GPCRs in Medicinal Chemistry
8th RSC / SCI symposium on GPCRs in Medicinal Chemistry
Wednesday-Friday, 5th-7th October 2022
Evotec Campus Levi-Montalcini, Verona, Italy
Downloads and Links
Registration closing dates:
6th September – registration against invoice (bank transfers): Tuesday, 6th September
30th September – online registration (card payments)
The key role of G protein-coupled receptors (GPCRs) in human disease underpins their importance to modern medicine. We were pleased to hold this 8th meeting in the series on GPCR drug discovery, which combined cutting edge medicinal chemistry with innovative structural biology and novel drug design approaches.
The meeting will consisted of:
• Case studies in GPCR drug discovery and development
• Structural biology advances and impact on drug design
• Showcasing multiple modalities and drug discovery approaches to modulating GPCRs
Also: poster session – trade exhibition opportunities – two evening dinners and vineyard visit – accommodation agency booking service.
Call for Abstracts
Applications for oral and poster presentation were welcome. Posters were displayed throughout the meeting and applicants indicated whether they wished to be considered for a short flash oral presentation when submitting an abstract. The closing dates were 31st March (oral, extended date) and 11th August (poster).
Poster Prize Winners
The winner of the Judges’ First Prize is Elissa Fink of University of California-San Francisco in the USA, poster number 7, entitled “Structure-based discovery of novel non-opioid analgesics acting through the α2A-adrenergic receptor”. She wins a £200 book voucher from RSC Chemical Biology, and £100 cash from ACS Journals.
The winner of the Judges’ Second Prize is Shubham Vishnoi of Bernal Institute University of Limerick in Ireland, poster number 20, entitled “Structural and functional characterization peptide co-agonists targeting class B1 G protein-coupled receptors as therapeutic targets for metabolic disorders”. He wins a £100 RSC book voucher from RSC Medicinal Chemistry, and £50 cash from ACS Journals.
The winners of the People’s Prize are Paul Eisenhuth and Fabian Liessmann of Leipzig University in Germany, poster number 11, entitled “Ultra-large library docking in Rosetta EvoLigand tackles challenging GPCR targets in drug discovery”. They win a £100 book voucher from RSC Medicinal Chemistry, and £50 cash from ACS Journals.
Well done to all four!
Wednesday, 5th October
|08:30||Registration and refreshments|
|Session chair: Nigel Swain, Sosei Heptares, UK|
Karen Lackey, Evotec US (video)
Ciriaco Maraschiello, Evotec, IT
Caroline Low, Co-chair of the Organising Committee
|09:50||Structure-guided GPCR drug discovery
Keynote: Bryan Roth, University of North Carolina Chapel Hill Medical School, US
|10:40||Discovery of PF-07081532: a small molecule GLP-1 receptor agonist suitable for once-daily oral administration
David Griffith, Pfizer, US
|11:20||Refreshments, exhibition and posters|
|11:50||The resolution revolution:GPCR structure-based drug design in 20:20 vision (in 2022)
James Errey, Evotec, UK
|12:20||Discovery of AZD5462, an oral agonist of the Relaxin family peptide receptor 1 (RXFP1) for the treatment of cardiorenal disease
Kenneth Granberg, AstraZeneca, SE
|12:50||Lunch, exhibition and posters|
|Session chair: Iuni Trist, Evotec, IT|
|14:00||Discovery of the clinical candidate ACT-777991, a potent CXCR3 antagonist with therapeutic potential in autoimmune diseases
Eva Caroff, Idorsia, CH
|14:30||AlphaFold applied to GPCRs
Miles Congreve and Caroline Low, Isomorphic Laboratories, UK
|15:00||Refreshments, exhibition and posters|
|15:30||Discovery of potent and selective S1P2 receptor antagonists for treatment of idiopathic pulmonary fibrosis
Bertrand Heckmann, Galapagos, FR
