7th RSC / SCI symposium on GPCRs

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

The meeting consisted 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 were welcome. Posters were displayed throughout the meeting and applicants indicated whether they wished to be considered for a flash oral presentation when submitting an abstract (two minutes, single slide), and the flash presentation programme may be found here. The closing date was 11th July.

The closing date for oral abstracts submissions was 2nd January.

Programme

Monday, 10th September
08.30	Registration and refreshments
	Session chair: Adrian Hall, UCB, Belgium
09.20	Opening remarks Simone Braggio, SVP Discovery Alliance Management, Evotec, and Adrian Hall, Co-chairman of the GPCRs Organising Committee
09:30	Keynote: GPCR 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, USA
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: Duncan Hay, Vertex Pharmaceuticals, UK
13.30	Trisubstituted cyclohexanes as dual antagonists of CCR2 and CCR5 Robert Cherney, BMS, USA
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	Keynote: Application of structure-based drug design to peptidergic GPCRs Miles Congreve, Heptares Therapeutics, UK
15.40	Flash oral poster presentations (two-minute slots) Flash presentation programme may be downloaded here
15.40	Application of luminescence and BRET to GPCR biology: development of new assay formats for screening and compound profiling Gary Allenby, Aurelia Bioscience Ltd, UK
15.42	Understanding PAR2 active-state through a combined structure-based drug design and mutagenesis study Flavio Ballante, Uppsala University, Sweden
15.44	The design, synthesis and pharmacological evaluation of highly potent and selective fluorescently-labelled A2A AR antagonists based on preladenant (SCH420814) Eleonora Comeo, University of Nottingham, UK
15.46	Development of a high affinity, selective fluorescent ligand for CB2 receptor Anna Cooper, University of Otago, New Zealand
15.48	Expanding the pharmacological toolbox to study chemokine receptor CXCR4 by developing fluorescent probes Sebastian Dekkers, University of Nottingham, UK
15.50	Development of a novel biophysical fragment screening platform for detergent-free purified GPCRs Daniel Hothersall, Domainex Ltd, UK
15.52	Optimisation of peptide linker-based fluorescent ligands for histamine H1 receptor Zhi Yuan Kok, University of Nottingham, UK
15.54	Identification of novel MRGX2-agonists which dose-dependently activate mast cells Helen Kühn, University Hospital Erlangen, Germany
15.56	Probing inactive states of the A2A receptor by 19F NMR Erik Landin, University of Bristol, UK
15.58	Development of molecular tools for the study of adenosine A1 receptors Martin Lochner, University of Bern, Switzerland
16.00	G protein specific bias in a series of CCR5 chemokine analogs Emily Lorenzen, Rockefeller University, USA
16.02	The Salipro® system for stabilization of membrane proteins Robin Löving, Salipro Biotech, Sweden
16.04	Novel biased agonists for immune-metabolic receptor GPR84 induce distinct responses in primary murine macrophages Daniel Lucy, University of Oxford, UK
16.06	Structure-activity relationships of imidazothiazinones and analogs as antagonists of the cannabinoid-activated orphan G protein-coupled receptor GPR18 Andhika Mahardhika, University of Bonn, Germany
16.08	Enhancing GPCR structures with computer-assisted drug design Juan Carlos Mobarec, Heptares Therapeutics Ltd, UK
16.10	Design, synthesis and evaluation of a diazirine photoaffinity probe for Ligand-based receptor capture targeting on GPCRs Frederike Müskens, University of Glasgow, UK
16.12	Functional effects of biased oxyntomodulin analogues Phil Pickford, Imperial College London, UK
16.14	Computational design of thermostabilizing point mutations for G protein-coupled receptors Petr Popov, Moscow Institute of Physics and Technology, Russia
16.16	Developing PAR1 Inhibitors based on KLK4 protease for clinical translation as therapeutic anticancer agents Eitan Rabinovich, Ben-Gurion University of the Negev, Israel
16.18	Molecular modeling studies on MOR endogenous and exogenous agonists and antagonists Simone Ronsisvalle, University of Catania, Italy
16.20	MDPI Poster prize-winner Development of covalent inhibitors of GRK5 for treatment of heart failure Rachel Rowlands, University of Michigan, USA
16.22	Tag-lite, a powerful non-radioactive platform for kinetic binding Pauline Scholler, Cisbio Bioassays, France
