Refreshments, exhibition and posters

15.20

Rapid identification and optimization of a novel CGRP receptor antagonist chemotype

Brendan Crowley, Merck, USA

16.10

Chemical optimization of centrally acting anti-obesity agents

Lothar Schwink, Sanofi-Aventis Deutschland, Germany

16.40

Close

16.50

Coaches depart for evening visits

17.30

Arrive Tommasi vineyard

18.40

Travel to Villa Quaranta

19.10

Arrive Villa Quaranta, dinner

21.20

Depart Villa Quaranta

22.00

Arrive Giardini Pradaval, Verona city centre

 

 

Wednesday, 12th September

 

Session chair:  Adrian Hall, UCB, Belgium

09.30

Keynote:  Shedding light on G protein bias: structures of GPCRs coupled to G proteins determined by cryo-EM and X-ray crystallography

Chris Tate, MRC Laboratory of Molecular Biology, UK

10.20

Program building and chemical devalidation of GPR39 agonism as a diabetes target

Stefan Peukert, Novartis Institute of Biomedical Research, USA

10.50

Refreshments, exhibition and posters

11.20

Triazolo-pyrimidines as adenosine receptor antagonists: an overview
Stephanie Federico, Università degli Studi di Trieste, Italy

11.50

GPCR hit identification via DNA-encoded libraries and optimization towards therapeutic agents for inflammation and oncology
Andy McRiner, X-Chem Pharmaceuticals, USA

12.20

Identification of highly selective orexin 1 receptor antagonists: structure-based scaffold modifications to improve subtype selectivity and synthesis of a novel bicyclic scaffold
Uta Lessel, Boehringer Ingelheim, Germany

12.50

Lunch, exhibition and posters

 

 

Session chair:  Caroline Low, Consultant

13.50

GPCR drug discovery with structural insights

Xiaomin Chen, Pfizer, USA

14.20

Discovery of Balovaptan, a vasopressin 1a receptor antagonist for the treatment of autism

Patrick Schnider, Roche, Switzerland

14.50

Closing remarks

Adrian Hall, Co-chairman of the GPCRs Organising Committee

15.00

Close and depart

 

Registration, Fees and Bursaries

Online registration - for payment by card

Registration form - for payment by bank transfer or cheque

 

Registration fees include Monday evening's dinner and Tuesday evening's vineyard visit and dinner.

Early rates for payments received by 5th June
£430  RSC or SCI member
£530  Non-member
£180  RSC or SCI student* member
£228  Student* non-member

Standard rates for payments received between 6th June and 8th August
£505  RSC or SCI member
£600  Non-member
£205  RSC or SCI student* member
£260  Student* non-member

Late rates for payments received from 9th August onwards
£40  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 or SCI.

Discounted rates are offered to RSC and SCI student members, and some student bursaries are available.  Closing date is 30th July.  Please download a bursary application form here.

 

Cancellation Policy

In the event of cancellation by 27th August, 80% of the registration fee paid will be refunded. Cancellations must be received in writing. Refunds will not be possible from 28th August onwards, although substitutions are possible at any time.

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, Dinners and Social Activities

For all accommodation requests (including last-minute bookings), we suggest you use the 24-hour service provided by Verona Booking, using this weblink.

 

The registration fees include dinners on Monday and Tuesday evening and vineyard tour.

 

Monday:  Meet at Ristorante San Matteo Church for dinner (choice of pizza or pasta), dessert, drinks and networking.

 

Tuesday:  Coach travel from Aptuit, and visit to Tommasi Vineyard with tour and post-tour drink.  Coach to Villa Quaranta for dinner, and return coach to Verona city.

 

Venue and Travel

Address:

Aptuit, Via Alessandro Fleming 4, 37135 Verona, Italy, telephone +39 (0)45 821 8111.  Directions may be found here.

 

Distances and Journey Times by Car from Aptuit:

Verona Villafranca airport, 7.5 miles, 15-20 minutes

Verona Porta Nuova railway station, 3.5 miles, 15-20 minutes

Verona city centre, 3.5 miles, 15-20 minutes.

 

Coaches provided by Conference

A coach service will be provided gratis between Verona city centre

(Giardini Pradaval location map) and Aptuit at the beginning and end of each day, and on a daily basis.

 

Transport between the Airport and Railway Station

Aerobus provides public transport between the city centre, the railway station and the airport, running every 20 minutes.  Further information may be found on this weblink and Aerobus tickets may be bought via this weblink.

 

Public Bus to Aptuit

Bus lines       51 and 52 (urban lines), and 148 (extra-urban line)
Direction      Sacra Famiglia / Castel d’Azzano
Bus stop        via Dell’Esperanto/Glaxo (see this map)
Website        for routes and timetable
Journey time 15-20 minutes from Verona Porta Nuova railway station, depending on traffic.

Bus-stop        plan showing location of bus-stop at Aptuit
 

Taxi

Aptuit's preferred taxi supplier is Ready Car Service, who offer special rates when you quote “Aptuit-GPCR conference – please apply Aptuit rate”.   To book online, please use this weblink, and to book by e-mail, please use this e-mail address. 

Telephone +39 (0)45 505066

Fax            +39 (0)45 505118

Mobile       +39 (0)3497 589992 (24-hour service)

 

Ready Car Service Aptuit rates are:

- Verona city centre car: (3 people) 17.50€ minivan, (8 people) 23.50€
- Verona airport: car (3 people) 21€, minivan (8 people) 28.50€
- Verona railway station: similar rates to Verona city centre.
Public taxis may cost a little less on average, but rates may vary depending on journey time / traffic.

 

RadioTaxi App
Website
Telephone     +39 (0)45 532666 (24-hour service)

Mobile           +39 (0)3403 210021
Fare               0.97€/km (city centre itineraries)
Payment         cash (Euro), or credit card payments upon request

                      at time of taxi booking (not AmEx).

 

Exhibition Opportunities

Exhibition packages are available, priced at:
£1,320     Exhibition stand including one full delegate
£1,740     Exhibition stand including two full delegates
 

Each exhibition package includes stand space measuring 3 m wide x 2 m deep (including table), electrical and wi-fi access, and full attendance at the technical programme, poster sessions, Monday evening dinner, and Tuesday evening vineyard visit and dinner.

Delegate pack inserts may be booked, charged at £200 (maximum of two sheets of A4 fixed together).
 

Sponsors

Special thanks to Aptuit and Evotec for supporting this event. Additional sponsors would be welcomed.

 

 

We are grateful to EFMC and COMS for supporting this event

 

 

Organising Committee

Adrian Hall (co-chairman), UCB
Caroline Low, Consultant
Jon Mason, Heptares
Fabrizio Micheli, Aptuit
David Miller (co-chairman), Inflazome
Sarah Skerratt, Vertex

 

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 

 

Registration is open

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