|16:00||Targeting chemokine receptor CCR2 - from insurmountable antagonists to affinity-based probes
Laura Heitman, University of Leiden, NL
|Session chair: Nadia Ahmad, Charles River, UK|
|16:30||Flash oral poster presentations|
|17.00||Poster session and drinks reception|
|18:00||Coaches depart for Verona, a little free time|
|19:00||Dinner at Ristorante Trisapori, Verona city centre, followed by free time|
Thursday, 6th October
|Session chair: Duncan Hay, Vertex Pharmaceuticals, UK|
|09.30||Biased signaling atlas and community guidelines
Keynote: David Gloriam, University of Copenhagen (virtual speaker)
|10:20||Discovery of MK-4710: a potent, selective, and bioavailable M4 positive allosteric modulator
Michael Lo, MSD, US
|10:50||Refreshments, exhibition and posters|
|11:20||The discovery of CFTX-1554 as an inhibitor of the angiotensin II type 2 receptor, a clinically validated target for the treatment of neuropathic pain
Ann De Blieck, Confo Therapeutics, BE
|11:50||Structure-based drug discovery across the medicinal chemical GPCRome
Chris de Graaf, Sosei Heptares, UK
|12:20||Lunch, exhibition and posters|
|12:30||Evotec site tour 1: Drug Discovery tour (pre-booking required, 45 minutes, lunch box)|
|12:30||Evotec site tour 2: Drug Development tour (pre-booking required, 45 minutes, lunch box)|
|Session chair: Nadia Ahmad, Charles River Laboratories, UK|
|13:30||Novel paradigms of allostery and bias at Class A GPCRs
Keynote: Celine Valant, Monash University, AU
|14:20||Impact of GPCR structure-based drug discovery on identification and optimisation of allosteric modulators that bind at the receptor-membrane interface
Anna Cooper, Sosei Heptares, UK
|14:50||Refreshments, exhibition and posters|
|15:20||GPCR-based drug design with fragment molecular orbital method
Alexander Heifetz, Evotec, UK
|15:50||Achieving fine control of GPCR function via learning and simulation of 3D structure
Keynote: Ron Dror, Stanford University, US (virtual speaker)
|16:45||Coaches depart for evening visits|
|17:35||Arrive vineyard, cellar tour, aperitif|
|22.00||Arrive Giardini Pradaval|
Friday, 7th October
|Session chair: Daniele Andreotti, Evotec, IT|
|09.30||Tools for studying purine-activated and related orphan G protein-coupled receptors
Keynote: Christa Müller, University of Bonn, DE
|10:20||Identification of H4R antagonist HTL0032547 as a potential therapy for atopic dermatitis
Charlotte Fieldhouse, Sosei Heptares, UK
|10:50||Refreshments, exhibition and posters|
|11:25||Discovery of VU6028418: a highly selective and orally bioavailable M4 muscarinic acetylcholine receptor antagonist
Aaron Bender, Vanderbilt University, US
|11:55||Discovery of Pecavaptan: a novel dual acting vasopressin V1a/V2 receptor antagonist for the treatment of worsening chronic heart failure
Carsten Schmeck, Bayer, DE
|12:25||Lunch, exhibition and posters|
|Session chair: Caroline Low, Isomorphic Laboratories, UK|
|13:20||Selection of a clinical candidate profile based on GPCR signalling pathways: discovery of FPR2 agonist BMS-986331
Nick Wurtz, Bristol-Myers Squibb, US
|13:50||Salipro DirectMX® enables discovery of novel therapeutics against GPCRs
Robin Löving, Salipro, SE
|14:20||Closing remarks by Caroline Low, Co-chair of the Organising Committee|
|14:30||Coaches depart for railway station and airport|
Registration and the Pandemic
This event was held at the Evotec Campus Levi-Montalcini in Verona, Italy, with a small number of virtual speakers. Should the COVID situation have impaired a face-to-face meeting, it would have been re-organised as a virtual event. Those who did not wish to attend the meeting in a virtual format would have been refunded in full; and those registered delegates who did wish to attend the rearranged virtual meeting would have been given partial refunds.