16.24	Summarizing and understanding SAR and activity cliffs in GPCRs Giovanna Tedesco, Cresset, UK
16.26	Development of water-soluble prodrugs of 8-sulfonamido¬phenylxanthines – potent and selective adenosine A2B receptor antagonists Ahmed Temirak, University of Bonn, Germany
16.28	Development of fluorescent ligands to detect cannabinoid type 2 receptor (CB2) Francesco Spinelli, Università degli Studi di Bari Aldo Moro, Italy
16.30	Detection of allostery with rigidity propagation across GPCR networks Adnan Sljoka, Kwansei Gakuin University, Japan
16.32	Poster session and drinks reception
18.00	Coaches depart Verona, a little free time
19.30	Dinner at San Matteo Church Ristorante, Verona city centre, followed by free time
	Tuesday, 11th September
	Session chair: David Miller, Inflazome, Ireland
09.30	Keynote: Structure and mechanism of human CNS GPCRs Daniel Rosenbaum, University of Texas Southwestern Medical Center, USA
10.20	Mining structural GPCR-ligand interaction maps to navigate medicinal chemistry space Chris de Graaf, Heptares Therapeutics, UK and Vrije Universiteit Amsterdam, The Netherlands
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, UK
11.50	Novel and potent spirocyclic compounds as ghrelin receptor agonists Cristina Gardelli, AstraZeneca, Sweden
12.20	Lunch, exhibition and posters Over the lunch break, Aptuit has kindly offered two site tours, each lasting 30 minutes. Spaces are very limited, and Aptuit reserves the right to decline requests from certain organisations: 12.25 MedChem tour (30 minutes) 12.55 DMPK tour (30 minutes)
	Session chair: Caroline Low, Consultant, UK
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
16.45	Coaches depart for evening visits
17.35	Arrive Tommasi vineyard
18.45	Travel to Villa Quaranta
19.15	Arrive Villa Quaranta, dinner
21.25	Depart Villa Quaranta
22.05	Arrive Giardini Pradaval, Verona city centre
	Wednesday, 12th September
	Session chair: Fabrizio Micheli, Aptuit, Italy
09.30	Keynote: GPCR drug design comes of age: structure drives rational design with key lessons and learnings to enhance future success Jonathan Mason, Scientific Advisor and Heptares Therapeutics 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 Radoslaw Lipinski, Boehringer Ingelheim, Germany
12.50	Lunch, exhibition and posters
	Session chair: Caroline Low, Consultant, UK
13.50	The Confobody Technology: a new platform to enable fragment screening on GPCRs Dr Christel Menet, CSO, Confo Therapeutics, Belgium
14.20	Discovery of Balovaptan, a vasopressin 1a receptor antagonist for the treatment of autism Patrick Schnider, Roche, Switzerland
14.50	Closing remarks David Miller, Co-chairman of the GPCRs Organising Committee
15.05	Close and depart

Registration, Fees and Bursaries

Registration is closed. Registration fees included 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 fcor 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 were offered to RSC and SCI student members, and some student bursaries were available. The closing date was 30th July.

Cancellation Policy

In the event of cancellation by 27^th August, 80% of the registration fee paid will be refunded. Cancellations must be received in writing. Refunds will not be possible from 28^th 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 suggested using the 24-hour service provided by Verona Booking.

The registration fees included 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 (an Evotec company), 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 was 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.

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)
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”.

Telephone +39 (0)45 505066

Fax +39 (0)45 505118

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

Ready Car Service rates will be quoted for each individual journey. Public taxis may cost a little less on average, but rates may vary depending on journey time / traffic.

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

Mobile +39 (0)3403 210021
Payment cash (Euro), or credit card payments upon request

at time of taxi booking

Exhibition Opportunities

The exhibition was fully booked.

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

Each exhibition package included 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 could be booked, charged at £200 (maximum of two sheets of A4 fixed together).