Registration is closed. There was an option for Exhibitor and Sponsor registrations at the foot of the registration page, and you may have paid by card or requested an invoice for settlement by bank transfer. Registration fee were:
Early rate, for payment by 4th July:
£500 Member* of the RSC or SCI
£200 Student** member, unemployed member, retired member
£300 Student** non-member, unemployed non-member, retired non-member
Standard rate, for payment between 5th July and 5th September:
£600 Member* of the RSC or SCI
£250 Student** member, unemployed member, retired member
£350 Student** non-member, unemployed non-member, retired non-member
Late rate, for payment from 6th September (due prior to event):
£675 Member* of the RSC or SCI
£325 Student** member, unemployed member, retired member
£425 Student** non-member, unemployed non-member, retired non-member
Registration closing dates:
Online registration (card payments): Friday, 30th September 2022 at 17:00 (BST)
Registration against invoice (bank transfers): Tuesday, 6th September 2022
* Member is a paid-up member of the RSC or SCI
** Student rates apply to undergraduate and post-graduate students only, but not post-doctoral students or students in full-time employment.
Registration fees included:
– coach transport between Verona city centre and the Evotec campus at the start and end of each day
– dinner on Wednesday evening at the Ristorante Trisapori
– vineyard visit and dinner on Thursday evening at Rocca Sveva.
Registrations could be cancelled up to 12:00 (BST) on Tuesday, 20th September when an 80% refund would have been given. Please note that cancellations were only accepted in writing. We regret that there were no refunds for cancellations received after 12:00 (BST) on 20th September.
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.
The RSC BMCS and the SCI offered some student bursaries to cover the registration fee and to contribute towards accommodation and/or travel. Applications were invited from PhD and post-doctoral students studying at an academic institution, preferably members of the RSC, SCI or EFMC.
The closing date for bursary application was 23rd August.
Networking Social Activities and Accommodation
The informal evening dinner on the first evening was a great time to come together to enjoy a traditional three-course meal. The dinner took place on Wednesday, 5th October at Ristorante Trisapori (formerly Scaligero), Via Guglielmo Marconi 7.
A vineyard visit and informal dinner was held on Thursday, 6th October. The visit to Rocca Sveva consisted of a guided tour of the underground cellars of Cantina Soave, an explanation of the wines to be served at dinner, an aperitivo outside the restaurant, an opportunity to use the wine shop, and a fantastic dinner with wine-sampling in the Locanda del Borgo. (Coach transport was provided.)
For all accommodation requests (including last-minute bookings), we suggested using the 24-hour service provided by Verona Booking, using this weblink.
Venue and Travel
Detailed travel information may be found in this Venue Guide.
Please note that Evotec was able to provide wi-fi connection for our exhibitors only, so attendees were asked to make alternative arrangements.
Coaches provided by Conference
A gratis coach service was provided by the conference between Verona city centre (Giardini Pradaval) and Evotec at the beginning and end of each day, and on a daily basis. On Thursday afternoon, the gratis coach service travelled to the vineyard and later back to Verona city centre.
The exhibition space is now fully booked – sorry!
The Exhibitor Package comprised:
– stand space measuring 3 metres wide x 2 metres deep
– table measuring 160 cm wide x 80 cm deep and chair
– electrical and wi-fi access
– your logo and full promotional page in the delegate handbook
– your web-linked company name on this page
– your logo in the rolling slides, shown during the breaks
– full attendance at the technical programme, poster sessions, Wednesday evening dinner, and Thursday evening vineyard visit and dinner.
Important further information about Evotec’s requirements for advance deliveries may be found here.
Exhibitor Packages included full participation in the social activities and charges are below.
£1,600 including one full delegate
£2,000 including two full delegates
Delegate pack inserts, comprising no more than two pages of A4 fixed together, were available to book at a charge of £200 – sponsor provided the inserts.
Sponsors and Supporters
We are grateful to Evotec for their generous support, as well as Vertex, UCB, SB Drug Discovery, Sosei Heptares, Pharmacelera, Charles River, and InSingulo AB.
We are grateful to our supporters:
Daniele Andreotti, Evotec, IT
Adrian Hall (co-chairman), UCB, BE
Duncan Hay (treasurer), Vertex, UK
Caroline Low (co-chairman), Isomorphic Laboratories, UK
Nigel Swain, Sosei Heptares, UK
Secretariat Contact and Further Information
Maggi Churchouse (Mrs), UK